CN105726567A - Oral chemotherapy tablets for treating gastric cancer - Google Patents
Oral chemotherapy tablets for treating gastric cancer Download PDFInfo
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- CN105726567A CN105726567A CN201410747818.XA CN201410747818A CN105726567A CN 105726567 A CN105726567 A CN 105726567A CN 201410747818 A CN201410747818 A CN 201410747818A CN 105726567 A CN105726567 A CN 105726567A
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- gastric cancer
- tablets
- capecitabine
- starch
- oral chemotherapy
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- 206010017758 gastric cancer Diseases 0.000 title claims abstract description 19
- 208000005718 Stomach Neoplasms Diseases 0.000 title claims abstract description 18
- 201000011549 stomach cancer Diseases 0.000 title claims abstract description 18
- 238000002512 chemotherapy Methods 0.000 title claims abstract description 14
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims abstract description 18
- GAGWJHPBXLXJQN-UORFTKCHSA-N Capecitabine Chemical compound C1=C(F)C(NC(=O)OCCCCC)=NC(=O)N1[C@H]1[C@H](O)[C@H](O)[C@@H](C)O1 GAGWJHPBXLXJQN-UORFTKCHSA-N 0.000 claims abstract description 14
- RYYCJUAHISIHTL-UHFFFAOYSA-N 5-azaorotic acid Chemical compound OC(=O)C1=NC(=O)NC(=O)N1 RYYCJUAHISIHTL-UHFFFAOYSA-N 0.000 claims abstract description 13
- GAGWJHPBXLXJQN-UHFFFAOYSA-N Capecitabine Natural products C1=C(F)C(NC(=O)OCCCCC)=NC(=O)N1C1C(O)C(O)C(C)O1 GAGWJHPBXLXJQN-UHFFFAOYSA-N 0.000 claims abstract description 13
- 229960004117 capecitabine Drugs 0.000 claims abstract description 13
- 239000003814 drug Substances 0.000 claims abstract description 13
- 229950000193 oteracil Drugs 0.000 claims abstract description 13
- 229920002472 Starch Polymers 0.000 claims abstract description 10
- 239000008107 starch Substances 0.000 claims abstract description 10
- 235000019698 starch Nutrition 0.000 claims abstract description 10
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims abstract description 9
- 229920000881 Modified starch Polymers 0.000 claims abstract description 9
- 235000019359 magnesium stearate Nutrition 0.000 claims abstract description 9
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims abstract description 9
- 239000008108 microcrystalline cellulose Substances 0.000 claims abstract description 9
- 229940016286 microcrystalline cellulose Drugs 0.000 claims abstract description 9
- 229940079593 drug Drugs 0.000 claims abstract description 3
- WSVLPVUVIUVCRA-KPKNDVKVSA-N Alpha-lactose monohydrate Chemical compound O.O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O WSVLPVUVIUVCRA-KPKNDVKVSA-N 0.000 claims description 8
- DQLATGHUWYMOKM-UHFFFAOYSA-L cisplatin Chemical compound N[Pt](N)(Cl)Cl DQLATGHUWYMOKM-UHFFFAOYSA-L 0.000 claims description 8
- 229960004316 cisplatin Drugs 0.000 claims description 8
- 239000002502 liposome Substances 0.000 claims description 8
- -1 Lipoplatin Chemical compound 0.000 claims description 2
- 230000000694 effects Effects 0.000 abstract description 8
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 abstract description 3
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 abstract 1
- 239000008101 lactose Substances 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 description 8
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- 208000024891 symptom Diseases 0.000 description 6
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- 230000002496 gastric effect Effects 0.000 description 3
- 206010012735 Diarrhoea Diseases 0.000 description 2
- 206010053155 Epigastric discomfort Diseases 0.000 description 2
- 206010061968 Gastric neoplasm Diseases 0.000 description 2
- 206010047700 Vomiting Diseases 0.000 description 2
- 230000036528 appetite Effects 0.000 description 2
- 235000019789 appetite Nutrition 0.000 description 2
- 201000011510 cancer Diseases 0.000 description 2
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- 239000000232 Lipid Bilayer Substances 0.000 description 1
- 208000002720 Malnutrition Diseases 0.000 description 1
- 206010029803 Nosocomial infection Diseases 0.000 description 1
- 208000008469 Peptic Ulcer Diseases 0.000 description 1
- 206010052428 Wound Diseases 0.000 description 1
- 206010000059 abdominal discomfort Diseases 0.000 description 1
- 239000002671 adjuvant Substances 0.000 description 1
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- 150000001450 anions Chemical class 0.000 description 1
