CN105796588A - Medicine composition containing glucosamine and used for articular cavity injection - Google Patents
Medicine composition containing glucosamine and used for articular cavity injection Download PDFInfo
- Publication number
- CN105796588A CN105796588A CN201610208328.1A CN201610208328A CN105796588A CN 105796588 A CN105796588 A CN 105796588A CN 201610208328 A CN201610208328 A CN 201610208328A CN 105796588 A CN105796588 A CN 105796588A
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- Prior art keywords
- glucosamine
- articular cavity
- concentration
- glucosamine hydrochloride
- injections
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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
- A61K31/726—Glycosaminoglycans, i.e. mucopolysaccharides
- A61K31/728—Hyaluronic acid
-
- 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
- A61K31/7008—Compounds having an amino group directly attached to a carbon atom of the saccharide radical, e.g. D-galactosamine, ranimustine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/02—Inorganic compounds
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
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- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Molecular Biology (AREA)
- Dermatology (AREA)
- Inorganic Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The invention discloses medicine composition containing glucosamine and used for articular cavity injection. The medicine composition contains glucosamine hydrochloride and sodium hyaluronate, wherein the concentration of glucosamine hydrochloride ranges from 5% to 20%, the molecular weight of sodium hyaluronate is 800,000-2000,000 Dalton and the concentration of sodium hyaluronate is 0.5%-1.5%. The medicine composition has the advantages that micromolecular glucosamine is rapidly absorbed and has a rapid repairing function, also has the advantages of good viscoelasticity and buffering property relative to high-molecular-weight sodium hyaluronate and capability of promoting slow release of glucosamine and can be used for treating arthritis through articular cavity injection.
Description
Technical field
The invention belongs to pharmaceutical technology field, be specifically related to a kind of injections in articular cavity medicine containing glucosamine
Compositions.
Background technology
Osteoarthritis (Osteoarthritis, OA), also known as osteoarthritis, is that a class is caused by multifactor,
The joint disease of basic pathological changes is become with articular cartilage degeneration, common with middle-older patient.In the crowd of more than 60 years old
Prevalence is up to 50%, and the crowd of 75 years old then reaches 80%.The disability rate of this disease may be up to 53%.
Along with population in the world aging, the sickness rate cumulative year after year of osteoarthritis.China be osteoarthritis " super greatly
State ".Now there are about 1.3 hundred million people and undergo the torment of osteoarthritis.Osteoarthritis is except affecting motor capacity and life matter
Amount, and then produce beyond depression and anxiety, also can produce huge financial burden.In the U.S., the medical treatment about OA in 2008
Expense adds up to and has exceeded 185,000,000,000 yuan.Arthritis brings the biggest economy and stress to patient and family, it has also become
Serious public health problem.
At present, we also cannot accomplish osteoarthritis is carried out early diagnosis, and late period, osteoarthritis was except taking
Beyond analgesic drug product or joint replacement, also can not find other more preferable Therapeutic Method.Therefore, osteoarthritis is except prevention ahead of time
Outward, also to give effectively to treat in phase morning, noon and afternoon or acute stage that find osteoarthritis, it is desirable to be possible not only to alleviate joint
Pain, delays PD and can repair cartilage, radical curing of disease.Therefore, this new drug is researched and developed very urgent.
Glucosamine (C6H13NO5), also known as glucamine, is a kind of natural amino monosaccharide, and it is synthesis cartilage base
The main component of poly-glucosamine in matter and synovial fluid.Human body can pass through amination glucose synthesizing amino glucose, have with
The diverse physiological function of glucose.D-glucosamine content will gradually decrease in human body the most with advancing age after 30 years old, 70 years old
The most internal almost no longer synthesize.Research finds that ectogenic glucosamine can stimulate chondrocyte synthetic proteins polysaccharide, mends
Fill the missing element of cartilage matrix, improve the water such as the repair ability of chondrocyte, suppression lysosomal enzyme, collagenase and phospholipase A2
Solve the release of enzyme, reduce the hydrolysis to articular cartilage matrix and destroy, and the generation of the super oxyradical of damaging cells can be prevented,
Promoting the repair and reconstruction of cartilage matrix, alleviate arthralgia, improve function of joint, being considered in treatment osteoarthritis is peace
Complete effective cartilage protection.D-glucosamine product is based on oral formulations the most on the market, although according to clinical verification at a part of bone
In arthritic effective in cure, but its onset is slow, bioavailability is relatively low, only treats Osteoarthritis in early days,
Centering patients with terminal action effect is inconspicuous, and part population is administered orally this medicine and has nauseating, constipation, abdominal distention and diarrheal disease
Shape；Long-term taking is to Liver and kidney toxic side effect etc..Therefore, develop new D-glucosamine product and become a weight for the treatment of osteoarthritis
Want direction.
