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WO2021179319A1 - Composition contenant du sulfate de chondroïtine hydrolysé pour la prévention et le traitement de l'ostéoarthropathie - Google Patents

Composition contenant du sulfate de chondroïtine hydrolysé pour la prévention et le traitement de l'ostéoarthropathie Download PDF

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Publication number
WO2021179319A1
WO2021179319A1 PCT/CN2020/079335 CN2020079335W WO2021179319A1 WO 2021179319 A1 WO2021179319 A1 WO 2021179319A1 CN 2020079335 W CN2020079335 W CN 2020079335W WO 2021179319 A1 WO2021179319 A1 WO 2021179319A1
Authority
WO
WIPO (PCT)
Prior art keywords
chondroitin sulfate
composition
composition containing
hydrolyzed chondroitin
containing hydrolyzed
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/CN2020/079335
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English (en)
Chinese (zh)
Inventor
宋季磊
伍平华
金波
张昊宁
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.)
Nanjing Hanxin Pharmaceutical Technology Co Ltd
Original Assignee
Nanjing Hanxin Pharmaceutical Technology Co Ltd
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
Application filed by Nanjing Hanxin Pharmaceutical Technology Co Ltd filed Critical Nanjing Hanxin Pharmaceutical Technology Co Ltd
Priority to PCT/CN2020/079335 priority Critical patent/WO2021179319A1/fr
Priority to KR1020227018141A priority patent/KR20220091552A/ko
Priority to PCT/CN2020/126003 priority patent/WO2021083384A1/fr
Priority to JP2022525450A priority patent/JP2023500294A/ja
Priority to CA3159355A priority patent/CA3159355A1/fr
Priority to EP20882136.3A priority patent/EP4053290A4/fr
Priority to BR112022008397A priority patent/BR112022008397A8/pt
Priority to AU2020374934A priority patent/AU2020374934B2/en
Priority to CN202080076790.5A priority patent/CN114846147B/zh
Priority to US17/335,837 priority patent/US11572421B2/en
Publication of WO2021179319A1 publication Critical patent/WO2021179319A1/fr
Anticipated expiration legal-status Critical
Priority to US18/092,051 priority patent/US20230250199A1/en
Ceased legal-status Critical Current

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/715—Polysaccharides, i.e. having more than five saccharide radicals attached to each other by glycosidic linkages; Derivatives thereof, e.g. ethers, esters
    • A61K31/737—Sulfated polysaccharides, e.g. chondroitin sulfate, dermatan sulfate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]

