CN101491526A - Use of tetrahydropyridines in preparing medicine for treating arthritis - Google Patents
Use of tetrahydropyridines in preparing medicine for treating arthritis Download PDFInfo
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- CN101491526A CN101491526A CNA2009100146290A CN200910014629A CN101491526A CN 101491526 A CN101491526 A CN 101491526A CN A2009100146290 A CNA2009100146290 A CN A2009100146290A CN 200910014629 A CN200910014629 A CN 200910014629A CN 101491526 A CN101491526 A CN 101491526A
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- tetrahydropyrimidine
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Abstract
The invention discloses novel application for Ectoine, namely application of the Ectoine in preparing medicines of treating arthritis. The effective dosage range of the Ectoine is 0.1 to 100 mg/kg of body weight, preferably 8 to 50mg/kg of the body weight. When in use, the Ectoine can be used independently, or can be combined with other medicines for use. The Ectoine has high water solubility and osmoregulation function; and the experiment proves that the Ectoine can stabilize joint tissue and joint synovia, improve the adaptability of the joint tissue to environment change and improve the curative effect of other components in a preparation except for the Ectoine, so the Ectoine can be used for treating the arthritis.
Description
Technical field
The present invention relates to the application of tetrahydropyrimidine in the medicine of preparation treatment of arthritis.
Background technology
Arthritis is one of old people's common disease, and arthritis is a kind of common chronic disease, and modal is two kinds of osteoarthritis and rheumatoid arthritis, and the present arthritic of China estimates at more than 100,000,000, and number is also in continuous increase.According to another statistics, China more than 50 years old among the crowd half suffer from osteoarthritis; 90% women and 80% male suffer from osteoarthritis among the over-65s crowd.Rheumatoid arthritis is 0.34%～0.36% in the prevalence of China.Its pathogeny still imperfectly understands, and directly acts on the therapeutical effect that site of pathological change can better be brought into play medicine by the joint intracavitary administration.The effective ingredient of the joint cavity injection preparation of treatment of arthritis is mainly two kinds at present, and a kind of is hormone medicine, and another kind of is transparent hyaluronic acid preparation.
Hormone medicine: some doctor is still adopting intraarticular injection hormone medicine treatment osteoarthritis at present.Though it can temporarily ease the pain, yet repeatedly the intraarticular injection hormone medicine can make articular degeneration, causes " corticosteroid arthrosis ".Hormone also can suppress the substrate of natural joint cartilage and synthesize, and also can increase possibility of infection.
Hyaluronic acid preparation: the high viscosity of synovial fluid can provide almost friction free surface to joint motions in the articular cavity, thereby very favourable to normal function of joint.During osteoarthritis, hyaluronic acid is destroyed, and synovial fluid viscosity reduces, the smooth LOM of lubrication disappearance and articular surface, thus cause the joint further to be destroyed.The supplement therapy of macromolecule hyaluronic acid helps alleviating arthralgia in the articular cavity, increases mobility, eliminates synovial membrane inflammation and delays progression of disease.This class medicine is mainly used in knee joint osseous arthritis, is suitable for the conventional therapy unsatisfactory curative effect, maybe can not tolerate analgesic or on-steroidal AID therapist.
1,4,5,6-tetrahydrochysene-2-methyl-4-pyrimidine carboxylic is commonly called as tetrahydropyrimidine (Ectoine), is a kind of novel amino of finding in 1985, be that many salt-durable microbes are to keep the osmotic pressure balance and a kind of compatible solute of producing in cell, have high water soluble.Tetrahydropyrimidine can be stablized the hydration layer of native protein; biomacromolecule such as protective enzyme, DNA and membrane structure; help various adverse circumstances such as cell resistance is freezing, arid, high temperature, high salt, radiation; the commercial use of exploitation concentrates on cosmetics at present; patent documentation WO0219978 discloses its application in mouth care, and patent documentation DE102004016129 discloses its application in skin nursing and disease prevention.Have not yet to see tetrahydropyrimidine and be used for the treatment of arthritic correlational study and report.
Summary of the invention
At above-mentioned prior art, the invention provides a kind of new purposes of tetrahydropyrimidine.
The present invention comes down to the application of tetrahydropyrimidine in the medicine of preparation treatment of arthritis.
The effective dose of described tetrahydropyrimidine is the 0.1-100mg/kg body weight, preferred 8-50mg/kg body weight.
Described tetrahydropyrimidine uses separately in the medicine of preparation treatment of arthritis.
Described tetrahydropyrimidine is united use with hormone medicine in the medicine of preparation treatment of arthritis.
Described hormone medicine comprises prednisone, meticortelone, dexamethasone.