Hyaluronic acid sodium is to be repeated, by β-n acetylglucosamine n and D-glucuronic acid monosaccharide, the chain polymer that is formed by connecting, is
Ingredient important in knuckle synovia, has the mechanical protection effect such as damping, lubrication to articular cartilage, maintains the normal merit of synovial fluid
Can be extremely important.In the knuckle synovia of arthritic, the molecular weight of hyaluronic acid sodium, concentration and viscoelasticity are equal
Substantially reduce, by directly giving the hyaluronic acid sodium of high molecular in articular cavity, natural cover can be re-formed, prevent cartilage
Substrate destroys disappearance further；Improve the biological function of pathological state inferior synovial membrane, joint friction and pain are mitigated or eliminated, but
Repairing speed relatively slow, the course for the treatment of is longer.
Summary of the invention
It is an object of the invention to provide and a kind of absorbed quickly, repair quickly containing note in the articular cavity of glucosamine
Penetrate pharmaceutical composition.
For achieving the above object, the solution of the present invention is:
A kind of medicinal composition for injections in articular cavity containing glucosamine hydrochloride, wherein this pharmaceutical composition contains hydrochloric acid
Glucosamine and hyaluronic acid sodium, wherein glucosamine hydrochloride concentration 5%-20%, hyaluronic acid sodium molecular weight is 80-200 ten thousand road
Er Dun, concentration is 0.5%-1.5%.
Concentration 8%-15% of described glucosamine.
The concentration 10% of described glucosamine.
Concentration 0.8%-1.2% of described hyaluronic acid sodium.
The concentration 1% of described hyaluronic acid sodium.
Described compositions is liquid preparation or gel.
The PH scope of described compositions is 5.5-7.4.
After using such scheme, according to pathogenesis and the clinical manifestation of osteoarthritis, and the numerous studies of the present invention
Finding, hyaluronic acid sodium and the effect of drug treatment in glucosamine use in conjunction articular cavity are than independent joint cavity injection Hyaluronic Acid
Sodium or glucosamine are better.Because on the one hand the hyaluronic acid sodium of macromolecule has the machine such as damping, lubrication to articular cartilage
Tool protective effect, prevents impaired cartilage from continuing to increase the weight of, and on the one hand as slow releasing preparation, discharges glucosamine for a long time,
And glucosamine is as one of composition synthesizing cartilage, the structure of cartilage be can directly participate in, regeneration and the reparation of cartilage accelerated,
Owing to molecular weight is relatively small, can rapid osmotic in cartilage, the damaging cartilage not having blood supply is had well by this
Repair.The two synergism, the most atraumatic cartilage continues to deteriorate, the most long-term, accelerates to repair cartilage.
Detailed description of the invention
Present invention is disclosed a kind of medicinal composition for injections in articular cavity containing glucosamine hydrochloride, wherein this medicine
Compositions contains glucosamine hydrochloride and hyaluronic acid sodium, wherein glucosamine hydrochloride concentration 5%-20%, and hyaluronic acid sodium divides
Son amount is 80-200 ten thousand dalton, and concentration is 0.5%-1.5%.Described compositions is liquid preparation or gel.Described compositions
PH scope be 5.5-7.4.
Embodiment 1
Prescription:
Embodiment 2
Prescription:
Embodiment 3
Prescription:
Test data:
The embodiment of the present invention 1 effectiveness study to osteoarthritis
The preparation of 1 laboratory sample
1. test group: the embodiment of the present invention 1.
2. compareing 1 group: take glucosamine hydrochloride 10g, be added without hyaluronic acid sodium, remaining is with the embodiment of the present invention 1.
3. 2 groups are compareed: take hyaluronic acid sodium 1g(relatively high molecular weight 1,800,000 dalton), it is added without aminoguanidine hydrochloride Fructus Vitis viniferae
Sugar, remaining is with the embodiment of the present invention 1
4. negative control group: normal saline
2 laboratory animal packets
Taking healthy new zealand white rabbit 40, body weight 2-2.5KG, male and female do not limit, and are randomly divided into 4 groups: 1. 2. test group compares 1 group
3. compare 2 groups and 4. compare 3 groups of 5. negative control group.
The preparation of osteoarthritis and administration
Cause osteoarthritis varying model by injecting papain in articular cavity, be injected separately in 5 groups of right knee joint cavities of rabbit
Papain solution 0.3 ml.After 3 days, then inject the 2nd time, within the 7th day, inject the 3rd time, injection 3 times altogether.After modeling
14 days, 5 groups of experimental rabbits are injected above-mentioned sample 0.3ml, 1 times a week, totally 5 weeks in the same area of articular cavity respectively.
The collection of sample and detection
After final injection the 7th day, puts to death rabbit.Hair around scraping rabbit knee, opens articular cavity row gross examination of skeletal muscle, then
Complete taking-up cartilage and joint fluid, articular cartilage tissue is fixed, and is dehydrated routinely, paraffin embedding, is then cut into cutting of 5-6nm
Sheet, is HE respectively, and Ali Xinlan dyes, section om observation.
