[go: up one dir, main page]

WO2017032111A1 - Use of dihydroxyacetone in preparation of anti-tumour drug - Google Patents

Use of dihydroxyacetone in preparation of anti-tumour drug Download PDF

Info

Publication number
WO2017032111A1
WO2017032111A1 PCT/CN2016/083466 CN2016083466W WO2017032111A1 WO 2017032111 A1 WO2017032111 A1 WO 2017032111A1 CN 2016083466 W CN2016083466 W CN 2016083466W WO 2017032111 A1 WO2017032111 A1 WO 2017032111A1
Authority
WO
WIPO (PCT)
Prior art keywords
cancer
tumor
dihydroxyacetone
group
system tumor
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Ceased
Application number
PCT/CN2016/083466
Other languages
French (fr)
Chinese (zh)
Inventor
张建国
任武贤
王鹏
堐榜琴
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Shanxi Yabao Health Products Co Ltd
Yabao Pharmaceutical Group Corp
Original Assignee
Shanxi Yabao Health Products Co Ltd
Yabao Pharmaceutical Group Corp
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority claimed from CN201510867079.2A external-priority patent/CN106806382B/en
Priority claimed from CN201510867132.9A external-priority patent/CN106474097B/en
Application filed by Shanxi Yabao Health Products Co Ltd, Yabao Pharmaceutical Group Corp filed Critical Shanxi Yabao Health Products Co Ltd
Priority to KR1020187004813A priority Critical patent/KR101965319B1/en
Priority to JP2018503509A priority patent/JP6533866B2/en
Priority to AU2016311704A priority patent/AU2016311704B2/en
Priority to EP16838371.9A priority patent/EP3342406B1/en
Priority to US15/750,726 priority patent/US10300026B2/en
Priority to CA2992629A priority patent/CA2992629C/en
Publication of WO2017032111A1 publication Critical patent/WO2017032111A1/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

Images

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/12Ketones
    • A61K31/121Ketones acyclic
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/28Compounds containing heavy metals
    • A61K31/282Platinum compounds

Definitions

  • the application number is 201510523222.6, the application date is August 24, 2015, the application number is 201510867132.9, the application date is December 1, 2015, and the application number is 201510867079.2.
  • the application date is December 1, 2015, and the application date is The priority of the Chinese Patent Application of the State Intellectual Property Office is hereby incorporated by reference in its entirety for all its purposes as being expressly incorporated herein by reference.
  • the invention belongs to the field of medicines, and in particular relates to a novel use of a compound, in particular to its use in the preparation of a medicament for antitumor.
  • 1,3-Dihydroxyacetone English name 1,3-dihydroxyaeetone or dihydroxyacetone, abbreviated as DHA, is the simplest three-keto syrup, the appearance is white or off-white powdery crystal, has a sweet, cool taste, easy to absorb moisture And decomposed.
  • Dihydroxyacetone has the functions of moisturizing, sunscreen and anti-ultraviolet radiation, can prevent excessive evaporation of skin moisture, and can be used as a raw material for cosmetics, especially as a sunscreen.
  • Dihydroxyacetone is an intermediate product of sugar metabolism and plays an important role in the process of glucose metabolism. It has the effect of reducing body fat and increasing lean meat rate. Supplementation with dihydroxyacetone can increase the body's metabolic rate and fatty acid oxidation, potentially can effectively burn fat and reduce body fat, thus reducing weight, reducing the incidence of related diseases, and improving insulin sensitivity and reducing high cholesterol diet.
  • the level of plasma cholesterol, long-term supplementation can increase blood sugar utilization and save muscle glycogen, and athletes can improve aerobic endurance.
  • DHA dihydroxyacetone
  • Cisplatin chemically known as cis-diaminodichloroplatinum, is a cell cycle non-specific drug that is cytotoxic and inhibits the DNA replication process of cancer cells and damages the structure of its cell membrane. It has a strong broad-spectrum anti-cancer effect. effect. However, its side effects are large, and the clinical manifestations are bone marrow transplantation, leukopenia, strong gastrointestinal reactions, nausea, vomiting, diarrhea, etc., irreversible Renal toxicity and kidney failure, neurotoxicity, allergic reactions, electrolyte imbalances, etc. Although cisplatin is so toxic, it is still the first line of clinical treatment of solid tumors due to its exact broad-spectrum anti-tumor effect.
  • the present invention aims to solve at least one of the technical problems in the related art to some extent.
  • This invention relates to new uses of dihydroxyacetone.
  • the novel use of the present invention mainly includes the use of dihydroxyacetone in the preparation of antitumor drugs.
  • the novel use of dihydroxyacetone provided by the present invention exhibits relatively good activity against various cancers.
  • dihydroxyacetone has been widely used in human body and is a chemical substance with good safety. Therefore, the new use provided by the present invention has newly expanded the application of the substance in human body, and is expected to be in health food, medicine, etc. The field gets more applications.
  • the antitumor type of dihydroxyacetone provided by the present invention is not particularly limited, and examples thereof include malignant melanoma, malignant lymphoma, digestive organ cancer, lung cancer, esophageal cancer, gastric cancer, colon cancer, rectal cancer, colon cancer, and ureteral tumor.
  • Gallbladder cancer Gallbladder cancer, biliary tract cancer, breast cancer, liver cancer, pancreatic cancer, testicular tumor, upper jaw cancer, tongue cancer, lip cancer, oral cancer, laryngeal cancer, laryngeal cancer, ovarian cancer, uterine cancer, prostate cancer, thyroid cancer, brain tumor, sarcoma , hemangioma, leukemia, polycythemia vera, neuroblastoma, retinoblastoma, myeloma, bladder tumor, osteosarcoma, muscle tumor, skin cancer, basal cell carcinoma, cutaneous cancer, skin metastasis, skin Melanoma and the like.
  • the tumor may be a nervous system tumor including, but not limited to, neuroblastoma, glioma.
  • the tumor may be a digestive system tumor including, but not limited to, colon cancer, rectal cancer, liver cancer, gastric cancer, pancreatic cancer.
  • the tumor may be a reproductive, urinary system tumor including, but not limited to, cervical cancer, breast cancer, ovarian cancer, prostate cancer, bladder cancer.
  • the tumor may be a skin and bone, joint system tumor, including but not limited to melanoma, epidermal squamous cell carcinoma, rhabdomyosarcoma, multiple myeloma, sarcoma.
  • the tumor may be a respiratory tumor, including but not limited to lung cancer, throat cancer, oral cancer.
  • the tumor can be a blood and gland tumor, including but not limited to leukemia, lymphoma, thyroid cancer.
  • the invention provides the use of dihydroxyacetone for the preparation of a medicament for the treatment of a tumor.
  • the tumor comprises a tumor selected from the group consisting of a nervous system tumor, a digestive system tumor, a reproductive system tumor, a urinary system tumor, a skin tumor, a bone tumor, a joint system tumor, a respiratory tumor, a blood, and a gland tumor. At least one.
  • the tumor comprises a patient selected from the group consisting of neuroblastoma, glioma, colon cancer, rectal cancer, liver cancer, gastric cancer, pancreatic cancer, cervical cancer, breast cancer, ovarian cancer, prostate cancer, bladder cancer.
  • melanoma epidermal squamous cell carcinoma, rhabdomyosarcoma, multiple myeloma, sarcoma, lung cancer, throat cancer, oral cancer, leukemia, lymphoma, thyroid cancer.
  • the invention provides the use of dihydroxyacetone in the treatment of a tumor.
  • the tumor comprises a tumor selected from the group consisting of a nervous system tumor, a digestive system tumor, a reproductive system tumor, a urinary system tumor, a skin tumor, a bone tumor, a joint system tumor, a respiratory tumor, a blood, and a gland tumor. At least one.
  • the tumor comprises a patient selected from the group consisting of neuroblastoma, glioma, colon cancer, rectal cancer, liver cancer, gastric cancer, pancreatic cancer, cervical cancer, breast cancer, ovarian cancer, prostate cancer, bladder cancer.
  • melanoma epidermal squamous cell carcinoma, rhabdomyosarcoma, multiple myeloma, sarcoma, lung cancer, throat cancer, oral cancer, leukemia, lymphoma, thyroid cancer.
  • the present invention provides a method of treating a tumor comprising administering to a patient dihydroxyacetone.
  • the tumor comprises a tumor selected from the group consisting of a nervous system tumor, a digestive system tumor, a reproductive system tumor, a urinary system tumor, a skin tumor, a bone tumor, a joint system tumor, a respiratory tumor, a blood, and a gland tumor. At least one.
  • the tumor comprises a patient selected from the group consisting of neuroblastoma, glioma, colon cancer, rectal cancer, liver cancer, gastric cancer, pancreatic cancer, cervical cancer, breast cancer, ovarian cancer, prostate cancer, bladder cancer.
  • melanoma epidermal squamous cell carcinoma, rhabdomyosarcoma, multiple myeloma, sarcoma, lung cancer, throat cancer, oral cancer, leukemia, lymphoma, thyroid cancer.
  • the present invention provides an antitumor pharmaceutical composition comprising dihydroxyacetone as an active ingredient.
  • the tumor comprises a tumor selected from the group consisting of a nervous system tumor, a digestive system tumor, a reproductive system tumor, a urinary system tumor, a skin tumor, a bone tumor, a joint system tumor, a respiratory tumor, a blood, and a gland tumor. At least one.
  • the tumor comprises a patient selected from the group consisting of neuroblastoma, glioma, colon cancer, rectal cancer, liver cancer, gastric cancer, pancreatic cancer, cervical cancer, breast cancer, ovarian cancer, prostate cancer and bladder cancer.
  • a patient selected from the group consisting of neuroblastoma, glioma, colon cancer, rectal cancer, liver cancer, gastric cancer, pancreatic cancer, cervical cancer, breast cancer, ovarian cancer, prostate cancer and bladder cancer.
  • the invention provides an anti-tumor application of a combination of dihydroxyacetone and cisplatin.
  • the present invention provides an antitumor pharmaceutical composition
  • dihydroxyacetone and cisplatin as active ingredients.
  • Dihydroxyacetone and cisplatin have a certain synergistic effect in the treatment of tumors.
  • the combination of dihydroxyacetone and cisplatin is superior to the treatment of tumors with dihydroxyacetone or cisplatin alone, and dihydroxyacetone does not increase the side effects of cisplatin.
  • the tumor comprises a tumor selected from the group consisting of a nervous system tumor, a digestive system tumor, a reproductive system tumor, a urinary system tumor, a skin tumor, a bone tumor, a joint system tumor, a respiratory tumor, a blood, and a gland tumor. At least one.
  • the tumor comprises a patient selected from the group consisting of neuroblastoma, glioma, colon cancer, rectal cancer, liver cancer, gastric cancer, pancreatic cancer, cervical cancer, breast cancer, ovarian cancer, prostate cancer and bladder cancer.
  • a patient selected from the group consisting of neuroblastoma, glioma, colon cancer, rectal cancer, liver cancer, gastric cancer, pancreatic cancer, cervical cancer, breast cancer, ovarian cancer, prostate cancer and bladder cancer.
  • the present invention provides an antitumor drug combination consisting of dihydroxyacetone and cisplatin.
  • Dihydroxyacetone and cisplatin have a certain synergistic effect in the treatment of tumors.
  • the combination of dihydroxyacetone and cisplatin is superior to the treatment of tumors with dihydroxyacetone or cisplatin alone, and dihydroxyacetone does not increase the side effects of cisplatin.
  • the dihydroxyacetone in the pharmaceutical combination may be in the form of an oral preparation, and the cisplatin may be in the form of an injection.
  • the tumor comprises a tumor selected from the group consisting of a nervous system tumor, a digestive system tumor, a reproductive system tumor, a urinary system tumor, a skin tumor, a bone tumor, a joint system tumor, a respiratory tumor, a blood, and a gland tumor. At least one.
  • the tumor comprises a patient selected from the group consisting of neuroblastoma, glioma, colon cancer, rectal cancer, liver cancer, gastric cancer, pancreatic cancer, cervical cancer, breast cancer, ovarian cancer, prostate cancer and bladder cancer.
  • a patient selected from the group consisting of neuroblastoma, glioma, colon cancer, rectal cancer, liver cancer, gastric cancer, pancreatic cancer, cervical cancer, breast cancer, ovarian cancer, prostate cancer and bladder cancer.
  • the present invention provides the use of dihydroxyacetone for the preparation of a medicament for use in anti-tumor, simultaneous administration of dihydroxyacetone and cisplatin to a subject.
  • the mode of administration can be according to their respective conventional routes of administration. Diameter, usage and frequency.
  • the tumor comprises a tumor selected from the group consisting of a nervous system tumor, a digestive system tumor, a reproductive system tumor, a urinary system tumor, a skin tumor, a bone tumor, a joint system tumor, a respiratory tumor, a blood, and a gland tumor. At least one.
  • the tumor comprises a patient selected from the group consisting of neuroblastoma, glioma, colon cancer, rectal cancer, liver cancer, gastric cancer, pancreatic cancer, cervical cancer, breast cancer, ovarian cancer, prostate cancer and bladder cancer.
  • a patient selected from the group consisting of neuroblastoma, glioma, colon cancer, rectal cancer, liver cancer, gastric cancer, pancreatic cancer, cervical cancer, breast cancer, ovarian cancer, prostate cancer and bladder cancer.
  • the present invention provides the use of dihydroxyacetone in the treatment of a tumor, wherein the subject is simultaneously administered with dihydroxyacetone and cisplatin.
  • the mode of administration can be in accordance with their respective usual routes of administration, dosage and frequency.
  • the tumor comprises a tumor selected from the group consisting of a nervous system tumor, a digestive system tumor, a reproductive system tumor, a urinary system tumor, a skin tumor, a bone tumor, a joint system tumor, a respiratory tumor, a blood, and a gland tumor. At least one.
  • the tumor comprises a patient selected from the group consisting of neuroblastoma, glioma, colon cancer, rectal cancer, liver cancer, gastric cancer, pancreatic cancer, cervical cancer, breast cancer, ovarian cancer, prostate cancer and bladder cancer.
  • a patient selected from the group consisting of neuroblastoma, glioma, colon cancer, rectal cancer, liver cancer, gastric cancer, pancreatic cancer, cervical cancer, breast cancer, ovarian cancer, prostate cancer and bladder cancer.
  • the present invention provides a method of treating a tumor comprising administering to a patient dihydroxyacetone, wherein the subject is simultaneously administered with dihydroxyacetone and cisplatin.
  • the mode of administration can be in accordance with their respective usual routes of administration, dosage and frequency.
  • the tumor comprises a tumor selected from the group consisting of a nervous system tumor, a digestive system tumor, a reproductive system tumor, a urinary system tumor, a skin tumor, a bone tumor, a joint system tumor, a respiratory tumor, a blood, and a gland tumor. At least one.
  • the tumor comprises a patient selected from the group consisting of neuroblastoma, glioma, colon cancer, rectal cancer, liver cancer, gastric cancer, pancreatic cancer, cervical cancer, breast cancer, ovarian cancer, prostate cancer and bladder cancer.
  • a patient selected from the group consisting of neuroblastoma, glioma, colon cancer, rectal cancer, liver cancer, gastric cancer, pancreatic cancer, cervical cancer, breast cancer, ovarian cancer, prostate cancer and bladder cancer.
  • the present invention provides the use of a combination of dihydroxyacetone and cisplatin for the preparation of a medicament for use in anti-tumor.
  • Dihydroxyacetone and cisplatin have a certain synergistic effect in the treatment of tumors.
  • the combination of dihydroxyacetone and cisplatin is superior to the treatment of tumors with dihydroxyacetone or cisplatin alone, and dihydroxyacetone does not increase the side effects of cisplatin.
  • the tumor comprises a tumor selected from the group consisting of a nervous system tumor, a digestive system tumor, a reproductive system tumor, a urinary system tumor, a skin tumor, a bone tumor, a joint system tumor, a respiratory tumor, a blood, and a gland tumor. At least one.
  • the tumor comprises a patient selected from the group consisting of neuroblastoma, glioma, colon cancer, rectal cancer, liver cancer, gastric cancer, pancreatic cancer, cervical cancer, breast cancer, ovarian cancer, prostate cancer and bladder cancer.
  • a patient selected from the group consisting of neuroblastoma, glioma, colon cancer, rectal cancer, liver cancer, gastric cancer, pancreatic cancer, cervical cancer, breast cancer, ovarian cancer, prostate cancer and bladder cancer.
  • the invention provides the use of a combination of dihydroxyacetone and cisplatin in the treatment of a tumor.
  • Dihydroxyacetone and cisplatin have a certain synergistic effect in the treatment of tumors.
  • the combination of dihydroxyacetone and cisplatin is superior to the treatment of tumors with dihydroxyacetone or cisplatin alone, and dihydroxyacetone does not increase the side effects of cisplatin.
  • the tumor comprises a tumor selected from the group consisting of a nervous system tumor, a digestive system tumor, a reproductive system tumor, a urinary system tumor, a skin tumor, a bone tumor, a joint system tumor, a respiratory tumor, a blood, and a gland tumor. At least one.
  • the tumor comprises a patient selected from the group consisting of neuroblastoma, glioma, colon cancer, rectal cancer, liver cancer, gastric cancer, pancreatic cancer, cervical cancer, breast cancer, ovarian cancer, prostate cancer and bladder cancer.
  • a patient selected from the group consisting of neuroblastoma, glioma, colon cancer, rectal cancer, liver cancer, gastric cancer, pancreatic cancer, cervical cancer, breast cancer, ovarian cancer, prostate cancer and bladder cancer.
  • the present invention provides a method of treating a tumor comprising administering to a patient a combination of dihydroxyacetone and cisplatin.
  • Dihydroxyacetone and cisplatin have a certain synergistic effect in the treatment of tumors.
  • the combination of dihydroxyacetone and cisplatin is superior to the treatment of tumors with dihydroxyacetone or cisplatin alone, and dihydroxyacetone does not increase the side effects of cisplatin.
  • the tumor comprises a tumor selected from the group consisting of a nervous system tumor, a digestive system tumor, a reproductive system tumor, a urinary system tumor, a skin tumor, a bone tumor, a joint system tumor, a respiratory tumor, a blood, and a gland tumor. At least one.
  • the tumor comprises a patient selected from the group consisting of neuroblastoma, glioma, colon cancer, rectal cancer, liver cancer, gastric cancer, pancreatic cancer, cervical cancer, breast cancer, ovarian cancer, prostate cancer and bladder cancer.
  • a patient selected from the group consisting of neuroblastoma, glioma, colon cancer, rectal cancer, liver cancer, gastric cancer, pancreatic cancer, cervical cancer, breast cancer, ovarian cancer, prostate cancer and bladder cancer.
  • the present invention provides a kit for antitumor comprising dihydroxyacetone and cisplatin.
  • Dihydroxyacetone and cisplatin have a synergistic effect in the treatment of tumors.
  • the combination of dihydroxyacetone and cisplatin is more effective than tumor treatment with dihydroxyacetone or cisplatin alone, and dihydroxyacetone does not increase cisplatin. toxic side effect.
  • the dihydroxyacetone and cisplatin in the kit are placed in separate containers.
  • the dihydroxyacetone is in the form of an oral preparation and the cisplatin is in the form of an injection.
  • the weight ratio of dihydroxyacetone to cisplatin in the kit is (3375-4125):1.
  • the weight ratio of dihydroxyacetone to cisplatin is 3750:1.
  • the tumor comprises a tumor selected from the group consisting of a nervous system tumor, a digestive system tumor, a reproductive system tumor, a urinary system tumor, a skin tumor, a bone tumor, a joint system tumor, a respiratory tumor, a blood, and a gland tumor. At least one.
  • the tumor comprises a patient selected from the group consisting of neuroblastoma, glioma, colon cancer, rectal cancer, liver cancer, gastric cancer, pancreatic cancer, cervical cancer, breast cancer, ovarian cancer, prostate cancer and bladder cancer.
  • a patient selected from the group consisting of neuroblastoma, glioma, colon cancer, rectal cancer, liver cancer, gastric cancer, pancreatic cancer, cervical cancer, breast cancer, ovarian cancer, prostate cancer and bladder cancer.
  • the invention provides the use of a combination of dihydroxyacetone and cisplatin for the preparation of a kit for use in anti-tumor.
  • the tumor comprises a tumor selected from the group consisting of a nervous system tumor, a digestive system tumor, a reproductive system tumor, a urinary system tumor, a skin tumor, a bone tumor, a joint system tumor, a respiratory tumor, a blood, and a gland tumor. At least one.
  • the tumor comprises a patient selected from the group consisting of neuroblastoma, glioma, colon cancer, rectal cancer, liver cancer, gastric cancer, pancreatic cancer, cervical cancer, breast cancer, ovarian cancer, prostate cancer and bladder cancer.
  • a patient selected from the group consisting of neuroblastoma, glioma, colon cancer, rectal cancer, liver cancer, gastric cancer, pancreatic cancer, cervical cancer, breast cancer, ovarian cancer, prostate cancer and bladder cancer.
  • the application provided by the present invention includes both the application in malignant tumors and the application in benign tumors.
  • dihydroxyacetone can be used to inhibit cancer metastasis and is particularly useful as a post-surgical cancer metastasis inhibitor.
  • dihydroxyacetone as used herein is to be understood broadly, that is, it may include dihydroxyacetone in a monomeric form, and should also cover the common forms of dihydroxyacetone, such as various crystal forms, Dimer or multimer, hydrate, etc.
  • the dihydroxyacetone may be a monomer, a dimer or a multimer.
  • dihydroxyacetone can be administered in human or animal in various forms, and can be oral, intravenous, intramuscular, subcutaneous or intradermal, intrarectal, mucosal, etc. the way.
  • the form of the oral preparation can be exemplified by tablets, pills, granules, powders, capsules, oral liquids, suspensions, emulsions, syrups. Wait.
  • the non-oral preparation may, for example, be a transdermal absorption agent such as an injection, a drop, a nasal drop, an inhalant, a suppository, an ointment, a cream, a powder coating agent or a patch.
  • the use of the present invention also includes the incorporation of dihydroxyacetone into a pellet and a sustained release formulation prepared using known techniques.
  • the medicament of the present invention is suitably used in the form of a pharmaceutical composition.
  • Such compositions may be combined in a conventional manner with one or more pharmaceutically acceptable carriers or excipients. If possible, dihydroxyacetone is administered as a drug substance therapeutically.
  • a pharmaceutically acceptable carrier can be added as needed.
  • Dihydroxyacetone is used as one of the main or main drugs.
  • the pharmaceutical composition of the present invention may contain a pharmaceutically acceptable carrier as needed, wherein dihydroxyacetone is a pharmaceutically active ingredient, which may be 0.01-99.99% by weight in the preparation, and the balance being a pharmaceutically acceptable carrier.
  • the pharmaceutical preparation of the present invention is in the form of a unit dosage form, which means a unit of the preparation, such as each tablet of the tablet, each capsule of the capsule, each bottle of the oral solution, granules per bag, and each injection. Branch and so on.
  • the pharmaceutical composition of the present invention may contain conventional excipients such as a binder, a filler, a diluent, a tablet, a lubricant, a disintegrant, a coloring agent, a flavoring agent, and a moisturizing agent.
  • a binder such as a polyethylene glycol dimethacrylate, polyethylene glycol dimethacrylate, polypropylene glycol dimethacrylate, a steaglycerin, glycerin, glycerin, glycerin, glycerin, glycerin, glycerin, glycerin, glycerin, a talct, talct, talct, talct, talct, talct copolymer, graft copolymer, graft copolymer, graft copolymer, graft copolymer, graft copolymer, graft copolymer,
  • Suitable fillers include cellulose, mannitol, lactose and other similar fillers.
  • Suitable disintegrants include starch, polyvinylpyrrolidone and starch derivatives such as sodium starch glycolate.
  • Suitable lubricants include, for example, magnesium stearate.
  • Suitable pharmaceutically acceptable wetting agents include sodium lauryl sulfate.
  • Solid oral compositions can be prepared by conventional methods such as mixing, filling, tableting, and the like. Repeated mixing allows the active material to be distributed throughout those compositions that use large amounts of filler.
  • the oral liquid preparation may be in the form of, for example, an aqueous or oily suspension, solution, emulsion, syrup or elixir, or may be a dry product which may be formulated with water or other suitable carrier before use.
  • Such liquid preparations may contain conventional additives such as suspending agents such as sorbitol, syrup, methylcellulose, gelatin, hydroxyethylcellulose, carboxymethylcellulose, aluminum stearate gel or hydrogenated edible fats.
  • Emulsifiers such as lecithin, sorbitan monooleate or gum arabic; non-aqueous vehicles (which may include edible oils), such as almond oil, fractionated coconut oil, oily esters of esters such as glycerol, propylene glycol or ethanol;
  • the agent for example, p-hydroxybenzyl or propylparaben or sorbic acid, and if desired, may contain conventional flavoring or coloring agents.
  • the liquid unit dosage form prepared contains the active substance of the invention and a sterile vehicle.
  • This compound can be suspended or dissolved depending on the carrier and concentration.
  • the solution is usually prepared by dissolving the active substance in a carrier, sterilizing it by filtration before filling it into a suitable vial or ampoule, and then sealing. Excipients such as a local anesthetic, preservative and buffer may also be dissolved in such a carrier.
  • the composition can be frozen after filling the vial and the water removed under vacuum.
  • the pharmaceutical composition of the present invention may optionally be added to a suitable pharmaceutically acceptable carrier when prepared as a medicament, the pharmaceutically acceptable carrier being selected from the group consisting of: mannitol, sorbitol, sodium metabisulfite, sodium hydrogen sulfite, sulfur Sodium sulfate, cysteine hydrochloride, thioglycolic acid, methionine, vitamin C, disodium EDTA, calcium EDTA, monovalent alkali metal carbonate, acetate, phosphate or its aqueous solution, hydrochloric acid, acetic acid, sulfuric acid , phosphoric acid, amino acid, sodium chloride, potassium chloride, sodium lactate, xylitol, maltose, glucose, fructose, dextran, glycine, starch, sucrose, lactose, mannitol, silicon derivatives, cellulose and their derivatives , alginate, gelatin, polyvinylpyrrolidone, glycerin,
  • Example 1 is a graph showing IC50 results of dihydroxyacetone to H460, HT29, and SGC7901 cell lines according to Example 1 of the present invention
  • Example 2 is an IC 50 statistical result of dihydroxyacetone to HepG2, HCT116, SH-SY5Y, C-33A, and MDA-MB-231 cell lines according to Example 1 of the present invention.
  • Figure 3 is a graph showing statistical results of relative tumor volume of each group in Example 13 according to the present invention.
  • Figure 4 is a graph showing the results of body weight statistics of each group of experimental animals in Example 13 according to the present invention.
  • Figure 5 is a graph showing statistical results of tumor weight of each group in Example 13 according to the present invention.
  • Figure 6 is a schematic illustration of a medicine cartridge in accordance with Example 16 of the present invention.
  • Control compound cisplatin (DDP): Qilu Pharmaceutical Co., Ltd., batch number: 2WA2A1404016A, 20 mg/bottle; a 1 mg/ml stock solution was prepared using a 5% dextrose solution and stored at -20 °C.
  • DDP cisplatin
  • batch number 2WA2A1404016A, 20 mg/bottle
  • a 1 mg/ml stock solution was prepared using a 5% dextrose solution and stored at -20 °C.
  • the sample was diluted to different concentrations in RPMI-1640 medium, and then used by German LOSER ice point osmotic pressure The instrument measures the osmotic pressure of the sample.
  • the cells were diluted to 1.25 ⁇ 10 5 /ml, inoculated into 384-well plates (5000 cells/well) at 40 ⁇ l per well, then centrifuged at 1500 rpm for 1 min, and placed in an incubator for incubation. overnight.
  • the luminescence cell viability assay kit detects cell viability.
  • the concentration of the cells administered is as follows:
  • the cell viability calculation formula is as follows:
  • Viability% 100% ⁇ (LUM sample to be tested - LUM blank ) / (LUM solvent control - LUM blank )
  • N/A means that IC 50 is not obtained.
  • dihydroxyacetone has a broad spectrum of anti-tumor cell proliferation effects, and the IC 50 (semi-inhibitory concentration) values can be obtained for the 34 common tumor cell lines involved in the experiment. It shows that dihydroxyacetone has different inhibitory effects on common tumors, especially for sarcoma, neuroblastoma, myeloma, colon cancer, lung cancer, stomach cancer, leukemia and thyroid tumor.
  • the novel use of the dihydroxyacetone provided by the present invention exhibits relatively good activity against various cancers.
  • dihydroxyacetone has been widely used in human body and is a chemical substance with good safety. Therefore, the new use provided by the present invention has newly expanded the application of the substance in human body, and is expected to be in health food, medicine, etc. The field gets more applications.
  • dihydroxyacetone is added to a pharmaceutical carrier and prepared according to conventional techniques of preparation, such as the following preparation method:
  • dihydroxyacetone is added to a pharmaceutical carrier and prepared according to conventional techniques of preparation, such as the following preparation method:
  • dihydroxyacetone is added to a pharmaceutical carrier and prepared according to conventional techniques of preparation, such as the following preparation method:
  • dihydroxyacetone is added to a pharmaceutical carrier and prepared according to conventional techniques of preparation, such as the following preparation method:
  • dihydroxyacetone is added to a pharmaceutical carrier and prepared according to conventional techniques of preparation, such as the following preparation method:
  • dihydroxyacetone is added to a pharmaceutical carrier and prepared according to conventional techniques of preparation, such as the following preparation method:
  • dihydroxyacetone is added to a pharmaceutical carrier and prepared according to conventional techniques of preparation, such as the following preparation method:
  • dihydroxyacetone is added to a pharmaceutical carrier and prepared according to conventional techniques of preparation, such as the following preparation method:
  • dihydroxyacetone is added to a pharmaceutical carrier and prepared according to conventional techniques of preparation, such as the following preparation method:
  • dihydroxyacetone is added to a pharmaceutical carrier and prepared according to conventional techniques of preparation, such as the following preparation method:
  • dihydroxyacetone is added to a pharmaceutical carrier and prepared according to conventional techniques of preparation, such as the following preparation method:
  • Cisplatin for injection batch number: 2WA2A1408055A, manufacturer: Qilu Pharmaceutical Co., Ltd., specification: 20mg/bottle
  • mice Balb/c-nude nude mice, SPF grade
  • Nude mice were subcutaneously inoculated with H460 cells (human large cell lung cancer cell line). When the tumor grew to a volume of about 100 mm 3 , 36 nude mice with similar tumor volume and good shape were selected from 70 nude mice, and divided into 6 groups. Group of 6 animals;
  • DHA group p.o., administration volume is 0.1mL/10g, bid, for three weeks;
  • DHA+Cisplatin group dihydroxyacetone (DHA): po, administration volume 0.1 mL/10 g, bid; Cisplatin: 4 mg/kg, injection volume 0.1 mL/10 g, ip, once every 5 days for 3 weeks ;
  • Cisplatin group 4 mg/kg, injection volume 0.1 mL/10 g, i.p, once every 5 days for a total of three weeks;
  • Blank group 0.9% sodium chloride injection, the same as the DHA group.
  • nude mice were injected subcutaneously on the right side of the back, 0.1 mL/only, that is, the number of cells per nude mouse was 2 ⁇ 10 6 ;
  • DHA Weigh 15.0 g of solid powder in a 100 mL volumetric flask, dilute to the mark with 5% glucose injection, and shake until ultrasonically dissolved completely. Refrigerated at 4 ° C when not in use.
  • DHA+Cisplatin Weigh 15.0 g of solid powder dihydroxyacetone in a 100 mL volumetric flask, dilute to the mark with 5% glucose injection, and shake until ultrasonically dissolved completely. A solution of 0.6 mg/mL cisplatin solution 4.0 mL and 2.0 mL of physiological saline was added to prepare a 0.4 mg/mL (4 mg/kg) cisplatin solution, which was chilled at 4 ° C when not used.
  • Tumor volume and body weight were measured 3 times per week from the first day of administration. On the 22nd day, the nude mice were sacrificed, the tumors were removed and photographed, and the tumor inhibition rate was calculated.
  • Tumor volume change ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇
  • RTV TV t /TV 1 , where TV 1 is the tumor volume when the cage is administered (ie, d 1 ), and TV t is the tumor volume at each measurement.
  • T TW tumor weight of treatment group
  • C TW tumor weight of blank control group
  • TW (tumor weight) tumor weight.
  • Table 2 Number of animals, body weight, tumor volume (TV), relative tumor volume (RTV), relative tumor growth rate (T/C)
  • the DHA+Cisplatin group was significantly more potent in the human large cell lung cancer H460 cell xenograft model than the Cisplatin group, and did not increase the toxicity of the chemical cisplatin. It is believed that DHA can be combined with the chemical cisplatin. Play a better anti-tumor effect.
  • DHA dihydroxyacetone
  • 300 g of DHA, 200 g of hypromellose was added, and 40 tablets of tablets were prepared by a conventional method, and sealed.
  • 0.0792 g of cisplatin and 0.7 g of sodium chloride were added to 80 ml of distilled water, and aseptically packaged as 4 injections.
  • DHA tablets and cisplatin injections are placed in the same package and packaged as a kit in a conventional manner.
  • DHA dihydroxyacetone
  • Cisplatin 0.076g, divided into 4 parts on average, sealed package as a vial. When used, it is dissolved by glucose for injection. DHA orally, 0.13g / kg (calculated according to human body weight of 60kg, the same below), twice a day, continuous use for 20 days. Intravenous infusion or intramuscular injection of cisplatin, 0.317mg/kg, once every 5 days.
  • the anti-tumor kit is shown in Figure 6.
  • the vial (101) contains 4 vials (102), which are respectively sealed with 5 ml of cisplatin injection (concentration 3.98 mg/ml). Another 40 sealed packaging bags (103) were provided with 6.75 g of dihydroxyacetone particles. A sterile syringe (104) and a medication cup (105) are also provided in the kit. When in use, the dihydroxyacetone particles are placed in the medication cup (105), dissolved in an appropriate amount of water, orally administered after meals, 112.5 mg/kg twice a day. Cisplatin was intramuscularly injected with a syringe (104) at 0.339 mg/kg once every 5 days.
  • first and second are used for descriptive purposes only, and are not to be construed as indicating or implying a relative importance or implicitly indicating the number of technical features indicated. Thus, features defining “first” and “second” may include one or more of the features either explicitly or implicitly. Further, in the description of the present invention, the meaning of "a plurality" is two or more unless otherwise specified.