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- 239000011230 binding agent Substances 0.000 description 1
- 238000001574 biopsy Methods 0.000 description 1
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- 210000000170 cell membrane Anatomy 0.000 description 1
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- 230000036737 immune function Effects 0.000 description 1
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- 238000000034 method Methods 0.000 description 1
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- 230000000291 postprandial effect Effects 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
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- 229940053867 xeloda Drugs 0.000 description 1
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- Medicinal Preparation (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
The invention belongs to the technical field of medicines, and in particular relates to oral chemotherapy tablets for treating gastric cancer. The oral chemotherapy tablets are prepared from the following components by weight: 55-79 mg of capecitabine, 15.8-19.5 mg of Lipoplatin, 16.2-22.4 mg of potassium oxonate, 3.4-5.2 mg of water-containing lactose, 2.5-3.6 mg of magnesium stearate, 2.8-4.2 mg of microcrystalline cellulose, 3.7-4.6 mg of pregelatinized starch, the balance of starch, and the total weight of the components is 150 mg, wherein capecitabine, Lipoplatin and potassium oxonate are medicinal components. The oral chemotherapy tablets have the characteristics of being convenient to use, short in course of treatment, obvious in curative effects, and small in side effects.
Description
Technical field
The invention belongs to technical field of pharmaceuticals, particularly to a kind of oral chemotherapy tablet treating gastric cancer.
Background technology
Gastric cancer ranks first in the various malignant tumor of China.Early gastric cancer majority patient's non-evident sympton, a few peoples have Nausea and vomiting or the digestive symptoms of similar Peptic Ulcers.Pain is with to lose weight be the modal clinical symptoms of advanced gastric carcinoma.The digestive symptoms that patient Chang You is comparatively clear and definite, as epigastric discomfort, feed after glutted, along with sb.'s illness took a turn for the worse progress increase the weight of for Upper abdominal pain, appetite decline, weak.The symptoms such as late gastric cancer patient often may occur in which anemia, becomes thin, malnutrition even cachexia.
For the treatment of gastric cancer, main employing is performed the operation or chemotherapeutic treatment.But all defective property of method of operation and chemotherapeutic treatment, operative treatment is the means of local treatment, like water off a duck's back for the tumor cell transferred in blood or its hetero-organization；Chemotherapy can effectively hinder cancerous cell, but can kill normal cell again simultaneously and cause that the immunologic function of patient is suppressed, and more complication occurs, brings very big damage to patient body.The appearance of new oral chemotherapeutics, because its curative effect is more excellent, side effect less brings new hope to cancer patient.Its toxic and side effects is relatively small, can substantially alleviate the untoward reaction such as stomatitis, nausea and vomiting, diarrhoea, leukopenia, Neutropenia.Additionally, the patient of oral chemotherapeutics does not need Vein Tube, so open wound can be reduced cause the danger infected, eliminate the complication that venous cannulation causes, reduce and be hospitalized for observation the time, it is to avoid doctor's cross infection in hospital, this is extremely important for the late gastric cancer patient that immunity is relatively low.And oral chemotherapeutics is not only patient and saves the number of times of hospital admission, connects the subject time, also reduce and treat the misery that relevant untoward reaction brings, making patients with gastric cancer have the more time together with family and friends, improving the quality of living.
Xeloda (capecitabine sheet) is oral chemotherapeutics main on market, but because it has cardiac toxicity, easily causes the limitation such as dehydration, hinders it to promote the use of further.
Summary of the invention
It is an object of the invention to provide a kind of oral chemotherapy tablet treating gastric cancer, there is easy to use, short treating period and feature evident in efficacy, that side effect is little.