Definitions

  • the invention belongs to the field of health food, and particularly relates to a hydrolyzed chondroitin sulfate composition.
  • Chondroitin sulfate is a mucopolysaccharide substance extracted from cartilage tissues such as animal larynx and trachea. Its basic units are D-glucuronic acid and N-acetyl-D-galactosamine sulfate. Chondroitin sulfate is a macromolecular substance with diverse biological activities. With its unique pharmacological activity, it has a wide range of applications in the fields of medicine and health products. It can not only treat bone and joint diseases, lower blood lipids, but also can be used as a nutritional health product to improve Body immunity. At present, the molecular weight of chondroitin sulfate on the market is generally 10kDa-50kDa.
  • chondroitin sulfate has a relatively large molecular weight and is difficult to penetrate biological cell membranes. Therefore, it cannot perform its various pharmacological functions well in the body.
  • human biological utilization The degree is about 10% to 15%, which seriously affects the curative effect.
  • digestion through the digestive juice of the gastrointestinal tract will cause obvious irritation to the upper digestive tract.
  • Stomach pain, stomach acid, bloating, and even Symptoms such as nausea and vomiting.
  • a large number of studies have shown that low molecular weight chondroitin sulfate has the advantages of low viscosity and good solubility, has higher bioavailability, and better promotes cartilage repair and other effects. Therefore, the preparation of hydrolyzed chondroitin sulfate by enzymatic hydrolysis of chondroitin sulfate is used to prepare health foods that increase bone density, improve osteoporosis, and relieve arthritis. The irritation is less.
  • the problem to be solved by the present invention is to provide a hydrolyzed chondroitin sulfate composition for increasing bone density and alleviating arthritis.
  • the daily human dosage of the hydrolyzed chondroitin sulfate and glucosamine composition is lower than that of currently known commercially available sulfuric acid.
  • the daily human dosage of chondroitin and glucosamine composition For example, the daily human dosage of chondroitin sulfate and glucosamine in Movefree is 1700mg/day; the daily human dosage of chondroitin sulfate and glucosamine in By-Health is 1160mg/day. sky.
  • a hydrolyzed chondroitin sulfate composition of the present invention adopts the following technical solutions:
  • composition containing hydrolyzed chondroitin sulfate of the present invention is characterized in that it contains a daily dosage of 50 mg to 800 mg of hydrolyzed chondroitin sulfate.
  • composition containing hydrolyzed chondroitin sulfate of the present invention is characterized in that the composition may contain glucosamine.
  • composition containing hydrolyzed chondroitin sulfate according to the present invention is characterized in that the glucosamine can be one or a mixture of glucosamine hydrochloride and glucosamine sulfate.
  • composition containing hydrolyzed chondroitin sulfate of the present invention is characterized in that the hydrolyzed chondroitin sulfate is a mixture of hydrolyzed chondroitin sulfate with different molecular weights.
  • the hydrolyzed chondroitin sulfate composition of the present invention is a mixture obtained by enzymatic hydrolysis, purification, concentration, and spray drying of chondroitin sulfate, and its molecular weight is 379-10000 Da.
  • composition containing hydrolyzed chondroitin sulfate of the present invention further includes pharmaceutically acceptable excipients, wherein the excipients are selected from fillers, disintegrants, adhesives, correctives, and lubricants.
  • excipients are selected from fillers, disintegrants, adhesives, correctives, and lubricants.
  • film coating agent is selected from fillers, disintegrants, adhesives, correctives, and lubricants.
  • the hydrolyzed chondroitin sulfate composition of the present invention and the preparation method thereof are characterized in that the filler in the preparation includes, but is not limited to, microcrystalline cellulose, starch, dextrin, mannitol, lactose, etc.; disintegration Agents include, but are not limited to, crospovidone, croscarmellose sodium, sodium carboxymethyl starch, hydroxypropyl starch, pre-crossed starch, low-substituted hydroxypropyl cellulose, sodium bicarbonate, citrate Acid, tartaric acid, etc.; binders include but are not limited to sodium carboxymethyl cellulose, hydroxypropyl cellulose, methyl cellulose, ethyl cellulose, hydroxypropyl methyl cellulose, polyvinylpyrrolidone, etc.; lubricants include But not limited to magnesium stearate, micronized silica gel, talc, hydrogenated vegetable oil, polyethylene glycol, stearic acid