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Provided is a use of dihydroxyacetone in the preparation of a drug, the drug being used for treating a tumour.

Description

二羟基丙酮在制备抗肿瘤的药物中的用途Use of dihydroxyacetone in the preparation of antitumor drugs

优先权信息Priority information

本申请要求申请号为201510523222.6,申请日为2015年8月24日,申请号为201510867132.9,申请日为2015年12月1日和申请号为201510867079.2,申请日为2015年12月1日,递交至国家知识产权局的中国专利申请的优先权,其通过参考的方式以其全文并入此处并且用于犹如本文所明确并且完全陈述的所有目的。The application number is 201510523222.6, the application date is August 24, 2015, the application number is 201510867132.9, the application date is December 1, 2015, and the application number is 201510867079.2. The application date is December 1, 2015, and the application date is The priority of the Chinese Patent Application of the State Intellectual Property Office is hereby incorporated by reference in its entirety for all its purposes as being expressly incorporated herein by reference.

技术领域Technical field

本发明属于药物领域,具体涉及一种化合物的新用途,特别涉及其在制备抗肿瘤的药物中的用途。The invention belongs to the field of medicines, and in particular relates to a novel use of a compound, in particular to its use in the preparation of a medicament for antitumor.

背景技术Background technique

1,3-二羟基丙酮,英文名1,3-dihydroxyaeetone或dihydroxyacetone,简写为DHA,是最简单的三碳酮糖,外观是白色或类白色粉末状结晶,具有甜、凉的味道,易吸湿并分解。一般状态下是二聚体(1,4-Dioxane)的结晶,能缓慢地溶于1份水中或15份乙醇中,微溶于乙醚,但经溶解或加热则变为单体,其单体易溶于水、乙醇、丙酮和乙醚等有机溶剂,熔点为75~80℃,水溶性>250g·L-1(20℃),在pH为6.0时稳定,是一种重要的化工、生化原料,医药、农药合成中间体和多功能食品添加剂,用途十分广泛。1,3-Dihydroxyacetone, English name 1,3-dihydroxyaeetone or dihydroxyacetone, abbreviated as DHA, is the simplest three-keto syrup, the appearance is white or off-white powdery crystal, has a sweet, cool taste, easy to absorb moisture And decomposed. In general, it is a crystal of dimer (1,4-Dioxane), which can be slowly dissolved in 1 part of water or 15 parts of ethanol, slightly soluble in ether, but becomes monomer after dissolution or heating, and its monomer Soluble in water, ethanol, acetone and ether and other organic solvents, melting point of 75 ~ 80 ° C, water solubility > 250g · L -1 (20 ° C), stable at pH 6.0, is an important chemical, biochemical raw materials , pharmaceutical, pesticide synthesis intermediates and multifunctional food additives, the use is very extensive.