The present invention provides a kind of oral chemotherapy tablet treating gastric cancer, composed of the following components: capecitabine 55～79mg, cisplatin liposome 15.8～19.5mg, oteracil potassium 16.2～22.4mg, lactose hydrous 3.4～5.2mg, magnesium stearate 2.5～3.6mg, microcrystalline Cellulose 2.8～4.2mg, pregelatinized Starch 3.7～4.6mg, surplus is starch, total amount amounts to 150mg, wherein, capecitabine, Lipoplatin, oteracil potassium are drug component.
More preferably composed of the following components: capecitabine 58.6mg, cisplatin liposome 17.9mg, oteracil potassium 20.4mg, lactose hydrous 4.6mg, magnesium stearate 2.8mg, microcrystalline Cellulose 3.3mg, pregelatinized Starch 4.2mg, starch 38.2mg.
Preparation method is medicine with adjuvant to be mixed and is pressed into lamellar, every 150mg.
In the present invention, capecitabine can be transformed into 5-FU in vivo, has targeting, it is possible to makes 5-FU be gathered in tumor stomach cell more, less acts on other healthy cells；Cisplatin liposome has targeting equally, and its anion lipid bilayer can promote that cell membrane crossed over by medicine, is beneficial to medicine of the present invention and reaches the effect of better killing off tumor cells；Oteracil potassium can block the phosphorylation of 5-Fu, and after oral administration, oteracil potassium has significantly high distributed density in gastrointestinal tissue, is distributed at gastrointestinal thus affecting 5-Fu, and then reduces the effect of 5-Fu toxicity.Lactose hydrous no hygroscopicity, compressibility is good, stable in properties, and with medicine not chemically reactive, the tablet being pressed into is bright and clean attractive in appearance, for filling the weight of tablet, it is simple to tabletting；Magnesium stearate is used as powder mould agent and lubricant, improves mobility and the compressibility of tablet；Microcrystalline cellulose have stronger adhesion, improves hardness and the disintegrating property of tablet；Binding agent, diluent and disintegrating agent are done in pregelatinized Starch, make starch have mobility and direct compressibility；Starch is as diluent and disintegrating agent, and character is highly stable, inoperative with medicine, and price is also relatively cheap, and the tablet hygroscopicity made is little, appearance luster good.
Take medicine of the present invention, one time 1, every day twice, point sooner or later two swallow inferior to use half an hour water after meal, be used in conjunction two weeks, have a rest one week, within three weeks, be a course for the treatment of.Should stopping treatment when continuing deterioration or generation not tolerant toxicity such as the state of an illness, gestation and women breast-feeding their children are cautious use of.
Outcome measure:
Effective: body constitution strengthens, limbs are strong, and abdominal discomfort disappears, and tumor stomach tumor body reduces, and other position has no nascent tumor；
Effective: body constitution strengthens, and tumor stomach has no increase, and other position has no nascent tumor；
Invalid: symptom is unchanged, tumor stomach tumor body increases, or nascent tumor occurs in other position.
Therapeutic outcome: treat 175 patients with gastric cancer, use 2 the course for the treatment of present invention medicine after, effective 159 examples, account for 90.9%, effective 15 examples, account for 8.6%, invalid 1 example, account for 0.5%.
Attached a few example case is described further:
nullCase 1: Luo，Female，76 years old，Patient started epigastric discomfort sense occur without obvious inducement before 1 year，With post-prandial fullness、Dull pain is main，Do not give from the beginning of mild degree and paying special attention to，Abdeminal pain sense and dull pain aggravation was started before half a year，Affect work and sleep，Obvious after the meal，Affect appetite，Body weight slightly declines，Give gastric acid inhibitory、After the protection treatment such as gastric mucosa and pain relieving, symptom is alleviated to some extent，But body weight is gradually reduced，Started before 1 month that row black stool occurs，Start not give attention，Rear progress is row's pitch sample loose stool，Household finds before its complexion is relatively greenish yellow simultaneously，Patient oneself also feels tired、Weak，Absent minded，Sometimes with dark and dim eyesight，Check that diagnosis is for gastric cancer to my institute，Then give medicine of the present invention to treat，Use after 2 courses for the treatment of effectively，After 3 courses for the treatment of effective，Follow up a case by regular visits to 1 year without recurrence.