Result
According to Mankin osteoarthritis histologic classification method, cartilage is marked, the results are shown in Table 1
Each test results is carried out statistical analysis show: each administration group all has pole significant difference with negative control group, its
The integration of middle test group is substantially less than a matched group, illustrates that the therapeutic effect of the embodiment of the present invention 1 is optimal.
Claims (7)
1. the medicinal composition for injections in articular cavity containing glucosamine hydrochloride, it is characterised in that: this drug regimen
Thing contains glucosamine hydrochloride and hyaluronic acid sodium, wherein glucosamine hydrochloride concentration 5%-20%, and hyaluronic acid sodium molecular weight is
80-200 ten thousand dalton, concentration is 0.5%-1.5%.
A kind of medicinal composition for injections in articular cavity containing glucosamine hydrochloride, it is special
Levy and be: concentration 8%-15% of described glucosamine.
A kind of medicinal composition for injections in articular cavity containing glucosamine hydrochloride, it is special
Levy and be: the concentration 10% of described glucosamine.
A kind of medicinal composition for injections in articular cavity containing glucosamine hydrochloride, it is special
Levy and be: concentration 0.8%-1.2% of described hyaluronic acid sodium.
A kind of medicinal composition for injections in articular cavity containing glucosamine hydrochloride, it is special
Levy and be: the concentration 1% of described hyaluronic acid sodium.
6. a kind of injections in articular cavity drug regimen containing glucosamine hydrochloride of any one as described in claim 1-5
Thing, it is characterised in that: described compositions is liquid preparation or gel.
A kind of medicinal composition for injections in articular cavity containing glucosamine hydrochloride, it is special
Levy and be: the PH scope of described compositions is 5.5-7.4.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610208328.1A CN105796588B (en) | 2016-04-06 | 2016-04-06 | A kind of medicinal composition for injections in articular cavity containing Glucosamine |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610208328.1A CN105796588B (en) | 2016-04-06 | 2016-04-06 | A kind of medicinal composition for injections in articular cavity containing Glucosamine |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN105796588A true CN105796588A (en) | 2016-07-27 |
| CN105796588B CN105796588B (en) | 2018-10-23 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201610208328.1A Active CN105796588B (en) | 2016-04-06 | 2016-04-06 | A kind of medicinal composition for injections in articular cavity containing Glucosamine |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110193006A (en) * | 2019-05-22 | 2019-09-03 | 四川农业大学 | Aminoglucose hydrochloride Bones and joints intelligent aqueous gel and its preparation method and application |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1714799A (en) * | 2004-06-30 | 2006-01-04 | 上海科宝生物技术有限公司 | Medicinal composition and its use in treating osteoarthritis |
| CN101112378A (en) * | 2006-07-24 | 2008-01-30 | 凌沛学 | Articular cavity inner injecting and administering reparations containing trehalose |
| US20080139500A1 (en) * | 2006-12-11 | 2008-06-12 | Isadore Elliott Goldberg | Use of composite monomer or monomers, catalyst, sodium hyaluronate or hyaluronic acid, glucosamide sulfate, chondroiten sulfate or chlorides, for the treatment of osteoarthritis by intraarticular application to a hip or knee joint |
| CN101810855A (en) * | 2010-05-20 | 2010-08-25 | 佟刚 | II-type collagen joint cartilage fluid and preparation method thereof |
-
2016
- 2016-04-06 CN CN201610208328.1A patent/CN105796588B/en active Active
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1714799A (en) * | 2004-06-30 | 2006-01-04 | 上海科宝生物技术有限公司 | Medicinal composition and its use in treating osteoarthritis |
| CN101112378A (en) * | 2006-07-24 | 2008-01-30 | 凌沛学 | Articular cavity inner injecting and administering reparations containing trehalose |
| US20080139500A1 (en) * | 2006-12-11 | 2008-06-12 | Isadore Elliott Goldberg | Use of composite monomer or monomers, catalyst, sodium hyaluronate or hyaluronic acid, glucosamide sulfate, chondroiten sulfate or chlorides, for the treatment of osteoarthritis by intraarticular application to a hip or knee joint |
| CN101810855A (en) * | 2010-05-20 | 2010-08-25 | 佟刚 | II-type collagen joint cartilage fluid and preparation method thereof |
Non-Patent Citations (1)
| Title |
|---|
| 陈永龙等: ""盐酸氨基葡萄糖协同关节腔内注射玻璃酸钠治疗膝关节骨关节炎疗效观察"", 《中国骨肿瘤病》 * |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110193006A (en) * | 2019-05-22 | 2019-09-03 | 四川农业大学 | Aminoglucose hydrochloride Bones and joints intelligent aqueous gel and its preparation method and application |
| CN110193006B (en) * | 2019-05-22 | 2022-11-25 | 四川农业大学 | Glucosamine hydrochloride bone joint intelligent hydrogel and preparation method and application thereof |
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| Publication number | Publication date |
|---|---|
| CN105796588B (en) | 2018-10-23 |
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