二羟基丙酮有保湿、防晒和防紫外线辐射的作用,能阻止皮肤水分的过度蒸发,可以用作化妆品的配方原料,尤其作为防晒霜有特殊效果。二羟基丙酮是糖代谢的中间产物,在糖代谢过程中起着重要作用,具有降低猪体脂肪的作用,提高瘦肉率。补充二羟基丙酮能够提高机体代谢率和脂肪酸氧化,可潜在地有效燃烧脂肪而降低体脂,因而具有减肥作用,并减少相关疾病的发病率,也可以改善胰岛素敏感性和降低高胆固醇膳食所致的血浆胆固醇水平,长期补充可使血糖利用率增加而节省肌糖元,对运动员则可以提高有氧耐力成绩。Dihydroxyacetone has the functions of moisturizing, sunscreen and anti-ultraviolet radiation, can prevent excessive evaporation of skin moisture, and can be used as a raw material for cosmetics, especially as a sunscreen. Dihydroxyacetone is an intermediate product of sugar metabolism and plays an important role in the process of glucose metabolism. It has the effect of reducing body fat and increasing lean meat rate. Supplementation with dihydroxyacetone can increase the body's metabolic rate and fatty acid oxidation, potentially can effectively burn fat and reduce body fat, thus reducing weight, reducing the incidence of related diseases, and improving insulin sensitivity and reducing high cholesterol diet. The level of plasma cholesterol, long-term supplementation can increase blood sugar utilization and save muscle glycogen, and athletes can improve aerobic endurance.

二羟基丙酮(DHA)用途虽然广泛,但目前没有关于其单独或联合用药在抗肿瘤方面效果的报道。Although the use of dihydroxyacetone (DHA) is extensive, there is currently no report on the effect of its use alone or in combination on antitumor effects.

顺铂,化学名为顺式二氨基二氯络铂,属细胞周期非特异性药物,具有细胞毒性,可抑制癌细胞的DNA复制过程,并损伤其细胞膜上结构,有较强的广谱抗癌作用。但其副作用大,临床表现为骨髓移植、白细胞减少,强烈的胃肠道反应、恶心呕吐腹泻等,不可逆 的肾脏毒性和肾衰竭,神经毒性,过敏反应,电解质紊乱等。虽然顺铂有如此强烈的毒性,但是由于其确切的广谱抑瘤作用,目前仍是临床治疗实体瘤的一线用药。Cisplatin, chemically known as cis-diaminodichloroplatinum, is a cell cycle non-specific drug that is cytotoxic and inhibits the DNA replication process of cancer cells and damages the structure of its cell membrane. It has a strong broad-spectrum anti-cancer effect. effect. However, its side effects are large, and the clinical manifestations are bone marrow transplantation, leukopenia, strong gastrointestinal reactions, nausea, vomiting, diarrhea, etc., irreversible Renal toxicity and kidney failure, neurotoxicity, allergic reactions, electrolyte imbalances, etc. Although cisplatin is so toxic, it is still the first line of clinical treatment of solid tumors due to its exact broad-spectrum anti-tumor effect.

然而临床不可能通过一味加大顺铂用量来增强疗效,故建立顺铂的联合用药方案、可以在不增加其毒性的情况下显著增强抑瘤效果,一直是肿瘤医学研究的重要课题。However, it is impossible to enhance the curative effect by increasing the amount of cisplatin in the clinic. Therefore, the establishment of a combination regimen of cisplatin can significantly enhance the antitumor effect without increasing its toxicity, and has been an important topic in oncology research.

发明内容Summary of the invention

本发明旨在至少在一定程度上解决相关技术中的技术问题之一。The present invention aims to solve at least one of the technical problems in the related art to some extent.

本发明涉及二羟基丙酮的新用途。This invention relates to new uses of dihydroxyacetone.

本发明所述的新用途,主要包括二羟基丙酮在制备抗肿瘤的药物中的用途。本发明提供的二羟基丙酮的新用途,其在抗多种癌症方面均表现出比较好的活性。加之二羟基丙酮在人体的应用已经非常广泛,是安全性良好的化学物质,因而本发明所提供的新用途,使得该物质在人体方面的应用得到了新的拓展,有望在保健食品、医药等领域得到更多的应用。The novel use of the present invention mainly includes the use of dihydroxyacetone in the preparation of antitumor drugs. The novel use of dihydroxyacetone provided by the present invention exhibits relatively good activity against various cancers. In addition, dihydroxyacetone has been widely used in human body and is a chemical substance with good safety. Therefore, the new use provided by the present invention has newly expanded the application of the substance in human body, and is expected to be in health food, medicine, etc. The field gets more applications.

本发明提供的二羟基丙酮的抗肿瘤的种类没有特别限定,例如可以列举恶性黑色素瘤、恶性淋巴瘤、消化器官癌、肺癌、食道癌、胃癌、大肠癌、直肠癌、结肠癌、输尿管肿瘤、胆囊癌、胆道癌、乳癌、肝癌、胰腺癌、睾丸肿瘤、上颚癌、舌癌、口唇癌、口腔癌、喉癌、喉头癌、卵巢癌、子宫癌、前列腺癌、甲状腺癌、脑肿瘤、肉瘤、血管瘤、白血病、真性红细胞增多症、神经母细胞瘤、视网膜母细胞瘤、骨髓瘤、膀胱瘤、骨肉瘤、肌肉瘤、皮肤癌、基底细胞癌、皮肤附属器官癌、皮肤转移癌、皮肤黑色素瘤等。The antitumor type of dihydroxyacetone provided by the present invention is not particularly limited, and examples thereof include malignant melanoma, malignant lymphoma, digestive organ cancer, lung cancer, esophageal cancer, gastric cancer, colon cancer, rectal cancer, colon cancer, and ureteral tumor. Gallbladder cancer, biliary tract cancer, breast cancer, liver cancer, pancreatic cancer, testicular tumor, upper jaw cancer, tongue cancer, lip cancer, oral cancer, laryngeal cancer, laryngeal cancer, ovarian cancer, uterine cancer, prostate cancer, thyroid cancer, brain tumor, sarcoma , hemangioma, leukemia, polycythemia vera, neuroblastoma, retinoblastoma, myeloma, bladder tumor, osteosarcoma, muscle tumor, skin cancer, basal cell carcinoma, cutaneous cancer, skin metastasis, skin Melanoma and the like.

根据本发明具体实施例,肿瘤可以为神经系统肿瘤,包括但不限于神经母细胞癌、胶质瘤。According to a particular embodiment of the invention, the tumor may be a nervous system tumor including, but not limited to, neuroblastoma, glioma.

根据本发明具体实施例,肿瘤可以为消化系统肿瘤,包括但不限于结肠癌、直肠癌、肝癌、胃癌、胰腺癌。According to a particular embodiment of the invention, the tumor may be a digestive system tumor including, but not limited to, colon cancer, rectal cancer, liver cancer, gastric cancer, pancreatic cancer.

根据本发明具体实施例,肿瘤可以为生殖、泌尿系统肿瘤,包括但不限于宫颈癌、乳腺癌、卵巢癌、前列腺癌、膀胱癌。According to a particular embodiment of the invention, the tumor may be a reproductive, urinary system tumor including, but not limited to, cervical cancer, breast cancer, ovarian cancer, prostate cancer, bladder cancer.

根据本发明具体实施例,肿瘤可以为皮肤及骨、关节系统肿瘤,包括但不限于黑色素瘤、表皮鳞状细胞癌、横纹肌瘤、多发性骨髓瘤、肉瘤。According to a specific embodiment of the present invention, the tumor may be a skin and bone, joint system tumor, including but not limited to melanoma, epidermal squamous cell carcinoma, rhabdomyosarcoma, multiple myeloma, sarcoma.

根据本发明具体实施例,肿瘤可以为呼吸系统肿瘤,包括但不限于肺癌、咽喉癌、口腔癌。According to a particular embodiment of the invention, the tumor may be a respiratory tumor, including but not limited to lung cancer, throat cancer, oral cancer.

根据本发明具体实施例,肿瘤可以为血液及腺体肿瘤,包括但不限于白血病、淋巴瘤、甲状腺癌。 According to a particular embodiment of the invention, the tumor can be a blood and gland tumor, including but not limited to leukemia, lymphoma, thyroid cancer.

根据本发明的一方面,本发明提供了二羟基丙酮在制备药物中的用途,所述药物用于治疗肿瘤。According to an aspect of the invention, the invention provides the use of dihydroxyacetone for the preparation of a medicament for the treatment of a tumor.

根据本发明的一些实施例,所述肿瘤包括选自神经系统肿瘤、消化系统肿瘤、生殖系统肿瘤、泌尿系统肿瘤、皮肤肿瘤、骨肿瘤、关节系统肿瘤、呼吸系统肿瘤、血液及腺体肿瘤的至少一种。According to some embodiments of the invention, the tumor comprises a tumor selected from the group consisting of a nervous system tumor, a digestive system tumor, a reproductive system tumor, a urinary system tumor, a skin tumor, a bone tumor, a joint system tumor, a respiratory tumor, a blood, and a gland tumor. At least one.

根据本发明的具体实施例,所述肿瘤包括选自神经母细胞癌、胶质瘤、结肠癌、直肠癌、肝癌、胃癌、胰腺癌、宫颈癌、乳腺癌、卵巢癌、前列腺癌、膀胱癌、黑色素瘤、表皮鳞状细胞癌、横纹肌瘤、多发性骨髓瘤、肉瘤、肺癌、咽喉癌、口腔癌、白血病、淋巴瘤、甲状腺癌的至少一种。According to a specific embodiment of the present invention, the tumor comprises a patient selected from the group consisting of neuroblastoma, glioma, colon cancer, rectal cancer, liver cancer, gastric cancer, pancreatic cancer, cervical cancer, breast cancer, ovarian cancer, prostate cancer, bladder cancer. At least one of melanoma, epidermal squamous cell carcinoma, rhabdomyosarcoma, multiple myeloma, sarcoma, lung cancer, throat cancer, oral cancer, leukemia, lymphoma, thyroid cancer.

根据本发明的另一个方面,本发明提供了二羟基丙酮在治疗肿瘤中的用途。According to another aspect of the invention, the invention provides the use of dihydroxyacetone in the treatment of a tumor.

根据本发明的一些实施例,所述肿瘤包括选自神经系统肿瘤、消化系统肿瘤、生殖系统肿瘤、泌尿系统肿瘤、皮肤肿瘤、骨肿瘤、关节系统肿瘤、呼吸系统肿瘤、血液及腺体肿瘤的至少一种。According to some embodiments of the invention, the tumor comprises a tumor selected from the group consisting of a nervous system tumor, a digestive system tumor, a reproductive system tumor, a urinary system tumor, a skin tumor, a bone tumor, a joint system tumor, a respiratory tumor, a blood, and a gland tumor. At least one.

根据本发明的具体实施例,所述肿瘤包括选自神经母细胞癌、胶质瘤、结肠癌、直肠癌、肝癌、胃癌、胰腺癌、宫颈癌、乳腺癌、卵巢癌、前列腺癌、膀胱癌、黑色素瘤、表皮鳞状细胞癌、横纹肌瘤、多发性骨髓瘤、肉瘤、肺癌、咽喉癌、口腔癌、白血病、淋巴瘤、甲状腺癌的至少一种。According to a specific embodiment of the present invention, the tumor comprises a patient selected from the group consisting of neuroblastoma, glioma, colon cancer, rectal cancer, liver cancer, gastric cancer, pancreatic cancer, cervical cancer, breast cancer, ovarian cancer, prostate cancer, bladder cancer. At least one of melanoma, epidermal squamous cell carcinoma, rhabdomyosarcoma, multiple myeloma, sarcoma, lung cancer, throat cancer, oral cancer, leukemia, lymphoma, thyroid cancer.

根据本发明的又一方面,本发明提供了一种治疗肿瘤的方法,包含给予患者二羟基丙酮。According to still another aspect of the present invention, the present invention provides a method of treating a tumor comprising administering to a patient dihydroxyacetone.

根据本发明的一些实施例,所述肿瘤包括选自神经系统肿瘤、消化系统肿瘤、生殖系统肿瘤、泌尿系统肿瘤、皮肤肿瘤、骨肿瘤、关节系统肿瘤、呼吸系统肿瘤、血液及腺体肿瘤的至少一种。According to some embodiments of the invention, the tumor comprises a tumor selected from the group consisting of a nervous system tumor, a digestive system tumor, a reproductive system tumor, a urinary system tumor, a skin tumor, a bone tumor, a joint system tumor, a respiratory tumor, a blood, and a gland tumor. At least one.

根据本发明的具体实施例,所述肿瘤包括选自神经母细胞癌、胶质瘤、结肠癌、直肠癌、肝癌、胃癌、胰腺癌、宫颈癌、乳腺癌、卵巢癌、前列腺癌、膀胱癌、黑色素瘤、表皮鳞状细胞癌、横纹肌瘤、多发性骨髓瘤、肉瘤、肺癌、咽喉癌、口腔癌、白血病、淋巴瘤、甲状腺癌的至少一种。According to a specific embodiment of the present invention, the tumor comprises a patient selected from the group consisting of neuroblastoma, glioma, colon cancer, rectal cancer, liver cancer, gastric cancer, pancreatic cancer, cervical cancer, breast cancer, ovarian cancer, prostate cancer, bladder cancer. At least one of melanoma, epidermal squamous cell carcinoma, rhabdomyosarcoma, multiple myeloma, sarcoma, lung cancer, throat cancer, oral cancer, leukemia, lymphoma, thyroid cancer.

根据本发明的又一方面,本发明提供了一种抗肿瘤的药物组合物,含有二羟基丙酮作为活性成分。According to still another aspect of the present invention, the present invention provides an antitumor pharmaceutical composition comprising dihydroxyacetone as an active ingredient.

根据本发明的一些实施例,所述肿瘤包括选自神经系统肿瘤、消化系统肿瘤、生殖系统肿瘤、泌尿系统肿瘤、皮肤肿瘤、骨肿瘤、关节系统肿瘤、呼吸系统肿瘤、血液及腺体肿瘤的至少一种。 According to some embodiments of the invention, the tumor comprises a tumor selected from the group consisting of a nervous system tumor, a digestive system tumor, a reproductive system tumor, a urinary system tumor, a skin tumor, a bone tumor, a joint system tumor, a respiratory tumor, a blood, and a gland tumor. At least one.

根据本发明的具体实施例,所述肿瘤包括选自神经母细胞癌、胶质瘤、结肠癌、直肠癌、肝癌、胃癌、胰腺癌、宫颈癌、乳腺癌、卵巢癌、前列腺癌和膀胱癌、黑色素瘤、表皮鳞状细胞癌、横纹肌瘤、多发性骨髓瘤、肉瘤、肺癌、咽喉癌、口腔癌、白血病、淋巴瘤、甲状腺癌的至少一种。According to a specific embodiment of the invention, the tumor comprises a patient selected from the group consisting of neuroblastoma, glioma, colon cancer, rectal cancer, liver cancer, gastric cancer, pancreatic cancer, cervical cancer, breast cancer, ovarian cancer, prostate cancer and bladder cancer. At least one of melanoma, epidermal squamous cell carcinoma, rhabdomyosarcoma, multiple myeloma, sarcoma, lung cancer, throat cancer, oral cancer, leukemia, lymphoma, thyroid cancer.

本发明提供了二羟基丙酮和顺铂联合用药在抗肿瘤方面的应用。The invention provides an anti-tumor application of a combination of dihydroxyacetone and cisplatin.

根据本发明的又一方面,本发明提供了一种抗肿瘤的药物组合物,含有二羟基丙酮和顺铂作为有效成分。二羟基丙酮和顺铂在治疗肿瘤方面具有一定协同作用,二羟基丙酮和顺铂联合用药治疗肿瘤效果明显优于单独使用二羟基丙酮或者顺铂,并且二羟基丙酮没有增加顺铂的毒副作用。According to still another aspect of the present invention, the present invention provides an antitumor pharmaceutical composition comprising dihydroxyacetone and cisplatin as active ingredients. Dihydroxyacetone and cisplatin have a certain synergistic effect in the treatment of tumors. The combination of dihydroxyacetone and cisplatin is superior to the treatment of tumors with dihydroxyacetone or cisplatin alone, and dihydroxyacetone does not increase the side effects of cisplatin.

根据本发明的一些实施例,所述肿瘤包括选自神经系统肿瘤、消化系统肿瘤、生殖系统肿瘤、泌尿系统肿瘤、皮肤肿瘤、骨肿瘤、关节系统肿瘤、呼吸系统肿瘤、血液及腺体肿瘤的至少一种。According to some embodiments of the invention, the tumor comprises a tumor selected from the group consisting of a nervous system tumor, a digestive system tumor, a reproductive system tumor, a urinary system tumor, a skin tumor, a bone tumor, a joint system tumor, a respiratory tumor, a blood, and a gland tumor. At least one.

根据本发明的具体实施例,所述肿瘤包括选自神经母细胞癌、胶质瘤、结肠癌、直肠癌、肝癌、胃癌、胰腺癌、宫颈癌、乳腺癌、卵巢癌、前列腺癌和膀胱癌、黑色素瘤、表皮鳞状细胞癌、横纹肌瘤、多发性骨髓瘤、肉瘤、肺癌、咽喉癌、口腔癌、白血病、淋巴瘤、甲状腺癌的至少一种。According to a specific embodiment of the invention, the tumor comprises a patient selected from the group consisting of neuroblastoma, glioma, colon cancer, rectal cancer, liver cancer, gastric cancer, pancreatic cancer, cervical cancer, breast cancer, ovarian cancer, prostate cancer and bladder cancer. At least one of melanoma, epidermal squamous cell carcinoma, rhabdomyosarcoma, multiple myeloma, sarcoma, lung cancer, throat cancer, oral cancer, leukemia, lymphoma, thyroid cancer.

根据本发明的又一方面,本发明提供了一种抗肿瘤的药物联合,由二羟基丙酮和顺铂组成。二羟基丙酮和顺铂在治疗肿瘤方面具有一定协同作用,二羟基丙酮和顺铂联合用药治疗肿瘤效果明显优于单独使用二羟基丙酮或者顺铂,并且二羟基丙酮没有增加顺铂的毒副作用。According to still another aspect of the present invention, the present invention provides an antitumor drug combination consisting of dihydroxyacetone and cisplatin. Dihydroxyacetone and cisplatin have a certain synergistic effect in the treatment of tumors. The combination of dihydroxyacetone and cisplatin is superior to the treatment of tumors with dihydroxyacetone or cisplatin alone, and dihydroxyacetone does not increase the side effects of cisplatin.

根据本发明的具体实施例,药物联合中二羟基丙酮可以呈口服制剂形式,顺铂可以呈注射剂形式。According to a particular embodiment of the invention, the dihydroxyacetone in the pharmaceutical combination may be in the form of an oral preparation, and the cisplatin may be in the form of an injection.

根据本发明的一些实施例,所述肿瘤包括选自神经系统肿瘤、消化系统肿瘤、生殖系统肿瘤、泌尿系统肿瘤、皮肤肿瘤、骨肿瘤、关节系统肿瘤、呼吸系统肿瘤、血液及腺体肿瘤的至少一种。According to some embodiments of the invention, the tumor comprises a tumor selected from the group consisting of a nervous system tumor, a digestive system tumor, a reproductive system tumor, a urinary system tumor, a skin tumor, a bone tumor, a joint system tumor, a respiratory tumor, a blood, and a gland tumor. At least one.