Case 2: grandson, man, 72 years old, because epigastrium pain is obvious, loss of appetite, health is substantially become thin, and body weight becomes thin about 15 jin, epigastrium has obvious lump, general 3 cm, and stool blackout is to our hospital, making epigastrium CT scan after being admitted to hospital, show that greater gastric curvature side protuberance type swells thing, profile is irregular, invading paries posterior gastricus, gastroscopic biopsy shows low differentiated squamous-cell carcinomas, then gives medicine of the present invention, after 2 courses for the treatment of effective, after half a year lump disappear, follow up a case by regular visits to half a year without recurrence.
Detailed description of the invention
Embodiment described below, is only the preferred embodiments of the invention, when not limiting the scope of the present invention, namely all done impartial change according to the application scope and modifies, all should still belong in covering scope of the present invention.
Embodiment 1:
A kind of oral chemotherapy tablet treating gastric cancer, composed of the following components: capecitabine 58.6mg, cisplatin liposome 17.9mg, oteracil potassium 20.4mg, lactose hydrous 4.6mg, magnesium stearate 2.8mg, microcrystalline Cellulose 3.3mg, pregelatinized Starch 4.2mg, starch 38.2mg.
Embodiment 2:
A kind of oral chemotherapy tablet treating gastric cancer, composed of the following components: capecitabine 55mg, cisplatin liposome 19.5mg, oteracil potassium 16.2mg, lactose hydrous 35.2mg, magnesium stearate 2.5mg, microcrystalline Cellulose 4.2mg, pregelatinized Starch 3.7mg, starch 13.7mg.
Embodiment 3:
A kind of oral chemotherapy tablet treating gastric cancer, composed of the following components: capecitabine 79mg, cisplatin liposome 15.8mg, oteracil potassium 22.4mg, lactose hydrous 3.4mg, magnesium stearate 3.6mg, microcrystalline Cellulose 2.8mg, pregelatinized Starch 4.6mg, starch 18.4mg.
Claims (2)
1. the oral chemotherapy tablet treating gastric cancer, it is characterized in that composed of the following components: capecitabine 55～79mg, cisplatin liposome 15.8～19.5mg, oteracil potassium 16.2～22.4mg, lactose hydrous 3.4～5.2mg, magnesium stearate 2.5～3.6mg, microcrystalline Cellulose 2.8～4.2mg, pregelatinized Starch 3.7～4.6mg, surplus is starch, total amount amounts to 150mg, wherein, capecitabine, Lipoplatin, oteracil potassium are drug component.
2. a kind of oral chemotherapy tablet treating gastric cancer as claimed in claim 1, it is characterized in that composed of the following components: capecitabine 58.6mg, cisplatin liposome 17.9mg, oteracil potassium 20.4mg, lactose hydrous 4.6mg, magnesium stearate 2.8mg, microcrystalline Cellulose 3.3mg, pregelatinized Starch 4.2mg, starch 38.2mg.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410747818.XA CN105726567A (en) | 2014-12-09 | 2014-12-09 | Oral chemotherapy tablets for treating gastric cancer |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410747818.XA CN105726567A (en) | 2014-12-09 | 2014-12-09 | Oral chemotherapy tablets for treating gastric cancer |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN105726567A true CN105726567A (en) | 2016-07-06 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201410747818.XA Pending CN105726567A (en) | 2014-12-09 | 2014-12-09 | Oral chemotherapy tablets for treating gastric cancer |
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| Country | Link |
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| CN (1) | CN105726567A (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106619689A (en) * | 2016-12-30 | 2017-05-10 | 陈晓华 | Medicine composition and kit for therapy of cancer and application thereof |
-
2014
- 2014-12-09 CN CN201410747818.XA patent/CN105726567A/en active Pending
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106619689A (en) * | 2016-12-30 | 2017-05-10 | 陈晓华 | Medicine composition and kit for therapy of cancer and application thereof |
| CN106619689B (en) * | 2016-12-30 | 2018-05-01 | 陈晓华 | It is a kind of for the pharmaceutical composition for the treatment of cancer, kit and its application |
| WO2018121669A1 (en) * | 2016-12-30 | 2018-07-05 | 陈晓华 | Pharmaceutical composition for treating cancer and use thereof |
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| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20160706 |
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| WD01 | Invention patent application deemed withdrawn after publication |