  • the hydrolyzed chondroitin sulfate composition and the preparation method thereof of the present invention are characterized in that the preparation includes, but is not limited to, tablets, granules, capsules, and pills.
  • composition of the present invention can be used to prepare medicines for reducing arthritis and alleviating pain.
  • the hydrolyzed chondroitin sulfate prepared by enzymatically hydrolyzing chondroitin sulfate of the present invention can be used to prepare health care products that increase bone density, improve osteoporosis, and relieve arthritis. Less irritating.
  • the daily human dosage of the components of the hydrolyzed chondroitin sulfate and glucosamine contained in the composition of the present invention is lower than the currently known human daily dosage of commercially available chondroitin sulfate and glucosamine. By reducing the dosage to improve the compliance of taking, but does not reduce the effect of increasing bone density and relieving arthritis.
  • the test of the difference in support force of mice is used to evaluate the pain degree of mouse arthritis and the daily dosage of human body.
  • Figure 1 A diagram of the effect of the composition on the body weight of mice.
  • Figure 2 A diagram of the influence of the composition on the supporting force of mice.
  • Example 1 Hydrolyzed chondroitin sulfate capsules
  • Example 7 Mouse medial meniscus instability (DMM) model test of the composition prepared by the present invention
  • Test sample The composition is prepared according to Examples 1-6 of the present invention.
  • the recommended daily dosage for humans is 2 tablets (Capsules)/day, 1 tablet (capsule) each morning and evening.
  • test sample is mixed into the feed to give the sample, example 1, example 2, example 3, example 4, example 5 and example 6, samples taken by mice every day Requires 150mg/day.
  • test substance The route of administration of the test substance: the samples of each example were administered to each group of animals by gavage.
  • the mouse was anesthetized with chloral hydrate, the knee joint hair of the right hind limb was shaved, and after iodine alcohol disinfection, an opening about 1 cm long was cut longitudinally along the inner side of the mouse bone to expose the knee joint.
  • the 6-0 absorbable suture is used to suture the joint capsule, the 6-0 suture is used to suture the skin of the joint, and a small amount of penicillin is applied to the sutured skin to prevent infection.
  • the blank group (9 mice) did the same operation, but did not cut the tibial ligament of the medial meniscus.
  • the DMM mice were randomly divided into 7 groups (1, model control group; 2, Example 1 group; 3, Example 2 group; 4, Example 3 group; 5, Example 4 group; 6. Example 5 group; 7. Example 6 group) 13 animals in each group.
  • mice On the second day after the operation, the mice were given intragastric administration.
  • the blank group and the model group were given the same volume of normal saline. It is administered once a day for 12 consecutive weeks, and the animal weight is weighed once a week, and the dosage is adjusted according to the body weight.
  • mice After the mice were gavaged for 12 weeks, the YLS-11A channel type mouse foot support force measuring instrument was used to detect the difference in the support force of the two hind legs of each group of mice when they were standing, so as to evaluate the degree of osteoarthritis pain in the mice. .
  • the mice were driven into a single channel for a 60-degree climbing experiment. When the mouse began to climb and stand, record the difference in support between the left and right hind legs of the mouse. The greater the difference in supporting force, the more severe the degree of osteoarthritis.
  • the pain degree of osteoarthritis in mice was evaluated by detecting the difference in support force of mice. The results are shown in Figure 2.
  • the difference in foot support force of the model group is the largest, indicating that the pain degree of osteoarthritis in the model group is the most severe .
  • Example 1, Example 2, Example 5 and Example 6 can significantly reduce the difference in foot support force (P ⁇ 0.01)
  • Example 3 and Example 4 can also reduce the difference in foot support force ( P ⁇ 0.05)