根据本发明的具体实施例,所述肿瘤包括选自神经母细胞癌、胶质瘤、结肠癌、直肠癌、肝癌、胃癌、胰腺癌、宫颈癌、乳腺癌、卵巢癌、前列腺癌和膀胱癌、黑色素瘤、表皮鳞状细胞癌、横纹肌瘤、多发性骨髓瘤、肉瘤、肺癌、咽喉癌、口腔癌、白血病、淋巴瘤、甲状腺癌的至少一种。According to a specific embodiment of the invention, the tumor comprises a patient selected from the group consisting of neuroblastoma, glioma, colon cancer, rectal cancer, liver cancer, gastric cancer, pancreatic cancer, cervical cancer, breast cancer, ovarian cancer, prostate cancer and bladder cancer. At least one of melanoma, epidermal squamous cell carcinoma, rhabdomyosarcoma, multiple myeloma, sarcoma, lung cancer, throat cancer, oral cancer, leukemia, lymphoma, thyroid cancer.

根据本发明的又一方面,本发明提供了二羟基丙酮在制备药物中的用途,所述药物用于抗肿瘤,为受试者同时给药二羟基丙酮和顺铂。给药方式可以按照其各自常规的给药途 径、用量和频次。According to still another aspect of the present invention, the present invention provides the use of dihydroxyacetone for the preparation of a medicament for use in anti-tumor, simultaneous administration of dihydroxyacetone and cisplatin to a subject. The mode of administration can be according to their respective conventional routes of administration. Diameter, usage and frequency.

根据本发明的一些实施例,所述肿瘤包括选自神经系统肿瘤、消化系统肿瘤、生殖系统肿瘤、泌尿系统肿瘤、皮肤肿瘤、骨肿瘤、关节系统肿瘤、呼吸系统肿瘤、血液及腺体肿瘤的至少一种。According to some embodiments of the invention, the tumor comprises a tumor selected from the group consisting of a nervous system tumor, a digestive system tumor, a reproductive system tumor, a urinary system tumor, a skin tumor, a bone tumor, a joint system tumor, a respiratory tumor, a blood, and a gland tumor. At least one.

根据本发明的具体实施例,所述肿瘤包括选自神经母细胞癌、胶质瘤、结肠癌、直肠癌、肝癌、胃癌、胰腺癌、宫颈癌、乳腺癌、卵巢癌、前列腺癌和膀胱癌、黑色素瘤、表皮鳞状细胞癌、横纹肌瘤、多发性骨髓瘤、肉瘤、肺癌、咽喉癌、口腔癌、白血病、淋巴瘤、甲状腺癌的至少一种。According to a specific embodiment of the invention, the tumor comprises a patient selected from the group consisting of neuroblastoma, glioma, colon cancer, rectal cancer, liver cancer, gastric cancer, pancreatic cancer, cervical cancer, breast cancer, ovarian cancer, prostate cancer and bladder cancer. At least one of melanoma, epidermal squamous cell carcinoma, rhabdomyosarcoma, multiple myeloma, sarcoma, lung cancer, throat cancer, oral cancer, leukemia, lymphoma, thyroid cancer.

根据本发明的又一方面,本发明提供了二羟基丙酮在治疗肿瘤中的用途,其中,为受试者同时给药二羟基丙酮和顺铂。给药方式可以按照其各自常规的给药途径、用量和频次。According to still another aspect of the present invention, the present invention provides the use of dihydroxyacetone in the treatment of a tumor, wherein the subject is simultaneously administered with dihydroxyacetone and cisplatin. The mode of administration can be in accordance with their respective usual routes of administration, dosage and frequency.

根据本发明的一些实施例,所述肿瘤包括选自神经系统肿瘤、消化系统肿瘤、生殖系统肿瘤、泌尿系统肿瘤、皮肤肿瘤、骨肿瘤、关节系统肿瘤、呼吸系统肿瘤、血液及腺体肿瘤的至少一种。According to some embodiments of the invention, the tumor comprises a tumor selected from the group consisting of a nervous system tumor, a digestive system tumor, a reproductive system tumor, a urinary system tumor, a skin tumor, a bone tumor, a joint system tumor, a respiratory tumor, a blood, and a gland tumor. At least one.

根据本发明的具体实施例,所述肿瘤包括选自神经母细胞癌、胶质瘤、结肠癌、直肠癌、肝癌、胃癌、胰腺癌、宫颈癌、乳腺癌、卵巢癌、前列腺癌和膀胱癌、黑色素瘤、表皮鳞状细胞癌、横纹肌瘤、多发性骨髓瘤、肉瘤、肺癌、咽喉癌、口腔癌、白血病、淋巴瘤、甲状腺癌的至少一种。According to a specific embodiment of the invention, the tumor comprises a patient selected from the group consisting of neuroblastoma, glioma, colon cancer, rectal cancer, liver cancer, gastric cancer, pancreatic cancer, cervical cancer, breast cancer, ovarian cancer, prostate cancer and bladder cancer. At least one of melanoma, epidermal squamous cell carcinoma, rhabdomyosarcoma, multiple myeloma, sarcoma, lung cancer, throat cancer, oral cancer, leukemia, lymphoma, thyroid cancer.

根据本发明的又一方面,本发明提供了一种治疗肿瘤的方法,包含给予患者二羟基丙酮,其中,为受试者同时给药二羟基丙酮和顺铂。给药方式可以按照其各自常规的给药途径、用量和频次。According to still another aspect of the present invention, the present invention provides a method of treating a tumor comprising administering to a patient dihydroxyacetone, wherein the subject is simultaneously administered with dihydroxyacetone and cisplatin. The mode of administration can be in accordance with their respective usual routes of administration, dosage and frequency.

根据本发明的一些实施例,所述肿瘤包括选自神经系统肿瘤、消化系统肿瘤、生殖系统肿瘤、泌尿系统肿瘤、皮肤肿瘤、骨肿瘤、关节系统肿瘤、呼吸系统肿瘤、血液及腺体肿瘤的至少一种。According to some embodiments of the invention, the tumor comprises a tumor selected from the group consisting of a nervous system tumor, a digestive system tumor, a reproductive system tumor, a urinary system tumor, a skin tumor, a bone tumor, a joint system tumor, a respiratory tumor, a blood, and a gland tumor. At least one.

根据本发明的具体实施例,所述肿瘤包括选自神经母细胞癌、胶质瘤、结肠癌、直肠癌、肝癌、胃癌、胰腺癌、宫颈癌、乳腺癌、卵巢癌、前列腺癌和膀胱癌、黑色素瘤、表皮鳞状细胞癌、横纹肌瘤、多发性骨髓瘤、肉瘤、肺癌、咽喉癌、口腔癌、白血病、淋巴瘤、甲状腺癌的至少一种。According to a specific embodiment of the invention, the tumor comprises a patient selected from the group consisting of neuroblastoma, glioma, colon cancer, rectal cancer, liver cancer, gastric cancer, pancreatic cancer, cervical cancer, breast cancer, ovarian cancer, prostate cancer and bladder cancer. At least one of melanoma, epidermal squamous cell carcinoma, rhabdomyosarcoma, multiple myeloma, sarcoma, lung cancer, throat cancer, oral cancer, leukemia, lymphoma, thyroid cancer.

根据本发明的又一方面,本发明提供了二羟基丙酮和顺铂的组合在制备药物中的用途,所述药物用于抗肿瘤。二羟基丙酮和顺铂在治疗肿瘤方面具有一定协同作用,二羟基丙酮和顺铂联合用药治疗肿瘤效果明显优于单独使用二羟基丙酮或者顺铂,并且二羟基丙酮没有增加顺铂的毒副作用。 According to still another aspect of the present invention, the present invention provides the use of a combination of dihydroxyacetone and cisplatin for the preparation of a medicament for use in anti-tumor. Dihydroxyacetone and cisplatin have a certain synergistic effect in the treatment of tumors. The combination of dihydroxyacetone and cisplatin is superior to the treatment of tumors with dihydroxyacetone or cisplatin alone, and dihydroxyacetone does not increase the side effects of cisplatin.

根据本发明的一些实施例,所述肿瘤包括选自神经系统肿瘤、消化系统肿瘤、生殖系统肿瘤、泌尿系统肿瘤、皮肤肿瘤、骨肿瘤、关节系统肿瘤、呼吸系统肿瘤、血液及腺体肿瘤的至少一种。According to some embodiments of the invention, the tumor comprises a tumor selected from the group consisting of a nervous system tumor, a digestive system tumor, a reproductive system tumor, a urinary system tumor, a skin tumor, a bone tumor, a joint system tumor, a respiratory tumor, a blood, and a gland tumor. At least one.

根据本发明的具体实施例,所述肿瘤包括选自神经母细胞癌、胶质瘤、结肠癌、直肠癌、肝癌、胃癌、胰腺癌、宫颈癌、乳腺癌、卵巢癌、前列腺癌和膀胱癌、黑色素瘤、表皮鳞状细胞癌、横纹肌瘤、多发性骨髓瘤、肉瘤、肺癌、咽喉癌、口腔癌、白血病、淋巴瘤、甲状腺癌的至少一种。According to a specific embodiment of the invention, the tumor comprises a patient selected from the group consisting of neuroblastoma, glioma, colon cancer, rectal cancer, liver cancer, gastric cancer, pancreatic cancer, cervical cancer, breast cancer, ovarian cancer, prostate cancer and bladder cancer. At least one of melanoma, epidermal squamous cell carcinoma, rhabdomyosarcoma, multiple myeloma, sarcoma, lung cancer, throat cancer, oral cancer, leukemia, lymphoma, thyroid cancer.

根据本发明的又一方面,本发明提供了二羟基丙酮和顺铂的组合在治疗肿瘤中的用途。二羟基丙酮和顺铂在治疗肿瘤方面具有一定协同作用,二羟基丙酮和顺铂联合用药治疗肿瘤效果明显优于单独使用二羟基丙酮或者顺铂,并且二羟基丙酮没有增加顺铂的毒副作用。According to yet another aspect of the invention, the invention provides the use of a combination of dihydroxyacetone and cisplatin in the treatment of a tumor. Dihydroxyacetone and cisplatin have a certain synergistic effect in the treatment of tumors. The combination of dihydroxyacetone and cisplatin is superior to the treatment of tumors with dihydroxyacetone or cisplatin alone, and dihydroxyacetone does not increase the side effects of cisplatin.

根据本发明的一些实施例,所述肿瘤包括选自神经系统肿瘤、消化系统肿瘤、生殖系统肿瘤、泌尿系统肿瘤、皮肤肿瘤、骨肿瘤、关节系统肿瘤、呼吸系统肿瘤、血液及腺体肿瘤的至少一种。According to some embodiments of the invention, the tumor comprises a tumor selected from the group consisting of a nervous system tumor, a digestive system tumor, a reproductive system tumor, a urinary system tumor, a skin tumor, a bone tumor, a joint system tumor, a respiratory tumor, a blood, and a gland tumor. At least one.

根据本发明的具体实施例,所述肿瘤包括选自神经母细胞癌、胶质瘤、结肠癌、直肠癌、肝癌、胃癌、胰腺癌、宫颈癌、乳腺癌、卵巢癌、前列腺癌和膀胱癌、黑色素瘤、表皮鳞状细胞癌、横纹肌瘤、多发性骨髓瘤、肉瘤、肺癌、咽喉癌、口腔癌、白血病、淋巴瘤、甲状腺癌的至少一种。According to a specific embodiment of the invention, the tumor comprises a patient selected from the group consisting of neuroblastoma, glioma, colon cancer, rectal cancer, liver cancer, gastric cancer, pancreatic cancer, cervical cancer, breast cancer, ovarian cancer, prostate cancer and bladder cancer. At least one of melanoma, epidermal squamous cell carcinoma, rhabdomyosarcoma, multiple myeloma, sarcoma, lung cancer, throat cancer, oral cancer, leukemia, lymphoma, thyroid cancer.

根据本发明的又一方面,本发明提供了一种治疗肿瘤的方法,包含给予患者二羟基丙酮和顺铂的组合。二羟基丙酮和顺铂在治疗肿瘤方面具有一定协同作用,二羟基丙酮和顺铂联合用药治疗肿瘤效果明显优于单独使用二羟基丙酮或者顺铂,并且二羟基丙酮没有增加顺铂的毒副作用。According to still another aspect of the present invention, the present invention provides a method of treating a tumor comprising administering to a patient a combination of dihydroxyacetone and cisplatin. Dihydroxyacetone and cisplatin have a certain synergistic effect in the treatment of tumors. The combination of dihydroxyacetone and cisplatin is superior to the treatment of tumors with dihydroxyacetone or cisplatin alone, and dihydroxyacetone does not increase the side effects of cisplatin.

根据本发明的一些实施例,所述肿瘤包括选自神经系统肿瘤、消化系统肿瘤、生殖系统肿瘤、泌尿系统肿瘤、皮肤肿瘤、骨肿瘤、关节系统肿瘤、呼吸系统肿瘤、血液及腺体肿瘤的至少一种。According to some embodiments of the invention, the tumor comprises a tumor selected from the group consisting of a nervous system tumor, a digestive system tumor, a reproductive system tumor, a urinary system tumor, a skin tumor, a bone tumor, a joint system tumor, a respiratory tumor, a blood, and a gland tumor. At least one.

根据本发明的具体实施例,所述肿瘤包括选自神经母细胞癌、胶质瘤、结肠癌、直肠癌、肝癌、胃癌、胰腺癌、宫颈癌、乳腺癌、卵巢癌、前列腺癌和膀胱癌、黑色素瘤、表皮鳞状细胞癌、横纹肌瘤、多发性骨髓瘤、肉瘤、肺癌、咽喉癌、口腔癌、白血病、淋巴瘤、甲状腺癌的至少一种。According to a specific embodiment of the invention, the tumor comprises a patient selected from the group consisting of neuroblastoma, glioma, colon cancer, rectal cancer, liver cancer, gastric cancer, pancreatic cancer, cervical cancer, breast cancer, ovarian cancer, prostate cancer and bladder cancer. At least one of melanoma, epidermal squamous cell carcinoma, rhabdomyosarcoma, multiple myeloma, sarcoma, lung cancer, throat cancer, oral cancer, leukemia, lymphoma, thyroid cancer.

根据本发明的又一方面,本发明提供了一种用于抗肿瘤的药盒,其中包括二羟基丙酮和顺铂。二羟基丙酮和顺铂在治疗肿瘤方面具有一定协同作用,二羟基丙酮和顺铂联合用药治疗肿瘤效果明显优于单独使用二羟基丙酮或者顺铂,并且二羟基丙酮没有增加顺铂的 毒副作用。According to still another aspect of the present invention, the present invention provides a kit for antitumor comprising dihydroxyacetone and cisplatin. Dihydroxyacetone and cisplatin have a synergistic effect in the treatment of tumors. The combination of dihydroxyacetone and cisplatin is more effective than tumor treatment with dihydroxyacetone or cisplatin alone, and dihydroxyacetone does not increase cisplatin. toxic side effect.

根据本发明的具体实施例,药盒中二羟基丙酮和顺铂被设置在不同的容器中。According to a particular embodiment of the invention, the dihydroxyacetone and cisplatin in the kit are placed in separate containers.

根据本发明的具体实施例,二羟基丙酮呈口服制剂形式,顺铂呈注射剂形式。According to a particular embodiment of the invention, the dihydroxyacetone is in the form of an oral preparation and the cisplatin is in the form of an injection.

根据本发明具体实施例,药盒中二羟基丙酮和顺铂的重量比为(3375-4125):1。优选地,二羟基丙酮和顺铂的重量比为3750:1。According to a particular embodiment of the invention, the weight ratio of dihydroxyacetone to cisplatin in the kit is (3375-4125):1. Preferably, the weight ratio of dihydroxyacetone to cisplatin is 3750:1.

根据本发明的一些实施例,所述肿瘤包括选自神经系统肿瘤、消化系统肿瘤、生殖系统肿瘤、泌尿系统肿瘤、皮肤肿瘤、骨肿瘤、关节系统肿瘤、呼吸系统肿瘤、血液及腺体肿瘤的至少一种。According to some embodiments of the invention, the tumor comprises a tumor selected from the group consisting of a nervous system tumor, a digestive system tumor, a reproductive system tumor, a urinary system tumor, a skin tumor, a bone tumor, a joint system tumor, a respiratory tumor, a blood, and a gland tumor. At least one.

根据本发明的具体实施例,所述肿瘤包括选自神经母细胞癌、胶质瘤、结肠癌、直肠癌、肝癌、胃癌、胰腺癌、宫颈癌、乳腺癌、卵巢癌、前列腺癌和膀胱癌、黑色素瘤、表皮鳞状细胞癌、横纹肌瘤、多发性骨髓瘤、肉瘤、肺癌、咽喉癌、口腔癌、白血病、淋巴瘤、甲状腺癌的至少一种。According to a specific embodiment of the invention, the tumor comprises a patient selected from the group consisting of neuroblastoma, glioma, colon cancer, rectal cancer, liver cancer, gastric cancer, pancreatic cancer, cervical cancer, breast cancer, ovarian cancer, prostate cancer and bladder cancer. At least one of melanoma, epidermal squamous cell carcinoma, rhabdomyosarcoma, multiple myeloma, sarcoma, lung cancer, throat cancer, oral cancer, leukemia, lymphoma, thyroid cancer.

根据本发明的又一方面,本发明提供了二羟基丙酮和顺铂的组合在制备药盒中的用途,所述药盒用于抗肿瘤。According to yet another aspect of the invention, the invention provides the use of a combination of dihydroxyacetone and cisplatin for the preparation of a kit for use in anti-tumor.

根据本发明的一些实施例,所述肿瘤包括选自神经系统肿瘤、消化系统肿瘤、生殖系统肿瘤、泌尿系统肿瘤、皮肤肿瘤、骨肿瘤、关节系统肿瘤、呼吸系统肿瘤、血液及腺体肿瘤的至少一种。According to some embodiments of the invention, the tumor comprises a tumor selected from the group consisting of a nervous system tumor, a digestive system tumor, a reproductive system tumor, a urinary system tumor, a skin tumor, a bone tumor, a joint system tumor, a respiratory tumor, a blood, and a gland tumor. At least one.

根据本发明的具体实施例,所述肿瘤包括选自神经母细胞癌、胶质瘤、结肠癌、直肠癌、肝癌、胃癌、胰腺癌、宫颈癌、乳腺癌、卵巢癌、前列腺癌和膀胱癌、黑色素瘤、表皮鳞状细胞癌、横纹肌瘤、多发性骨髓瘤、肉瘤、肺癌、咽喉癌、口腔癌、白血病、淋巴瘤、甲状腺癌的至少一种。According to a specific embodiment of the invention, the tumor comprises a patient selected from the group consisting of neuroblastoma, glioma, colon cancer, rectal cancer, liver cancer, gastric cancer, pancreatic cancer, cervical cancer, breast cancer, ovarian cancer, prostate cancer and bladder cancer. At least one of melanoma, epidermal squamous cell carcinoma, rhabdomyosarcoma, multiple myeloma, sarcoma, lung cancer, throat cancer, oral cancer, leukemia, lymphoma, thyroid cancer.

本发明提供的应用,既包括在恶性肿瘤中的应用,也包括在良性肿瘤中的应用。The application provided by the present invention includes both the application in malignant tumors and the application in benign tumors.

根据本发明的具体实施例,二羟基丙酮能用于抑制癌转移,作为术后的癌症转移抑制剂特别有用。According to a particular embodiment of the invention, dihydroxyacetone can be used to inhibit cancer metastasis and is particularly useful as a post-surgical cancer metastasis inhibitor.

需要说明的是,在本文中所使用的术语“二羟基丙酮”应做广义理解,即可以包括单体形式的二羟基丙酮,也应该覆盖二羟基丙酮的常见存在形式,例如各种晶型、二聚体或者多聚体、水合物等形式。It should be noted that the term "dihydroxyacetone" as used herein is to be understood broadly, that is, it may include dihydroxyacetone in a monomeric form, and should also cover the common forms of dihydroxyacetone, such as various crystal forms, Dimer or multimer, hydrate, etc.

根据本发明的一些实施例,二羟基丙酮可以为单体、二聚合体或多聚体。According to some embodiments of the invention, the dihydroxyacetone may be a monomer, a dimer or a multimer.

本发明的应用,二羟基丙酮可以各种形态在人或动物中给予,既可以是口服,也可以是静脉内注射、肌肉内注射、皮下或皮内注射、直肠内给药、粘膜给药等方式。口服剂的形态,可以列举为片剂、丸剂、颗粒剂、散剂、胶囊剂、口服液、悬浊剂、乳剂、糖浆剂 等。非口服制剂,可以列举为注射剂、滴剂、滴鼻剂、吸入剂、栓剂、软膏、乳霜、粉状涂布剂、贴剂等经皮吸收剂等。本发明的应用,还包括将二羟基丙酮埋入药丸中和使用公知技术制得的缓释性制剂。For the application of the present invention, dihydroxyacetone can be administered in human or animal in various forms, and can be oral, intravenous, intramuscular, subcutaneous or intradermal, intrarectal, mucosal, etc. the way. The form of the oral preparation can be exemplified by tablets, pills, granules, powders, capsules, oral liquids, suspensions, emulsions, syrups. Wait. The non-oral preparation may, for example, be a transdermal absorption agent such as an injection, a drop, a nasal drop, an inhalant, a suppository, an ointment, a cream, a powder coating agent or a patch. The use of the present invention also includes the incorporation of dihydroxyacetone into a pellet and a sustained release formulation prepared using known techniques.

本发明所述药物适宜以药物组合物的形式应用。这类组合物可以以常规方式与一种或多种药学上可接受的载体或赋形剂混合使用。若有可能在治疗上将二羟基丙酮作为原料药给药。The medicament of the present invention is suitably used in the form of a pharmaceutical composition. Such compositions may be combined in a conventional manner with one or more pharmaceutically acceptable carriers or excipients. If possible, dihydroxyacetone is administered as a drug substance therapeutically.

本发明的药物组合物在制备成药物制剂时,根据需要可以加入药学上可接受的载体。以二羟基丙酮作为主药或主药之一。When the pharmaceutical composition of the present invention is prepared into a pharmaceutical preparation, a pharmaceutically acceptable carrier can be added as needed. Dihydroxyacetone is used as one of the main or main drugs.

本发明的药物组合物,根据需要可以含有药物可接受的载体,其中二羟基丙酮作为药物活性成分,其在制剂中所占重量百分比可以是0.01-99.99%,其余为药物可接受的载体。本发明的药物制剂,以单位剂量形式存在,所述单位剂量形式是指制剂的单位,如片剂的每片,胶囊的每粒胶囊,口服液的每瓶,颗粒剂每袋,注射剂的每支等。The pharmaceutical composition of the present invention may contain a pharmaceutically acceptable carrier as needed, wherein dihydroxyacetone is a pharmaceutically active ingredient, which may be 0.01-99.99% by weight in the preparation, and the balance being a pharmaceutically acceptable carrier. The pharmaceutical preparation of the present invention is in the form of a unit dosage form, which means a unit of the preparation, such as each tablet of the tablet, each capsule of the capsule, each bottle of the oral solution, granules per bag, and each injection. Branch and so on.

本发明的药物组合物,其口服给药的制剂可含有常用的赋形剂,诸如粘合剂、填充剂、稀释剂、压片剂、润滑剂、崩解剂、着色剂、调味剂和湿润剂,必要时可对片剂进行包衣。The pharmaceutical composition of the present invention, which is orally administered, may contain conventional excipients such as a binder, a filler, a diluent, a tablet, a lubricant, a disintegrant, a coloring agent, a flavoring agent, and a moisturizing agent. The tablets can be coated if necessary.

适用的填充剂包括纤维素、甘露糖醇、乳糖和其它类似的填充剂。适宜的崩解剂包括淀粉、聚乙烯吡咯烷酮和淀粉衍生物,例如羟基乙酸淀粉钠。适宜的润滑剂包括,例如硬脂酸镁。适宜的药物可接受的湿润剂包括十二烷基硫酸钠。Suitable fillers include cellulose, mannitol, lactose and other similar fillers. Suitable disintegrants include starch, polyvinylpyrrolidone and starch derivatives such as sodium starch glycolate. Suitable lubricants include, for example, magnesium stearate. Suitable pharmaceutically acceptable wetting agents include sodium lauryl sulfate.

可通过混合,填充,压片等常用的方法制备固体口服组合物。进行反复混合可使活性物质分布在整个使用大量填充剂的那些组合物中。Solid oral compositions can be prepared by conventional methods such as mixing, filling, tableting, and the like. Repeated mixing allows the active material to be distributed throughout those compositions that use large amounts of filler.

口服液体制剂的形式例如可以是水性或油性悬浮液、溶液、乳剂、糖浆剂或酏剂,或者可以是一种在使用前可用水或其它适宜的载体复配的干燥产品。这种液体制剂可含有常规的添加剂,诸如悬浮剂,例如山梨醇、糖浆、甲基纤维素、明胶、羟乙基纤维素、羧甲基纤维素、硬脂酸铝凝胶或氢化食用脂肪,乳化剂,例如卵磷脂、脱水山梨醇一油酸酯或阿拉伯胶;非水性载体(它们可以包括食用油),例如杏仁油、分馏椰子油、诸如甘油的酯的油性酯、丙二醇或乙醇;防腐剂,例如对羟基苯甲酯或对羟基苯甲酸丙酯或山梨酸,并且如果需要,可含有常规的香味剂或着色剂。The oral liquid preparation may be in the form of, for example, an aqueous or oily suspension, solution, emulsion, syrup or elixir, or may be a dry product which may be formulated with water or other suitable carrier before use. Such liquid preparations may contain conventional additives such as suspending agents such as sorbitol, syrup, methylcellulose, gelatin, hydroxyethylcellulose, carboxymethylcellulose, aluminum stearate gel or hydrogenated edible fats. Emulsifiers such as lecithin, sorbitan monooleate or gum arabic; non-aqueous vehicles (which may include edible oils), such as almond oil, fractionated coconut oil, oily esters of esters such as glycerol, propylene glycol or ethanol; The agent, for example, p-hydroxybenzyl or propylparaben or sorbic acid, and if desired, may contain conventional flavoring or coloring agents.

对于注射剂,制备的液体单位剂型含有本发明的活性物质和无菌载体。根据载体和浓度,可以将此化合物悬浮或者溶解。溶液的制备通常是通过将活性物质溶解在一种载体中,在将其装入一种适宜的小瓶或安瓿前过滤消毒,然后密封。辅料例如一种局部麻醉剂、防腐剂和缓冲剂也可以溶解在这种载体中。为了提高其稳定性,可在装入小瓶以后将这种组合物冰冻,并在真空下将水除去。 For injection, the liquid unit dosage form prepared contains the active substance of the invention and a sterile vehicle. This compound can be suspended or dissolved depending on the carrier and concentration. The solution is usually prepared by dissolving the active substance in a carrier, sterilizing it by filtration before filling it into a suitable vial or ampoule, and then sealing. Excipients such as a local anesthetic, preservative and buffer may also be dissolved in such a carrier. To increase its stability, the composition can be frozen after filling the vial and the water removed under vacuum.

本发明的药物组合物,在制备成药剂时可选择性的加入适合的药物可接受的载体,所述药物可接受的载体选自:甘露醇、山梨醇、焦亚硫酸钠、亚硫酸氢钠、硫代硫酸钠、盐酸半胱氨酸、巯基乙酸、蛋氨酸、维生素C、EDTA二钠、EDTA钙钠,一价碱金属的碳酸盐、醋酸盐、磷酸盐或其水溶液、盐酸、醋酸、硫酸、磷酸、氨基酸、氯化钠、氯化钾、乳酸钠、木糖醇、麦芽糖、葡萄糖、果糖、右旋糖苷、甘氨酸、淀粉、蔗糖、乳糖、甘露糖醇、硅衍生物、纤维素及其衍生物、藻酸盐、明胶、聚乙烯吡咯烷酮、甘油、土温80、琼脂、碳酸钙、碳酸氢钙、表面活性剂、聚乙二醇、环糊精、β-环糊精、磷脂类材料、高岭土、滑石粉、硬脂酸钙、硬脂酸镁等。The pharmaceutical composition of the present invention may optionally be added to a suitable pharmaceutically acceptable carrier when prepared as a medicament, the pharmaceutically acceptable carrier being selected from the group consisting of: mannitol, sorbitol, sodium metabisulfite, sodium hydrogen sulfite, sulfur Sodium sulfate, cysteine hydrochloride, thioglycolic acid, methionine, vitamin C, disodium EDTA, calcium EDTA, monovalent alkali metal carbonate, acetate, phosphate or its aqueous solution, hydrochloric acid, acetic acid, sulfuric acid , phosphoric acid, amino acid, sodium chloride, potassium chloride, sodium lactate, xylitol, maltose, glucose, fructose, dextran, glycine, starch, sucrose, lactose, mannitol, silicon derivatives, cellulose and their derivatives , alginate, gelatin, polyvinylpyrrolidone, glycerin, earth temperature 80, agar, calcium carbonate, calcium hydrogencarbonate, surfactant, polyethylene glycol, cyclodextrin, β-cyclodextrin, phospholipids, Kaolin, talc, calcium stearate, magnesium stearate, and the like.

附图说明DRAWINGS

本发明的上述和/或附加的方面和优点从下面结合附图对实施例的描述中将变得明显和容易理解,其中:The above and/or additional aspects and advantages of the present invention will become apparent and readily understood from

图1是根据本发明的实施例1中二羟基丙酮对H460、HT29、SGC7901细胞株的IC50统计结果图;1 is a graph showing IC50 results of dihydroxyacetone to H460, HT29, and SGC7901 cell lines according to Example 1 of the present invention;

图2是根据本发明的实施例1中二羟基丙酮对HepG2、HCT116、SH-SY5Y、C-33A、MDA-MB-231细胞株的IC50统计结果。2 is an IC 50 statistical result of dihydroxyacetone to HepG2, HCT116, SH-SY5Y, C-33A, and MDA-MB-231 cell lines according to Example 1 of the present invention.

图3是根据本发明实施例13中各组相对肿瘤体积统计结果图;Figure 3 is a graph showing statistical results of relative tumor volume of each group in Example 13 according to the present invention;

图4是根据本发明实施例13中各组实验动物体重统计结果图;Figure 4 is a graph showing the results of body weight statistics of each group of experimental animals in Example 13 according to the present invention;

图5是根据本发明实施例13中各组肿瘤重量统计结果图;Figure 5 is a graph showing statistical results of tumor weight of each group in Example 13 according to the present invention;

图6是根据本发明实施例16中药盒示意图。Figure 6 is a schematic illustration of a medicine cartridge in accordance with Example 16 of the present invention.

发明详细描述Detailed description of the invention

下面详细描述本发明的实施例,所述实施例的示例在附图中示出,其中自始至终相同或类似的标号表示相同或类似的元件或具有相同或类似功能的元件。下面通过参考附图描述的实施例是示例性的,仅用于解释本发明,而不能理解为对本发明的限制。The embodiments of the present invention are described in detail below, and the examples of the embodiments are illustrated in the drawings, wherein the same or similar reference numerals are used to refer to the same or similar elements or elements having the same or similar functions. The embodiments described below with reference to the accompanying drawings are intended to be illustrative of the invention and are not to be construed as limiting.

实施例Example

实施例1Example 1

本发明中二羟基丙酮制药用途是通过以下实验证明的:The pharmaceutical use of dihydroxyacetone in the present invention is demonstrated by the following experiments:

1、实验方法1. Experimental method

1.1材料与设备 1.1 Materials and equipment

1.1.1试剂1.1.1 Reagents

Figure PCTCN2016083466-appb-000001
Figure PCTCN2016083466-appb-000001

1.1.2耗材1.1.2 consumables

Figure PCTCN2016083466-appb-000002
Figure PCTCN2016083466-appb-000002

1.1.3设备1.1.3 equipment

Figure PCTCN2016083466-appb-000003
Figure PCTCN2016083466-appb-000003

1.1.4实验药品1.1.4 Experimental drugs

市售1,3-二羟基丙酮固体粉末,每100mL 5%葡萄糖(输液瓶装)中加入该粉末15g,灌装至100瓶中。Commercially available 1,3-dihydroxyacetone solid powder, 15 g of this powder was added per 100 mL of 5% glucose (infusion bottle), and filled into 100 bottles.

对照化合物:顺铂(DDP):齐鲁制药有限公司,批号:2WA2A1404016A,20mg/瓶;使用5%葡萄糖溶液配置成1mg/ml储液,储存于-20℃。Control compound: cisplatin (DDP): Qilu Pharmaceutical Co., Ltd., batch number: 2WA2A1404016A, 20 mg/bottle; a 1 mg/ml stock solution was prepared using a 5% dextrose solution and stored at -20 °C.

1.2实验方法1.2 Experimental methods

1.2.1渗透压测定1.2.1 Determination of osmotic pressure

样品经过RPMI-1640培养基稀释至不同浓度,然后利用德国LOSER公司冰点渗透压 仪测定样品渗透压。The sample was diluted to different concentrations in RPMI-1640 medium, and then used by German LOSER ice point osmotic pressure The instrument measures the osmotic pressure of the sample.

1.2.2细胞培养条件1.2.2 Cell culture conditions

Figure PCTCN2016083466-appb-000004
Figure PCTCN2016083466-appb-000004

Figure PCTCN2016083466-appb-000005
Figure PCTCN2016083466-appb-000005

1.2.3细胞接种1.2.3 Cell Vaccination

消化细胞并计数(悬浮细胞直接计数)后,将细胞稀释至1.25×105个/ml,以每孔40μl接种至384孔板(5000细胞/孔),然后1500rpm离心1min,放至培养箱孵育过夜。After digesting cells and counting (suspensing cells directly counting), the cells were diluted to 1.25×10 5 /ml, inoculated into 384-well plates (5000 cells/well) at 40 μl per well, then centrifuged at 1500 rpm for 1 min, and placed in an incubator for incubation. overnight.

1.2.4细胞给药1.2.4 Cell Administration

将药物分别用5%葡萄糖溶液梯度稀释至5×,每孔给药10μl,每个浓度4个重复孔(n=4),培养箱继续培养72h后使用

Figure PCTCN2016083466-appb-000006
发光法细胞活力检测试剂盒检测细胞活力。The drug was diluted to 5× with 5% glucose solution, 10 μl per well, 4 replicate wells per concentration (n=4), and the incubator was further cultured for 72 h.
Figure PCTCN2016083466-appb-000006
The luminescence cell viability assay kit detects cell viability.

根据分子量折算,细胞给药浓度如下表:According to the molecular weight conversion, the concentration of the cells administered is as follows:

浓度设置Concentration setting mMmM 11 2020 22 1515 33 1010 44 55 55 2.52.5 66 1.251.25

1.2.5检测方法1.2.5 Detection method

每孔加入与培养基等体积的CellTiter-Glo试剂,置于振荡器上振荡5min摇匀,后1500rpm离心1min,室温避光孵育15min,于BMG PHERAstar检测化学发光。Add equal volume of CellTiter-Glo reagent to the medium, shake on a shaker for 5 min, shake at 1500 rpm for 1 min, incubate at room temperature for 15 min in the dark, and detect chemiluminescence at BMG PHERAstar.

细胞活力计算公式如下:The cell viability calculation formula is as follows:

细胞活力(Viability%)=100%×(LUM待测样品-LUMblank)/(LUM溶剂对照-LUMblank)Viability% = 100% × (LUM sample to be tested - LUM blank ) / (LUM solvent control - LUM blank )

1.2.6样品IC50计算1.2.6 Sample IC 50 calculation

利用Prism 6拟合Log[浓度]-细胞活力曲线,计算样品对各细胞系的IC50Fitting using Prism 6 Log [concentration] - cell viability curve, the samples for each cell line IC 50.

2实验结果2 experimental results

二羟基丙酮对肿瘤细胞增殖的影响如图1、2,表1。 The effect of dihydroxyacetone on tumor cell proliferation is shown in Figures 1, 2 and Table 1.

Figure PCTCN2016083466-appb-000007
Figure PCTCN2016083466-appb-000007

Figure PCTCN2016083466-appb-000008
Figure PCTCN2016083466-appb-000008

注:*,表示样品IC50以二羟基丙酮浓度计算;Note: *, indicating that the sample IC50 is calculated as the concentration of dihydroxyacetone;

N/A,表示未得到IC50N/A means that IC 50 is not obtained.

从结果可以看出,二羟基丙酮具有比较广谱的抗肿瘤细胞增殖的作用,实验中所涉及的34种常见的肿瘤细胞株,均可以得出IC50(半抑制浓度)值。说明二羟基丙酮对常见肿瘤均有强度不同的抑制作用,特别是对肉瘤、神经母细胞癌、骨髓瘤、结肠癌、肺癌、胃癌、白血病、甲状腺瘤等作用更加突出。It can be seen from the results that dihydroxyacetone has a broad spectrum of anti-tumor cell proliferation effects, and the IC 50 (semi-inhibitory concentration) values can be obtained for the 34 common tumor cell lines involved in the experiment. It shows that dihydroxyacetone has different inhibitory effects on common tumors, especially for sarcoma, neuroblastoma, myeloma, colon cancer, lung cancer, stomach cancer, leukemia and thyroid tumor.

综上所述,本发明提供的二羟基丙酮的新用途,其在抗多种癌症方面均表现出比较好的活性。加之二羟基丙酮在人体的应用已经非常广泛,是安全性良好的化学物质,因而本发明所提供的新用途,使得该物质在人体方面的应用得到了新的拓展,有望在保健食品、医药等领域得到更多的应用。In summary, the novel use of the dihydroxyacetone provided by the present invention exhibits relatively good activity against various cancers. In addition, dihydroxyacetone has been widely used in human body and is a chemical substance with good safety. Therefore, the new use provided by the present invention has newly expanded the application of the substance in human body, and is expected to be in health food, medicine, etc. The field gets more applications.