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Rheumatology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Immunology (AREA)
  • Pain & Pain Management (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Dermatology (AREA)
  • Molecular Biology (AREA)
  • Epidemiology (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

L'invention concerne une composition contenant du sulfate de chondroïtine hydrolysé pour la prévention et le traitement de l'ostéoarthropathie et son procédé de préparation. Les composants efficaces de la composition ont une biodisponibilité élevée, des dosages faibles, et peuvent être utilisés pour restaurer la fonction osseuse.
PCT/CN2020/079335 2019-11-01 2020-03-13 Composition contenant du sulfate de chondroïtine hydrolysé pour la prévention et le traitement de l'ostéoarthropathie Ceased WO2021179319A1 (fr)

Priority Applications (11)

Application Number Priority Date Filing Date Title
PCT/CN2020/079335 WO2021179319A1 (fr) 2020-03-13 2020-03-13 Composition contenant du sulfate de chondroïtine hydrolysé pour la prévention et le traitement de l'ostéoarthropathie
EP20882136.3A EP4053290A4 (fr) 2019-11-01 2020-11-02 Sulfate de chondroïtine de faible poids moléculaire, composition le contenant, son procédé de préparation et son utilisation
PCT/CN2020/126003 WO2021083384A1 (fr) 2019-11-01 2020-11-02 Sulfate de chondroïtine de faible poids moléculaire, composition le contenant, son procédé de préparation et son utilisation
JP2022525450A JP2023500294A (ja) 2019-11-01 2020-11-02 低分子量コンドロイチン硫酸、組成物、製造方法及びそれらの使用
CA3159355A CA3159355A1 (fr) 2019-11-01 2020-11-02 Sulfate de chondroitine de faible poids moleculaire, composition le contenant, son procede de preparation et son utilisation
KR1020227018141A KR20220091552A (ko) 2019-11-01 2020-11-02 저분자량 콘드로이틴 술페이트, 이를 함유하는 조성물, 및 이의 제조 방법 및 이의 용도
BR112022008397A BR112022008397A8 (pt) 2019-11-01 2020-11-02 Sulfato de condroitina com baixo peso molecular, composição, método de preparação e uso do mesmo
AU2020374934A AU2020374934B2 (en) 2019-11-01 2020-11-02 Low molecular weight chondroitin sulfate, composition containing same, and preparation method therefor and use thereof
CN202080076790.5A CN114846147B (zh) 2019-11-01 2020-11-02 低分子量硫酸软骨素、包含其的组合物、其制备方法以及其用途
US17/335,837 US11572421B2 (en) 2019-11-01 2021-06-01 Low molecular weight chondroitin sulfate, composition, preparation method and use thereof
US18/092,051 US20230250199A1 (en) 2019-11-01 2022-12-30 Low molecular weight chondroitin sulfate, composition, preparation method and use thereof

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
PCT/CN2020/079335 WO2021179319A1 (fr) 2020-03-13 2020-03-13 Composition contenant du sulfate de chondroïtine hydrolysé pour la prévention et le traitement de l'ostéoarthropathie

Publications (1)

Publication Number Publication Date
WO2021179319A1 true WO2021179319A1 (fr) 2021-09-16

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PCT/CN2020/079335 Ceased WO2021179319A1 (fr) 2019-11-01 2020-03-13 Composition contenant du sulfate de chondroïtine hydrolysé pour la prévention et le traitement de l'ostéoarthropathie

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Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3405120A (en) * 1966-01-27 1968-10-08 Green Cross Corp Low molecular chondroitin sulfate and method for manufacturing the same
CN1513471A (zh) * 2003-05-07 2004-07-21 毅 汤 低分子量硫酸软骨素注射剂及其制备方法
CN101057862A (zh) * 2007-05-24 2007-10-24 张义兴 一种防治老年性骨关节病的药物组合物
CN101658482A (zh) * 2008-08-26 2010-03-03 徐峥嵘 低分子硫酸软骨素口服制剂及其制法和用途
CN102228466A (zh) * 2011-03-25 2011-11-02 上海优能慧斯生物科技有限公司 硫酸软骨素氨糖片
CN104411363A (zh) * 2012-05-22 2015-03-11 诺西斯有限公司 用于预防骨关节炎的低分子量生物技术6-硫酸软骨素

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3405120A (en) * 1966-01-27 1968-10-08 Green Cross Corp Low molecular chondroitin sulfate and method for manufacturing the same
CN1513471A (zh) * 2003-05-07 2004-07-21 毅 汤 低分子量硫酸软骨素注射剂及其制备方法
CN101057862A (zh) * 2007-05-24 2007-10-24 张义兴 一种防治老年性骨关节病的药物组合物
CN101658482A (zh) * 2008-08-26 2010-03-03 徐峥嵘 低分子硫酸软骨素口服制剂及其制法和用途
CN102228466A (zh) * 2011-03-25 2011-11-02 上海优能慧斯生物科技有限公司 硫酸软骨素氨糖片
CN104411363A (zh) * 2012-05-22 2015-03-11 诺西斯有限公司 用于预防骨关节炎的低分子量生物技术6-硫酸软骨素

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