实施例2Example 2

片剂的制备Preparation of tablets

二羟基丙酮作为药物活性成分,加入药物载体,按照制剂学常规技术制备得到,如以下制备方法:As a pharmaceutically active ingredient, dihydroxyacetone is added to a pharmaceutical carrier and prepared according to conventional techniques of preparation, such as the following preparation method:

10mg二羟基丙酮,淀粉200mg,糖粉100mg,硬脂酸镁适量,用淀粉糊作为粘合剂,经混合,制粒,风干,整粒,压片,得到片剂。10 mg of dihydroxyacetone, 200 mg of starch, 100 mg of powdered sugar, and an appropriate amount of magnesium stearate were mixed with a starch paste as a binder, granulated, air-dried, sized, and tableted to obtain tablets.

实施例3Example 3

硬胶囊剂的制备Preparation of hard capsules

二羟基丙酮作为药物活性成分,加入药物载体,按照制剂学常规技术制备得到,如以下制备方法:As a pharmaceutically active ingredient, dihydroxyacetone is added to a pharmaceutical carrier and prepared according to conventional techniques of preparation, such as the following preparation method:

10mg二羟基丙酮,淀粉200mg,糖粉100mg,硬脂酸镁适量,用淀粉糊作为粘合剂,经混合,制粒,风干,整粒,装胶囊。10 mg of dihydroxyacetone, 200 mg of starch, 100 mg of powdered sugar, and an appropriate amount of magnesium stearate, using starch paste as a binder, mixing, granulating, air drying, whole granules, and capsules.

实施例4Example 4

软胶囊剂的制备 Preparation of soft capsules

二羟基丙酮作为药物活性成分,加入药物载体,按照制剂学常规技术制备得到,如以下制备方法:As a pharmaceutically active ingredient, dihydroxyacetone is added to a pharmaceutical carrier and prepared according to conventional techniques of preparation, such as the following preparation method:

10mg二羟基丙酮,大豆油100mg,聚乙二醇100mg,用明胶作囊壳,制备成软胶囊。10 mg of dihydroxyacetone, soybean oil 100 mg, and polyethylene glycol 100 mg were prepared into soft capsules using gelatin as a capsule.

实施例5Example 5

口服液的制备Preparation of oral liquid

二羟基丙酮作为药物活性成分,加入药物载体,按照制剂学常规技术制备得到,如以下制备方法:As a pharmaceutically active ingredient, dihydroxyacetone is added to a pharmaceutical carrier and prepared according to conventional techniques of preparation, such as the following preparation method:

10mg二羟基丙酮,甘油50mg,蔗糖100mg,香精适量,水加到10ml。10 mg of dihydroxyacetone, 50 mg of glycerin, 100 mg of sucrose, an appropriate amount of essence, and water was added to 10 ml.

实施例6Example 6

颗粒剂的制备Preparation of granules

二羟基丙酮作为药物活性成分,加入药物载体,按照制剂学常规技术制备得到,如以下制备方法:As a pharmaceutically active ingredient, dihydroxyacetone is added to a pharmaceutical carrier and prepared according to conventional techniques of preparation, such as the following preparation method:

10mg二羟基丙酮,糊精200mg,糖粉100mg,用水作为粘合剂,混合,制粒,风干,整粒,包装。10 mg of dihydroxyacetone, 200 mg of dextrin, 100 mg of powdered sugar, water as a binder, mixing, granulating, air drying, whole granules, and packaging.

实施例7Example 7

丸剂的制备Preparation of pills

二羟基丙酮作为药物活性成分,加入药物载体,按照制剂学常规技术制备得到,如以下制备方法:As a pharmaceutically active ingredient, dihydroxyacetone is added to a pharmaceutical carrier and prepared according to conventional techniques of preparation, such as the following preparation method:

10mg二羟基丙酮,加入羧甲基纤维素钠200mg,混和均匀,泛制丸,干燥,制成1000丸,包薄膜衣,即得。10 mg of dihydroxyacetone, 200 mg of sodium carboxymethylcellulose was added, and the mixture was uniformly mixed, and the pellet was prepared and dried to prepare 1000 pellets, which were obtained by coating a film.

实施例8Example 8

干混悬剂的制备Preparation of dry suspension

二羟基丙酮作为药物活性成分,加入药物载体,按照制剂学常规技术制备得到,如以下制备方法:As a pharmaceutically active ingredient, dihydroxyacetone is added to a pharmaceutical carrier and prepared according to conventional techniques of preparation, such as the following preparation method:

10g二羟基丙酮,羟丙甲基纤维素100g,微晶纤维素200g,蔗糖200g,混合:用50%乙醇制软材,制粒,风干,整粒,包装。 10 g of dihydroxyacetone, 100 g of hydroxypropylmethylcellulose, 200 g of microcrystalline cellulose, 200 g of sucrose, mixed: soft material made of 50% ethanol, granulated, air-dried, granulated, packaged.

实施例9Example 9

栓剂的制备Preparation of suppository

二羟基丙酮作为药物活性成分,加入药物载体,按照制剂学常规技术制备得到,如以下制备方法:As a pharmaceutically active ingredient, dihydroxyacetone is added to a pharmaceutical carrier and prepared according to conventional techniques of preparation, such as the following preparation method:

10g二羟基丙酮,可可豆脂600g,熔融基质、加入药物,混匀,注模、冷却、刮削、取出,即得。10g dihydroxyacetone, cocoa butter 600g, molten matrix, added drugs, mixed, injection molded, cooled, scraped, taken out, that is.

实施例10Example 10

滴丸剂的制备Preparation of pills

二羟基丙酮作为药物活性成分,加入药物载体,按照制剂学常规技术制备得到,如以下制备方法:As a pharmaceutically active ingredient, dihydroxyacetone is added to a pharmaceutical carrier and prepared according to conventional techniques of preparation, such as the following preparation method:

5g二羟基丙酮,60g聚乙二醇6000,5g dihydroxyacetone, 60g polyethylene glycol 6000,

取二羟基丙酮,加入已经融熔的聚乙二醇6000中混合,温度为60-90℃,融化并搅拌均匀后,移入滴丸机的滴灌中(保温70-90℃),滴入5-17℃的液状石蜡或甲基硅油中,取出滴丸,除去液状石蜡或甲基硅油,洗丸,干燥,制得滴丸1000丸。Take dihydroxyacetone, add it to the already melted polyethylene glycol 6000, the temperature is 60-90 ° C, melt and stir evenly, then transfer it into the drip irrigation of the dropping machine (insulation 70-90 ° C), drop 5- In the liquid paraffin or methyl silicone oil at 17 ° C, the dropping pills are taken out, the liquid paraffin or methyl silicone oil is removed, the pellet is washed, and dried to obtain 1000 pills of dropping pills.

实施例11Example 11

分散片剂的制备Preparation of dispersible tablets

二羟基丙酮作为药物活性成分,加入药物载体,按照制剂学常规技术制备得到,如以下制备方法:As a pharmaceutically active ingredient, dihydroxyacetone is added to a pharmaceutical carrier and prepared according to conventional techniques of preparation, such as the following preparation method:

5g二羟基丙酮,乳糖18g,预胶化淀粉25g,微晶纤维素35g,低取代羟丙基纤维素7g,聚乙烯吡咯烷酮6g,微粉硅胶1g.用水作为粘合剂,混合,制粒,风干,整粒,压片。5g dihydroxyacetone, lactose 18g, pregelatinized starch 25g, microcrystalline cellulose 35g, low substituted hydroxypropyl cellulose 7g, polyvinylpyrrolidone 6g, micronized silica gel 1g. Water as binder, mixing, granulation, air drying , whole grain, tableting.

实施例12Example 12

无糖颗粒剂的制备Preparation of sugar-free granules

二羟基丙酮作为药物活性成分,加入药物载体,按照制剂学常规技术制备得到,如以下制备方法:As a pharmaceutically active ingredient, dihydroxyacetone is added to a pharmaceutical carrier and prepared according to conventional techniques of preparation, such as the following preparation method:

10mg二羟基丙酮,甜菊素4mg糊精440mg。取组分1、糊精、甜菊素混匀,加95%乙醇制成软材,14目筛网制粒,50~55℃烘干,12目整粒,分装,即得。10 mg of dihydroxyacetone, stevioside 4 mg dextrin 440 mg. Take component 1, dextrin, stevia mixed, add 95% ethanol to make soft material, 14 mesh sieve granulation, 50 ~ 55 ° C drying, 12 mesh whole grain, sub-package, that is.

实施例13 Example 13

1试验材料1 test material

1.1供试品1.1 Test sample

名称:二羟基丙酮(DHA)固体粉末Name: Dihydroxyacetone (DHA) solid powder

提供单位:由苏州亚宝药物研发有限公司提供Provided by: Suzhou Yabao Drug Development Co., Ltd.

阳性对照:注射用顺铂(Cisplatin),批号:2WA2A1408055A,生产厂家:齐鲁制药有限公司,规格:20mg/瓶Positive control: Cisplatin for injection, batch number: 2WA2A1408055A, manufacturer: Qilu Pharmaceutical Co., Ltd., specification: 20mg/bottle

1.2试验动物1.2 test animals

种属、品系和等级:Balb/c-nude裸小鼠,SPF级Species, strains and ranks: Balb/c-nude nude mice, SPF grade

来源:上海灵畅生物科技有限公司Source: Shanghai Lingchang Biotechnology Co., Ltd.

许可证号:SCXK(沪)2013-00185License number: SCXK (Shanghai) 2013-00185

动物合格证号:2013001812253Animal certificate number: 2013001812253

体重:16-18g(到达时)Weight: 16-18g (on arrival)

性别:雄性Gender: Male

2试验方案2 test plan

裸鼠皮下接种H460细胞(人大细胞肺癌细胞株),待肿瘤长至体积100mm3左右时,从70只裸鼠中选出36只肿瘤体积相近、形状较好的裸鼠,分成6组,每组6只动物;Nude mice were subcutaneously inoculated with H460 cells (human large cell lung cancer cell line). When the tumor grew to a volume of about 100 mm 3 , 36 nude mice with similar tumor volume and good shape were selected from 70 nude mice, and divided into 6 groups. Group of 6 animals;

DHA组:p.o.,给药体积为0.1mL/10g,bid,共三周;DHA group: p.o., administration volume is 0.1mL/10g, bid, for three weeks;

DHA+Cisplatin组:二羟基丙酮(DHA):p.o.,给药体积为0.1mL/10g,bid;Cisplatin:4mg/kg,注射体积0.1mL/10g,i.p,每5天给药一次,共三周;DHA+Cisplatin group: dihydroxyacetone (DHA): po, administration volume 0.1 mL/10 g, bid; Cisplatin: 4 mg/kg, injection volume 0.1 mL/10 g, ip, once every 5 days for 3 weeks ;

Cisplatin组:4mg/kg,注射体积0.1mL/10g,i.p,每5天给药一次,共三周;Cisplatin group: 4 mg/kg, injection volume 0.1 mL/10 g, i.p, once every 5 days for a total of three weeks;

空白组:0.9%氯化钠注射液,给药方式同DHA组。Blank group: 0.9% sodium chloride injection, the same as the DHA group.

3实验方法3 experimental methods

3.1接种3.1 inoculation

3.1.1复苏并扩增H460细胞;3.1.1 Resuscitation and expansion of H460 cells;

3.1.2待扩增到足够的细胞,收集细胞,用不含血清的1640培养基配成浓度为2×107cell/mL的细胞悬液;3.1.2 To a sufficient number of cells to be expanded, collect the cells, and prepare a cell suspension with a concentration of 2×10 7 cells/mL using serum-free 1640 medium;

3.1.3裸鼠背部右侧皮下接种,0.1mL/只,即每只裸鼠接种细胞数为2×1063.1.3 nude mice were injected subcutaneously on the right side of the back, 0.1 mL/only, that is, the number of cells per nude mouse was 2×10 6 ;

3.1.4共接种70只裸鼠,接种后观察出瘤情况和肿瘤大小。3.1.4 A total of 70 nude mice were inoculated, and the tumor condition and tumor size were observed after inoculation.

3.2分组给药 3.2 group administration

3.2.1待肿瘤长至体积100mm3左右时,从70只裸鼠中选出36只肿瘤体积相近、形状较好的裸鼠,分成6组,每组各6只。3.2.1 When the tumor grew to a volume of about 100 mm 3 , 36 nude mice with similar tumor volume and good shape were selected from 70 nude mice, and divided into 6 groups, 6 in each group.

3.2.2分组3.2.2 grouping

同“2试验方案”Same as "2 test plan"

3.3药物配制3.3 drug preparation

DHA:称取固体粉末15.0g置于100mL容量瓶中,用5%葡萄糖注射液定容至刻度线,边超声边摇晃至完全溶解。未使用时4℃冷藏。DHA: Weigh 15.0 g of solid powder in a 100 mL volumetric flask, dilute to the mark with 5% glucose injection, and shake until ultrasonically dissolved completely. Refrigerated at 4 ° C when not in use.

DHA+Cisplatin:称取固体粉末二羟基丙酮15.0g置于100mL容量瓶中,用5%葡萄糖注射液定容至刻度线,边超声边摇晃至完全溶解。量取0.6mg/mL顺铂溶液4.0mL加2.0mL生理盐水,配制成0.4mg/mL(4mg/kg)顺铂溶液,未使用时4℃冷藏。DHA+Cisplatin: Weigh 15.0 g of solid powder dihydroxyacetone in a 100 mL volumetric flask, dilute to the mark with 5% glucose injection, and shake until ultrasonically dissolved completely. A solution of 0.6 mg/mL cisplatin solution 4.0 mL and 2.0 mL of physiological saline was added to prepare a 0.4 mg/mL (4 mg/kg) cisplatin solution, which was chilled at 4 ° C when not used.

所有样品每三天配置一次。All samples were configured every three days.

3.4测量3.4 Measurement

从给药第1天起,每周测量3次肿瘤体积和体重。第22天处死裸鼠,取出肿瘤称重、拍照,最后计算抑瘤率。Tumor volume and body weight were measured 3 times per week from the first day of administration. On the 22nd day, the nude mice were sacrificed, the tumors were removed and photographed, and the tumor inhibition rate was calculated.

3.5评价指标3.5 Evaluation indicators

肿瘤体积变化;动物体重变化;最后肿瘤重量。Tumor volume change; animal weight change; final tumor weight.

4检测指标及计算方法4 detection indicators and calculation methods

4.1肿瘤体积(tumor volume,TV)4.1 tumor volume (TV)

计算公式为:TV=1/2×a×b2,其中a、b分别表示长、宽。The calculation formula is: TV = 1/2 × a × b 2 , where a and b represent length and width, respectively.

4.2相对肿瘤体积(relative tumor volume,RTV)4.2 Relative tumor volume (RTV)

计算公式为:RTV=TVt/TV1,其中TV1为分笼给药时(即d1)肿瘤体积,TVt为每一次测量时的肿瘤体积。The formula is: RTV = TV t /TV 1 , where TV 1 is the tumor volume when the cage is administered (ie, d 1 ), and TV t is the tumor volume at each measurement.

4.3相对肿瘤增殖率T/C(%)4.3 Relative tumor proliferation rate T/C (%)

计算公式为:The calculation formula is:

Figure PCTCN2016083466-appb-000009
Figure PCTCN2016083466-appb-000009

TRTV:治疗组RTV;CRTV:空白对照组RTV。T RTV : treatment group RTV; C RTV : blank control group RTV.

4.4瘤重抑瘤率IR(%)4.4 tumor weight inhibition rate IR (%)

计算公式为: The calculation formula is:

Figure PCTCN2016083466-appb-000010
Figure PCTCN2016083466-appb-000010

TTW:治疗组瘤重;CTW:空白对照组瘤重;TW(tumor weight):肿瘤重量。T TW : tumor weight of treatment group; C TW : tumor weight of blank control group; TW (tumor weight): tumor weight.

5试验结果5 test results

具体结果见表2,表3和图3,图4及图5。The specific results are shown in Table 2, Table 3 and Figure 3, Figure 4 and Figure 5.

表2:动物数,体重,肿瘤体积(TV),相对肿瘤体积(RTV),相对肿瘤增殖率(T/C)Table 2: Number of animals, body weight, tumor volume (TV), relative tumor volume (RTV), relative tumor growth rate (T/C)

Figure PCTCN2016083466-appb-000011
Figure PCTCN2016083466-appb-000011

***P<0.01v.s.Blank(RTV)*:0.01<P<0.05v.s.Blank(RTV)***P<0.01v.s.Blank(RTV)*:0.01<P<0.05v.s.Blank(RTV)

表3:瘤重和瘤重抑瘤率Table 3: Tumor weight and tumor weight inhibition rate

Figure PCTCN2016083466-appb-000012
Figure PCTCN2016083466-appb-000012

*:0.01<P<0.05v.s.Blank *:0.01<P<0.05v.s.Blank

6结果讨论6 results discussion

6.1肿瘤生长情况:结果显示,各组肿瘤体积具有较好的离散度,标准偏差小于均数的1/4,空白组肿瘤生长良好,在试验终点时RTV=(1797.4±657.6)。6.1 Tumor growth: The results showed that the tumor volume of each group had a good dispersion, and the standard deviation was less than 1/4 of the mean. The tumor in the blank group grew well, and RTV=(1797.4±657.6) at the end of the experiment.

6.2体重:整个试验过程中,Cisplatin组、DHA+Cisplatin,体重下降明显,其余各组增长正常。6.2 Body weight: During the whole experiment, the Cisplatin group and DHA+Cisplatin showed significant weight loss, and the other groups grew normally.

6.3Cisplatin组:毒性反应非常明显,表现体重明显下降,体温下降,在试验终点时体重下降约16.7%,动物状态较差;定给药计划为每5天给药一次,最终给药次数4次。Cisplatin抑瘤效果明显(P=0.04),最后其T/C=60.3%,瘤重抑制率为44.6%。这也同时表明该试验体系可靠,可用于药效评价。6.3Cisplatin group: the toxicity was very obvious, the body weight decreased significantly, the body temperature decreased, the body weight decreased by about 16.7% at the end of the test, and the animal state was poor. The dosing schedule was once every 5 days, and the final dose was 4 times. . Cisplatin had a significant anti-tumor effect (P=0.04), and finally its T/C=60.3%, and the tumor weight inhibition rate was 44.6%. This also indicates that the test system is reliable and can be used for drug efficacy evaluation.

6.4DHA组:无毒性反应,本次试验模型中未表现出明显抑瘤作用。6.4 DHA group: no toxic reaction, no obvious anti-tumor effect in this test model.

6.5 DHA+Cisplatin组:有毒性反应,表现体重下降,体温下降,在试验终点时体重下降约15.7%,数值上较单独使用Cisplatin有所减少。DHA每天给药2次,Cisplatin定给药计划为每5天给药一次,最终给药次数4次。该组抑瘤效果非常明显(P=0.0059),最后其T/C=44.9%,瘤重抑制率为53.3%。6.5 DHA+Cisplatin group: toxic reaction, showing weight loss, decreased body temperature, weight loss at the end of the test was about 15.7%, and the value was reduced compared with Cisplatin alone. DHA is administered twice a day, Cisplatin is scheduled to be administered every 5 days, and the final dose is 4 times. The anti-tumor effect of this group was very obvious (P=0.0059), and finally its T/C=44.9%, and the tumor weight inhibition rate was 53.3%.

6.6小结6.6 Summary

在此次试验中,DHA+Cisplatin组在人大细胞肺癌H460细胞移植瘤模型上抑瘤效果明显强于Cisplatin组,且不会增加化药顺铂的毒性,认为DHA与化药顺铂联用可起到较好的抑瘤作用。In this trial, the DHA+Cisplatin group was significantly more potent in the human large cell lung cancer H460 cell xenograft model than the Cisplatin group, and did not increase the toxicity of the chemical cisplatin. It is believed that DHA can be combined with the chemical cisplatin. Play a better anti-tumor effect.

实施例14Example 14

市售二羟基丙酮(DHA),带有甜味的白色粉末状结晶。DHA 300g,加入羟丙甲纤维素200g,常规方法制成片剂40片、密封包装。顺铂0.0792g与氯化钠0.7g,加入蒸馏水80ml,无菌包装为注射剂4支。将DHA片剂和顺铂注射剂置入同一包装盒内,常规方法包装为药盒。Commercially available dihydroxyacetone (DHA) with a white powdery crystal of sweetness. 300 g of DHA, 200 g of hypromellose was added, and 40 tablets of tablets were prepared by a conventional method, and sealed. 0.0792 g of cisplatin and 0.7 g of sodium chloride were added to 80 ml of distilled water, and aseptically packaged as 4 injections. DHA tablets and cisplatin injections are placed in the same package and packaged as a kit in a conventional manner.

实施例15Example 15

市售二羟基丙酮(DHA)312g,平均分为40份,干燥室温环境下密封包装成小袋。顺铂0.076g,平均分为4份,密封包装为小瓶。使用时分别用注射用葡萄糖溶解。DHA口服,0.13g/kg(按人体重60kg计算,下同),一日两次,连续使用20天。顺铂静脉滴注或肌肉注射,0.317mg/kg,每5天用药一次。 Commercially available dihydroxyacetone (DHA) 312 g, divided into an average of 40 parts, was sealed and packaged into sachets under dry room temperature. Cisplatin 0.076g, divided into 4 parts on average, sealed package as a vial. When used, it is dissolved by glucose for injection. DHA orally, 0.13g / kg (calculated according to human body weight of 60kg, the same below), twice a day, continuous use for 20 days. Intravenous infusion or intramuscular injection of cisplatin, 0.317mg/kg, once every 5 days.

实施例16Example 16

抗肿瘤的药盒如图6所示。The anti-tumor kit is shown in Figure 6.

药盒(101)内置4个小瓶(102),分别密封包装顺铂注射液5ml(浓度3.98mg/ml)。另置40个密封包装袋(103),内分别有二羟基丙酮颗粒6.75g。药盒内还配有灭菌注射器(104)和服药杯(105)。使用时,将二羟基丙酮颗粒置于服药杯(105)内,溶于适量水中,餐后口服,112.5mg/kg,一日两次。顺铂用注射器(104)肌肉注射,0.339mg/kg,每5天注射1次。The vial (101) contains 4 vials (102), which are respectively sealed with 5 ml of cisplatin injection (concentration 3.98 mg/ml). Another 40 sealed packaging bags (103) were provided with 6.75 g of dihydroxyacetone particles. A sterile syringe (104) and a medication cup (105) are also provided in the kit. When in use, the dihydroxyacetone particles are placed in the medication cup (105), dissolved in an appropriate amount of water, orally administered after meals, 112.5 mg/kg twice a day. Cisplatin was intramuscularly injected with a syringe (104) at 0.339 mg/kg once every 5 days.

需要说明的是,术语“第一”、“第二”仅用于描述目的,而不能理解为指示或暗示相对重要性或者隐含指明所指示的技术特征的数量。由此,限定有“第一”、“第二”的特征可以明示或者隐含地包括一个或者更多个该特征。进一步地,在本发明的描述中,除非另有说明,“多个”的含义是两个或两个以上。It should be noted that the terms "first" and "second" are used for descriptive purposes only, and are not to be construed as indicating or implying a relative importance or implicitly indicating the number of technical features indicated. Thus, features defining "first" and "second" may include one or more of the features either explicitly or implicitly. Further, in the description of the present invention, the meaning of "a plurality" is two or more unless otherwise specified.

在本说明书的描述中,参考术语“一个实施例”、“一些实施例”、“示意性实施例”、“示例”、“具体示例”、或“一些示例”等的描述意指结合该实施例或示例描述的具体特征、结构、材料或者特点包含于本发明的至少一个实施例或示例中。在本说明书中,对上述术语的示意性表述不一定指的是相同的实施例或示例。而且,描述的具体特征、结构、材料或者特点可以在任何的一个或多个实施例或示例中以合适的方式结合。In the description of the present specification, the description with reference to the terms "one embodiment", "some embodiments", "illustrative embodiment", "example", "specific example", or "some examples", etc. Particular features, structures, materials or features described in the examples or examples are included in at least one embodiment or example of the invention. In the present specification, the schematic representation of the above terms does not necessarily mean the same embodiment or example. Furthermore, the particular features, structures, materials, or characteristics described may be combined in a suitable manner in any one or more embodiments or examples.

尽管本发明的具体实施方式已经得到详细的描述,本领域技术人员将会理解。根据已经公开的所有教导,可以对那些细节进行各种修改和替换,这些改变均在本发明的保护范围之内。本发明的全部范围由所附权利要求及其任何等同物给出。 Although specific embodiments of the invention have been described in detail, those skilled in the art will understand. Various modifications and alterations of the details are possible in light of the teachings of the invention. The full scope of the invention is given by the appended claims and any equivalents thereof.

Claims (46)

二羟基丙酮在制备药物中的用途,其中,所述药物用于治疗肿瘤。The use of dihydroxyacetone in the preparation of a medicament for the treatment of a tumor. 根据权利要求1所述的用途,其特征在于,所述肿瘤包括选自神经系统肿瘤、消化系统肿瘤、生殖系统肿瘤、泌尿系统肿瘤、皮肤肿瘤、骨肿瘤、关节系统肿瘤、呼吸系统肿瘤、血液及腺体肿瘤的至少一种。The use according to claim 1, wherein the tumor comprises a tumor selected from the group consisting of a nervous system tumor, a digestive system tumor, a reproductive system tumor, a urinary system tumor, a skin tumor, a bone tumor, a joint system tumor, a respiratory tumor, a blood. And at least one of glandular tumors. 根据权利要求1所述的用途,其特征在于,所述肿瘤包括选自神经母细胞癌、胶质瘤、结肠癌、直肠癌、肝癌、胃癌、胰腺癌、宫颈癌、乳腺癌、卵巢癌、前列腺癌、膀胱癌、黑色素瘤、表皮鳞状细胞癌、横纹肌瘤、多发性骨髓瘤、肉瘤、肺癌、咽喉癌、口腔癌、白血病、淋巴瘤、甲状腺癌的至少一种。The use according to claim 1, wherein the tumor comprises a patient selected from the group consisting of neuroblastoma, glioma, colon cancer, rectal cancer, liver cancer, gastric cancer, pancreatic cancer, cervical cancer, breast cancer, ovarian cancer, At least one of prostate cancer, bladder cancer, melanoma, epidermal squamous cell carcinoma, rhabdomyosarcoma, multiple myeloma, sarcoma, lung cancer, throat cancer, oral cancer, leukemia, lymphoma, thyroid cancer. 二羟基丙酮在治疗肿瘤中的用途。The use of dihydroxyacetone in the treatment of tumors. 根据权利要求4所述的用途,其特征在于,所述肿瘤包括选自神经系统肿瘤、消化系统肿瘤、生殖系统肿瘤、泌尿系统肿瘤、皮肤肿瘤、骨肿瘤、关节系统肿瘤、呼吸系统肿瘤、血液及腺体肿瘤的至少一种。The use according to claim 4, wherein the tumor comprises a tumor selected from the group consisting of a nervous system tumor, a digestive system tumor, a reproductive system tumor, a urinary system tumor, a skin tumor, a bone tumor, a joint system tumor, a respiratory tumor, a blood And at least one of glandular tumors. 根据权利要求4所述的用途,其特征在于,所述肿瘤包括选自神经母细胞癌、胶质瘤、结肠癌、直肠癌、肝癌、胃癌、胰腺癌、宫颈癌、乳腺癌、卵巢癌、前列腺癌、膀胱癌、黑色素瘤、表皮鳞状细胞癌、横纹肌瘤、多发性骨髓瘤、肉瘤、肺癌、咽喉癌、口腔癌、白血病、淋巴瘤、甲状腺癌的至少一种。The use according to claim 4, wherein the tumor comprises a patient selected from the group consisting of neuroblastoma, glioma, colon cancer, rectal cancer, liver cancer, gastric cancer, pancreatic cancer, cervical cancer, breast cancer, ovarian cancer, At least one of prostate cancer, bladder cancer, melanoma, epidermal squamous cell carcinoma, rhabdomyosarcoma, multiple myeloma, sarcoma, lung cancer, throat cancer, oral cancer, leukemia, lymphoma, thyroid cancer. 一种治疗肿瘤的方法,其特征在于,包含给予患者二羟基丙酮。A method of treating a tumor comprising administering to a patient dihydroxyacetone. 根据权利要求7所述的方法,其特征在于,所述肿瘤包括选自神经系统肿瘤、消化系统肿瘤、生殖系统肿瘤、泌尿系统肿瘤、皮肤肿瘤、骨肿瘤、关节系统肿瘤、呼吸系统肿瘤、血液及腺体肿瘤的至少一种。The method according to claim 7, wherein the tumor comprises a tumor selected from the group consisting of a nervous system tumor, a digestive system tumor, a reproductive system tumor, a urinary system tumor, a skin tumor, a bone tumor, a joint system tumor, a respiratory tumor, a blood. And at least one of glandular tumors. 根据权利要求7所述的方法,其特征在于,所述肿瘤包括选自神经母细胞癌、胶质瘤、结肠癌、直肠癌、肝癌、胃癌、胰腺癌、宫颈癌、乳腺癌、卵巢癌、前列腺癌、膀胱癌、黑色素瘤、表皮鳞状细胞癌、横纹肌瘤、多发性骨髓瘤、肉瘤、肺癌、咽喉癌、口腔癌、白血病、淋巴瘤、甲状腺癌的至少一种。The method according to claim 7, wherein the tumor comprises a patient selected from the group consisting of neuroblastoma, glioma, colon cancer, rectal cancer, liver cancer, gastric cancer, pancreatic cancer, cervical cancer, breast cancer, ovarian cancer, At least one of prostate cancer, bladder cancer, melanoma, epidermal squamous cell carcinoma, rhabdomyosarcoma, multiple myeloma, sarcoma, lung cancer, throat cancer, oral cancer, leukemia, lymphoma, thyroid cancer. 一种抗肿瘤的药物组合物,其特征在于,含有二羟基丙酮作为活性成分。An antitumor pharmaceutical composition comprising dihydroxyacetone as an active ingredient. 根据权利要求10所述的药物组合物,其特征在于,所述肿瘤包括选自神经系统肿瘤、消化系统肿瘤、生殖系统肿瘤、泌尿系统肿瘤、皮肤肿瘤、骨肿瘤、关节系统肿瘤、呼吸系统肿瘤、血液及腺体肿瘤的至少一种。The pharmaceutical composition according to claim 10, wherein the tumor comprises a tumor selected from the group consisting of a nervous system tumor, a digestive system tumor, a reproductive system tumor, a urinary system tumor, a skin tumor, a bone tumor, a joint system tumor, and a respiratory tumor. At least one of blood and gland tumors. 根据权利要求10所述的药物组合物,其特征在于,所述肿瘤包括选自神经母细胞 癌、胶质瘤、结肠癌、直肠癌、肝癌、胃癌、胰腺癌、宫颈癌、乳腺癌、卵巢癌、前列腺癌和膀胱癌、黑色素瘤、表皮鳞状细胞癌、横纹肌瘤、多发性骨髓瘤、肉瘤、肺癌、咽喉癌、口腔癌、白血病、淋巴瘤、甲状腺癌的至少一种。The pharmaceutical composition according to claim 10, wherein said tumor comprises a neuroblast selected from the group consisting of Cancer, glioma, colon cancer, rectal cancer, liver cancer, stomach cancer, pancreatic cancer, cervical cancer, breast cancer, ovarian cancer, prostate cancer and bladder cancer, melanoma, epidermal squamous cell carcinoma, rhabdomyomas, multiple myeloma At least one of sarcoma, lung cancer, throat cancer, oral cancer, leukemia, lymphoma, thyroid cancer. 一种抗肿瘤的药物组合物,其特征在于,含有二羟基丙酮和顺铂作为有效成分。An antitumor pharmaceutical composition comprising dihydroxyacetone and cisplatin as active ingredients. 根据权利要求13所述的药物组合物,其特征在于,所述肿瘤包括选自神经系统肿瘤、消化系统肿瘤、生殖系统肿瘤、泌尿系统肿瘤、皮肤肿瘤、骨肿瘤、关节系统肿瘤、呼吸系统肿瘤、血液及腺体肿瘤的至少一种。The pharmaceutical composition according to claim 13, wherein the tumor comprises a tumor selected from the group consisting of a nervous system tumor, a digestive system tumor, a reproductive system tumor, a urinary system tumor, a skin tumor, a bone tumor, a joint system tumor, and a respiratory tumor. At least one of blood and gland tumors. 根据权利要求13所述的药物组合物,其特征在于,所述肿瘤包括选自神经母细胞癌、胶质瘤、结肠癌、直肠癌、肝癌、胃癌、胰腺癌、宫颈癌、乳腺癌、卵巢癌、前列腺癌、膀胱癌、黑色素瘤、表皮鳞状细胞癌、横纹肌瘤、多发性骨髓瘤、肉瘤、肺癌、咽喉癌、口腔癌、白血病、淋巴瘤、甲状腺癌的至少一种。The pharmaceutical composition according to claim 13, wherein the tumor comprises a patient selected from the group consisting of neuroblastoma, glioma, colon cancer, rectal cancer, liver cancer, gastric cancer, pancreatic cancer, cervical cancer, breast cancer, and ovary At least one of cancer, prostate cancer, bladder cancer, melanoma, epidermal squamous cell carcinoma, rhabdomyosarcoma, multiple myeloma, sarcoma, lung cancer, throat cancer, oral cancer, leukemia, lymphoma, thyroid cancer. 一种抗肿瘤的药物联合,其特征在于,由二羟基丙酮和顺铂组成。An antitumor drug combination characterized by consisting of dihydroxyacetone and cisplatin. 根据权利要求16所述的药物联合,其特征在于,二羟基丙酮呈口服制剂形式,顺铂呈注射剂形式。The pharmaceutical combination according to claim 16, wherein the dihydroxyacetone is in the form of an oral preparation, and the cisplatin is in the form of an injection. 根据权利要求16所述的药物联合,其特征在于,所述肿瘤包括选自神经系统肿瘤、消化系统肿瘤、生殖系统肿瘤、泌尿系统肿瘤、皮肤肿瘤、骨肿瘤、关节系统肿瘤、呼吸系统肿瘤、血液及腺体肿瘤的至少一种。The pharmaceutical combination according to claim 16, wherein the tumor comprises a tumor selected from the group consisting of a nervous system tumor, a digestive system tumor, a reproductive system tumor, a urinary system tumor, a skin tumor, a bone tumor, a joint system tumor, a respiratory tumor, At least one of blood and gland tumors. 根据权利要求16所述的药物联合,其特征在于,所述肿瘤包括选自神经母细胞癌、胶质瘤、结肠癌、直肠癌、肝癌、胃癌、胰腺癌、宫颈癌、乳腺癌、卵巢癌、前列腺癌、膀胱癌、黑色素瘤、表皮鳞状细胞癌、横纹肌瘤、多发性骨髓瘤、肉瘤、肺癌、咽喉癌、口腔癌、白血病、淋巴瘤、甲状腺癌的至少一种。The pharmaceutical combination according to claim 16, wherein the tumor comprises a patient selected from the group consisting of neuroblastoma, glioma, colon cancer, rectal cancer, liver cancer, gastric cancer, pancreatic cancer, cervical cancer, breast cancer, ovarian cancer. At least one of prostate cancer, bladder cancer, melanoma, epidermal squamous cell carcinoma, rhabdomyosarcoma, multiple myeloma, sarcoma, lung cancer, throat cancer, oral cancer, leukemia, lymphoma, thyroid cancer. 二羟基丙酮在制备药物中的用途,其中,所述药物用于治疗肿瘤,为受试者同时给药二羟基丙酮和顺铂。The use of dihydroxyacetone in the preparation of a medicament for the treatment of a tumor, wherein the subject is simultaneously administered with dihydroxyacetone and cisplatin. 根据权利要求20所述的用途,其特征在于,所述肿瘤包括选自神经系统肿瘤、消化系统肿瘤、生殖系统肿瘤、泌尿系统肿瘤、皮肤肿瘤、骨肿瘤、关节系统肿瘤、呼吸系统肿瘤、血液及腺体肿瘤的至少一种。The use according to claim 20, wherein the tumor comprises a tumor selected from the group consisting of a nervous system tumor, a digestive system tumor, a reproductive system tumor, a urinary system tumor, a skin tumor, a bone tumor, a joint system tumor, a respiratory tumor, a blood And at least one of glandular tumors. 根据权利要求20所述的用途,其特征在于,所述肿瘤包括选自神经母细胞癌、胶质瘤、结肠癌、直肠癌、肝癌、胃癌、胰腺癌、宫颈癌、乳腺癌、卵巢癌、前列腺癌、膀胱癌、黑色素瘤、表皮鳞状细胞癌、横纹肌瘤、多发性骨髓瘤、肉瘤、肺癌、咽喉癌、口腔癌、白血病、淋巴瘤、甲状腺癌的至少一种。The use according to claim 20, wherein the tumor comprises a patient selected from the group consisting of neuroblastoma, glioma, colon cancer, rectal cancer, liver cancer, gastric cancer, pancreatic cancer, cervical cancer, breast cancer, ovarian cancer, At least one of prostate cancer, bladder cancer, melanoma, epidermal squamous cell carcinoma, rhabdomyosarcoma, multiple myeloma, sarcoma, lung cancer, throat cancer, oral cancer, leukemia, lymphoma, thyroid cancer. 二羟基丙酮在治疗肿瘤中的用途,其中,为受试者同时给药二羟基丙酮和顺铂。 The use of dihydroxyacetone in the treatment of tumors wherein dihydroxyacetone and cisplatin are administered simultaneously to the subject. 根据权利要求23所述的用途,其特征在于,所述肿瘤包括选自神经系统肿瘤、消化系统肿瘤、生殖系统肿瘤、泌尿系统肿瘤、皮肤肿瘤、骨肿瘤、关节系统肿瘤、呼吸系统肿瘤、血液及腺体肿瘤的至少一种。The use according to claim 23, wherein the tumor comprises a tumor selected from the group consisting of a nervous system tumor, a digestive system tumor, a reproductive system tumor, a urinary system tumor, a skin tumor, a bone tumor, a joint system tumor, a respiratory tumor, a blood And at least one of glandular tumors. 根据权利要求23所述的用途,其特征在于,所述肿瘤包括选自神经母细胞癌、胶质瘤、结肠癌、直肠癌、肝癌、胃癌、胰腺癌、宫颈癌、乳腺癌、卵巢癌、前列腺癌、膀胱癌、黑色素瘤、表皮鳞状细胞癌、横纹肌瘤、多发性骨髓瘤、肉瘤、肺癌、咽喉癌、口腔癌、白血病、淋巴瘤、甲状腺癌的至少一种。The use according to claim 23, wherein the tumor comprises a patient selected from the group consisting of neuroblastoma, glioma, colon cancer, rectal cancer, liver cancer, gastric cancer, pancreatic cancer, cervical cancer, breast cancer, ovarian cancer, At least one of prostate cancer, bladder cancer, melanoma, epidermal squamous cell carcinoma, rhabdomyosarcoma, multiple myeloma, sarcoma, lung cancer, throat cancer, oral cancer, leukemia, lymphoma, thyroid cancer. 一种治疗肿瘤的方法,其特征在于,包含给予患者二羟基丙酮,其中,为受试者同时给药二羟基丙酮和顺铂。A method for treating a tumor, comprising administering a dihydroxyacetone to a patient, wherein the subject simultaneously administered dihydroxyacetone and cisplatin. 根据权利要求26所述的方法,其特征在于,所述肿瘤包括选自神经系统肿瘤、消化系统肿瘤、生殖系统肿瘤、泌尿系统肿瘤、皮肤肿瘤、骨肿瘤、关节系统肿瘤、呼吸系统肿瘤、血液及腺体肿瘤的至少一种。The method according to claim 26, wherein said tumor comprises a tumor selected from the group consisting of a nervous system tumor, a digestive system tumor, a reproductive system tumor, a urinary system tumor, a skin tumor, a bone tumor, a joint system tumor, a respiratory tumor, a blood And at least one of glandular tumors. 根据权利要求26所述的方法,其特征在于,所述肿瘤包括选自神经母细胞癌、胶质瘤、结肠癌、直肠癌、肝癌、胃癌、胰腺癌、宫颈癌、乳腺癌、卵巢癌、前列腺癌、膀胱癌、黑色素瘤、表皮鳞状细胞癌、横纹肌瘤、多发性骨髓瘤、肉瘤、肺癌、咽喉癌、口腔癌、白血病、淋巴瘤、甲状腺癌的至少一种。The method according to claim 26, wherein said tumor comprises a patient selected from the group consisting of neuroblastoma, glioma, colon cancer, rectal cancer, liver cancer, gastric cancer, pancreatic cancer, cervical cancer, breast cancer, ovarian cancer, At least one of prostate cancer, bladder cancer, melanoma, epidermal squamous cell carcinoma, rhabdomyosarcoma, multiple myeloma, sarcoma, lung cancer, throat cancer, oral cancer, leukemia, lymphoma, thyroid cancer. 二羟基丙酮和顺铂的组合在制备药物中的用途,所述药物用于治疗肿瘤。The use of a combination of dihydroxyacetone and cisplatin for the preparation of a medicament for the treatment of a tumor. 根据权利要求29所述的用途,其特征在于,所述肿瘤包括选自神经系统肿瘤、消化系统肿瘤、生殖系统肿瘤、泌尿系统肿瘤、皮肤肿瘤、骨肿瘤、关节系统肿瘤、呼吸系统肿瘤、血液及腺体肿瘤的至少一种。The use according to claim 29, wherein the tumor comprises a tumor selected from the group consisting of a nervous system tumor, a digestive system tumor, a reproductive system tumor, a urinary system tumor, a skin tumor, a bone tumor, a joint system tumor, a respiratory tumor, a blood And at least one of glandular tumors. 根据权利要求29所述的用途,其特征在于,所述肿瘤包括选自神经母细胞癌、胶质瘤、结肠癌、直肠癌、肝癌、胃癌、胰腺癌、宫颈癌、乳腺癌、卵巢癌、前列腺癌、膀胱癌、黑色素瘤、表皮鳞状细胞癌、横纹肌瘤、多发性骨髓瘤、肉瘤、肺癌、咽喉癌、口腔癌、白血病、淋巴瘤、甲状腺癌的至少一种。The use according to claim 29, wherein the tumor comprises a patient selected from the group consisting of neuroblastoma, glioma, colon cancer, rectal cancer, liver cancer, gastric cancer, pancreatic cancer, cervical cancer, breast cancer, ovarian cancer, At least one of prostate cancer, bladder cancer, melanoma, epidermal squamous cell carcinoma, rhabdomyosarcoma, multiple myeloma, sarcoma, lung cancer, throat cancer, oral cancer, leukemia, lymphoma, thyroid cancer. 二羟基丙酮和顺铂的组合在治疗肿瘤中的用途。The use of a combination of dihydroxyacetone and cisplatin in the treatment of tumors. 根据权利要求32所述的用途,其特征在于,所述肿瘤包括选自神经系统肿瘤、消化系统肿瘤、生殖系统肿瘤、泌尿系统肿瘤、皮肤肿瘤、骨肿瘤、关节系统肿瘤、呼吸系统肿瘤、血液及腺体肿瘤的至少一种。The use according to claim 32, wherein the tumor comprises a tumor selected from the group consisting of a nervous system tumor, a digestive system tumor, a reproductive system tumor, a urinary system tumor, a skin tumor, a bone tumor, a joint system tumor, a respiratory tumor, a blood And at least one of glandular tumors. 根据权利要求32所述的用途,其特征在于,所述肿瘤包括选自神经母细胞癌、胶质瘤、结肠癌、直肠癌、肝癌、胃癌、胰腺癌、宫颈癌、乳腺癌、卵巢癌、前列腺癌、膀胱癌、黑色素瘤、表皮鳞状细胞癌、横纹肌瘤、多发性骨髓瘤、肉瘤、肺癌、咽喉癌、口 腔癌、白血病、淋巴瘤、甲状腺癌的至少一种。The use according to claim 32, wherein the tumor comprises a patient selected from the group consisting of neuroblastoma, glioma, colon cancer, rectal cancer, liver cancer, gastric cancer, pancreatic cancer, cervical cancer, breast cancer, ovarian cancer, Prostate cancer, bladder cancer, melanoma, epidermal squamous cell carcinoma, rhabdomyomas, multiple myeloma, sarcoma, lung cancer, throat cancer, mouth At least one of luminal cancer, leukemia, lymphoma, thyroid cancer. 一种治疗肿瘤的方法,其特征在于,包含给予患者二羟基丙酮和顺铂的组合。A method of treating a tumor comprising administering a combination of dihydroxyacetone and cisplatin to a patient. 根据权利要求35所述的方法,其特征在于,所述肿瘤包括选自神经系统肿瘤、消化系统肿瘤、生殖系统肿瘤、泌尿系统肿瘤、皮肤肿瘤、骨肿瘤、关节系统肿瘤、呼吸系统肿瘤、血液及腺体肿瘤的至少一种。The method according to claim 35, wherein said tumor comprises a tumor selected from the group consisting of a nervous system tumor, a digestive system tumor, a reproductive system tumor, a urinary system tumor, a skin tumor, a bone tumor, a joint system tumor, a respiratory tumor, a blood. And at least one of glandular tumors. 根据权利要求35所述的方法,其特征在于,所述肿瘤包括选自神经母细胞癌、胶质瘤、结肠癌、直肠癌、肝癌、胃癌、胰腺癌、宫颈癌、乳腺癌、卵巢癌、前列腺癌、膀胱癌、黑色素瘤、表皮鳞状细胞癌、横纹肌瘤、多发性骨髓瘤、肉瘤、肺癌、咽喉癌、口腔癌、白血病、淋巴瘤、甲状腺癌的至少一种。The method according to claim 35, wherein said tumor comprises a patient selected from the group consisting of neuroblastoma, glioma, colon cancer, rectal cancer, liver cancer, gastric cancer, pancreatic cancer, cervical cancer, breast cancer, ovarian cancer, At least one of prostate cancer, bladder cancer, melanoma, epidermal squamous cell carcinoma, rhabdomyosarcoma, multiple myeloma, sarcoma, lung cancer, throat cancer, oral cancer, leukemia, lymphoma, thyroid cancer. 一种用于抗肿瘤的药盒,其中包括二羟基丙酮和顺铂。A kit for anti-tumor, which includes dihydroxyacetone and cisplatin. 根据权利要求38所述的药盒,其特征在于,二羟基丙酮和顺铂设置在不同的容器中。A kit according to claim 38, wherein dihydroxyacetone and cisplatin are disposed in different containers. 根据权利要求38所述的药盒,其特征在于,二羟基丙酮呈口服制剂形式,顺铂呈注射剂形式。The kit according to claim 38, wherein the dihydroxyacetone is in the form of an oral preparation, and the cisplatin is in the form of an injection. 根据权利要求38所述的药盒,其特征在于,二羟基丙酮和顺铂的重量比为(3375-4125):1。The kit according to claim 38, wherein the weight ratio of dihydroxyacetone to cisplatin is (3375-4125):1. 根据权利要求38所述的药盒,其特征在于,所述肿瘤包括选自神经系统肿瘤、消化系统肿瘤、生殖系统肿瘤、泌尿系统肿瘤、皮肤肿瘤、骨肿瘤、关节系统肿瘤、呼吸系统肿瘤、血液及腺体肿瘤的至少一种。The kit according to claim 38, wherein said tumor comprises a tumor selected from the group consisting of a nervous system tumor, a digestive system tumor, a reproductive system tumor, a urinary system tumor, a skin tumor, a bone tumor, a joint system tumor, a respiratory tumor, At least one of blood and gland tumors. 根据权利要求38所述的药盒,其特征在于,所述肿瘤包括选自神经母细胞癌、胶质瘤、结肠癌、直肠癌、肝癌、胃癌、胰腺癌、宫颈癌、乳腺癌、卵巢癌、前列腺癌、膀胱癌、黑色素瘤、表皮鳞状细胞癌、横纹肌瘤、多发性骨髓瘤、肉瘤、肺癌、咽喉癌、口腔癌、白血病、淋巴瘤、甲状腺癌的至少一种。The kit according to claim 38, wherein said tumor comprises a patient selected from the group consisting of neuroblastoma, glioma, colon cancer, rectal cancer, liver cancer, gastric cancer, pancreatic cancer, cervical cancer, breast cancer, ovarian cancer At least one of prostate cancer, bladder cancer, melanoma, epidermal squamous cell carcinoma, rhabdomyosarcoma, multiple myeloma, sarcoma, lung cancer, throat cancer, oral cancer, leukemia, lymphoma, thyroid cancer. 二羟基丙酮和顺铂的组合在制备药盒中的用途,所述药盒用于治疗肿瘤。The use of a combination of dihydroxyacetone and cisplatin in the manufacture of a kit for the treatment of a tumor. 根据权利要求44所述的用途,其特征在于,所述肿瘤包括选自神经系统肿瘤、消化系统肿瘤、生殖系统肿瘤、泌尿系统肿瘤、皮肤肿瘤、骨肿瘤、关节系统肿瘤、呼吸系统肿瘤、血液及腺体肿瘤的至少一种。The use according to claim 44, wherein the tumor comprises a tumor selected from the group consisting of a nervous system tumor, a digestive system tumor, a reproductive system tumor, a urinary system tumor, a skin tumor, a bone tumor, a joint system tumor, a respiratory tumor, a blood And at least one of glandular tumors. 根据权利要求44所述的用途,其特征在于,所述肿瘤包括选自神经母细胞癌、胶质瘤、结肠癌、直肠癌、肝癌、胃癌、胰腺癌、宫颈癌、乳腺癌、卵巢癌、前列腺癌、膀胱癌、黑色素瘤、表皮鳞状细胞癌、横纹肌瘤、多发性骨髓瘤、肉瘤、肺癌、咽喉癌、口腔癌、白血病、淋巴瘤、甲状腺癌的至少一种。 The use according to claim 44, wherein the tumor comprises a patient selected from the group consisting of neuroblastoma, glioma, colon cancer, rectal cancer, liver cancer, gastric cancer, pancreatic cancer, cervical cancer, breast cancer, ovarian cancer, At least one of prostate cancer, bladder cancer, melanoma, epidermal squamous cell carcinoma, rhabdomyosarcoma, multiple myeloma, sarcoma, lung cancer, throat cancer, oral cancer, leukemia, lymphoma, thyroid cancer.
PCT/CN2016/083466 2015-08-24 2016-05-26 Use of dihydroxyacetone in preparation of anti-tumour drug Ceased WO2017032111A1 (en)

Priority Applications (6)

Application Number Priority Date Filing Date Title
KR1020187004813A KR101965319B1 (en) 2015-08-24 2016-05-26 Use of dihydroxyacetone in the manufacture of antitumor drugs
JP2018503509A JP6533866B2 (en) 2015-08-24 2016-05-26 Use of dihydroxyacetone for producing antineoplastic agents
AU2016311704A AU2016311704B2 (en) 2015-08-24 2016-05-26 Use of dihydroxyacetone in preparation of anti-cancer medicaments
EP16838371.9A EP3342406B1 (en) 2015-08-24 2016-05-26 Dihydroxyacetone for use in the preparation of an anti-tumour drug
US15/750,726 US10300026B2 (en) 2015-08-24 2016-05-26 Use of dihydroxyacetone in preparation of anti-cancer medicaments
CA2992629A CA2992629C (en) 2015-08-24 2016-05-26 Use of dihydroxyacetone in preparation of anti-cancer medicaments

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
CN201510523222.6 2015-08-24
CN201510523222 2015-08-24
CN201510867079.2A CN106806382B (en) 2015-12-01 2015-12-01 anticancer composition
CN201510867132.9 2015-12-01
CN201510867079.2 2015-12-01
CN201510867132.9A CN106474097B (en) 2015-08-24 2015-12-01 Anticancer agent

Publications (1)

Publication Number Publication Date
WO2017032111A1 true WO2017032111A1 (en) 2017-03-02

Family

ID=58099486

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/CN2016/083466 Ceased WO2017032111A1 (en) 2015-08-24 2016-05-26 Use of dihydroxyacetone in preparation of anti-tumour drug

Country Status (1)

Country Link
WO (1) WO2017032111A1 (en)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN111467329A (en) * 2020-05-22 2020-07-31 张建国 Application of 1, 3-dihydroxyacetone and 2, 4-dihydroxybenzoic acid in preparing food and medicine for treating cancer
CN113713026A (en) * 2021-08-20 2021-11-30 上海市第七人民医院(上海中医药大学附属第七人民医院) Anti-tumor extract of daphne genkwa as well as preparation method and application thereof

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1679526A (en) * 2005-01-21 2005-10-12 成中田 External-applied medicine for treating achromoderma and production thereof

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1679526A (en) * 2005-01-21 2005-10-12 成中田 External-applied medicine for treating achromoderma and production thereof

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
PETERSEN, A.B ET AL.: "Sunless skin tanning with dihydroxyacetone delays broad-spectrum ultraviolet photocarcinogenesis in hairless mice.", MUTATION RESEARCH, vol. 542, 31 December 2003 (2003-12-31), pages 129 - 138, XP055365041 *
See also references of EP3342406A4 *

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN111467329A (en) * 2020-05-22 2020-07-31 张建国 Application of 1, 3-dihydroxyacetone and 2, 4-dihydroxybenzoic acid in preparing food and medicine for treating cancer
CN113713026A (en) * 2021-08-20 2021-11-30 上海市第七人民医院(上海中医药大学附属第七人民医院) Anti-tumor extract of daphne genkwa as well as preparation method and application thereof

Similar Documents

Publication Publication Date Title
JP6577143B2 (en) Dosage form composition comprising an inhibitor of breton tyrosine kinase
TW200409640A (en) Stable oxaliplatin solution formulation and pharmaceutical composition, and method for stabilizing a formulation of oxaliplatin
WO2019007368A1 (en) Use of isovalerylspiramycin i, ii and/or iii in preparation of drug for treating and/or preventing tumour, and drug
CN105753719B (en) A kind of trientine hydrochloride compound
JP2016512526A (en) Onapristone polymorphs and methods of use
CN104918630A (en) Inhibition of drug resistant cancer cells
CN102441168B (en) Pharmaceutical composition containing apigenin, apigenin derivatives and Bcl-2 inhibitor and its application in preparation of medicine for treating cancer
WO2017032111A1 (en) Use of dihydroxyacetone in preparation of anti-tumour drug
CN106474097A (en) Anticarcinogen
AU2016311704B2 (en) Use of dihydroxyacetone in preparation of anti-cancer medicaments
KR102643626B1 (en) Formulations of (E)-2,4,6-trimethoxystyryl-3-[(carboxymethyl)amino]-4-methoxybenzylsulfone with improved stability and bioavailability
CN106806382B (en) anticancer composition
CN104086531B (en) A kind of Esomeprazole sodium compound and its pharmaceutical composition
WO2019201268A1 (en) Drug used for preventing and/or treating pain and/or fever, combination product, and use thereof
JP2009530284A (en) Methods and compositions for treating diastolic heart failure
CN104606189B (en) A kind of application of compound in mTOR inhibitors are prepared
HK1230099A1 (en) Anticarcinogen
HK1230099B (en) Anticarcinogen
CN104784109A (en) Temperature-sensitive controlled-release pharmaceutical composition of taxane drugs
HK1234991B (en) Anti-cancer composition
JP2010500387A5 (en)
HK1234991A1 (en) Anti-cancer composition
HK1234991A (en) Anti-cancer composition
HK1253277B (en) Use of ep4 receptor antagonists for the treatment of nash-associated liver cancer
TW200840590A (en) Compositions and methods for prevention and treatment of cachexia

Legal Events

Date Code Title Description
121 Ep: the epo has been informed by wipo that ep was designated in this application

Ref document number: 16838371

Country of ref document: EP

Kind code of ref document: A1

ENP Entry into the national phase

Ref document number: 2992629

Country of ref document: CA

ENP Entry into the national phase

Ref document number: 2018503509

Country of ref document: JP

Kind code of ref document: A

ENP Entry into the national phase

Ref document number: 2016311704

Country of ref document: AU

Date of ref document: 20160526

Kind code of ref document: A

ENP Entry into the national phase

Ref document number: 20187004813

Country of ref document: KR

Kind code of ref document: A

NENP Non-entry into the national phase

Ref country code: DE