Described tetrahydropyrimidine in the medicine of preparation treatment of arthritis with arthritis treatment medicine hyaluronate sodium, chondroitin sulfate, chitosan, methotrexate, somatostatin, diclofenac sodium, oxychloroquine, sulfasalazine in a kind of or appoint several uses of uniting.
Described tetrahydropyrimidine in the medicine of preparation treatment of arthritis with analgesics morphine, neostigmine, tramadol in a kind of or appoint several uses of uniting.
Be articular cavity inner injecting and administering during administration, dosage form can be gel or liquid preparation, but is not limited to gel and liquid preparation.
Tetrahydropyrimidine has high water soluble, has the osmotic pressure regulating action, and through evidence, it can stablize joint tissue and knuckle synovia, improves the adaptive capacity of joint tissue to environmental change, improves in the preparation therapeutic effect of other compositions except that tetrahydropyrimidine.Therefore, tetrahydropyrimidine can be used for treatment of arthritis.
The specific embodiment
The present invention is further illustrated below in conjunction with embodiment:
Embodiment 1: the injections in articular cavity medicine that contains tetrahydropyrimidine
Key component tetrahydropyrimidine 2.0g
Hyaluronate sodium 1.0g
Sulfasalazine 3.0g
Get the recipe quantity sulfasalazine and be dissolved in water for injection, tetrahydropyrimidine, hyaluronate sodium are ground well by the recipe quantity mixing, add above-mentioned solution gradually, adjust pH to 6.0-8.5 with phosphate buffer, add sterilized water for injection to 1000ml, adjust osmotic pressure to 220-336 ooze in the least equivalent/liter.Pressure sterilizing, packing promptly gets the injections in articular cavity liquid preparation that contains tetrahydropyrimidine.
Embodiment 2: the injections in articular cavity medicine that contains tetrahydropyrimidine
Key component tetrahydropyrimidine 3.0g
Meticortelone 1.0g
Chondroitin sulfate 4.0g
Neostigmine 1.0g
Get the recipe quantity chondroitin sulfate and be dissolved in ethanol, tetrahydropyrimidine, meticortelone are ground well by the recipe quantity mixing, add gradually and dissolve with 70 ℃ of waters for injection after neostigmine mixes, then two solution are mixed and stir and filter, adjust pH to 5.0-8.0 with phosphate buffer, add sterilized water for injection to 1000ml, adjust osmotic pressure to 220-336 ooze in the least equivalent/liter.Pressure sterilizing, packing promptly gets the injections in articular cavity liquid preparation that contains tetrahydropyrimidine.
Embodiment 3: the injections in articular cavity medicine that contains tetrahydropyrimidine
Key component tetrahydropyrimidine 3.0g
Chitosan 2.0g
Methotrexate 2.0g
With the carbomer is substrate, get carbomer 14.0g and add water-soluble expanding, to 6.0-8.0, other gets chitosan 2.0g and adds 80 ℃ of water for injection swellings, adds the recipe quantity tetrahydropyrimidine while hot with the phosphate buffer adjust pH, then while hot with two liquid mixing, stir, add sterilized water for injection to 1000ml, pressure sterilizing, packing promptly gets the injections in articular cavity preparation that contains tetrahydropyrimidine.
Embodiment 4: tetrahydropyrimidine reaches the pharmacodynamic study of associating other medicines to osteoarthritis separately
Get 30 of new zealand white rabbits, will lie on the back after the Animal Anesthesia on operating-table, get the inboard longitudinal incision of knee joint under the aseptic condition and be about 2cm, appear knee joint, ligamentaum cruciatum and medial collateral ligament before and after cutting off then, complete excision medial meniscus keeps articular cartilage face.Postoperative is not fixedly hindered limb, and is free movable, causes the osteoarthritis animal model, is divided into 5 groups subsequently at random, 6 every group.Model group intraarticular injection normal saline 2ml, the treatment group is intraarticular injection tetrahydropyrimidine (30mg/kg body weight), 1% hyaluronate sodium+tetrahydropyrimidine (30mg/kg body weight), meticortelone (10mg/kg body weight)+tetrahydropyrimidine (30mg/kg body weight), neostigmine (10mg/kg body weight)+tetrahydropyrimidine (30mg/kg body weight) respectively, observe the gait of animal after the administration weekly, after 4 weeks of administration, put to death animal, carry out microscopic examination, and record pathology integration.The result: 1. the change of experimental group osteoarthritis obviously alleviates than matched group.Treatment group gait is all normal than model group, and wherein neostigmine (10mg/kg body weight)+tetrahydropyrimidine (30mg/kg body weight) group gait is normal than other groups; 2. postoperative is during 4 weeks, and the experimental group perichondrium is smooth, chondrocyte marshalling, visible double-core chondrocyte; The matched group perichondrium is also smooth, chondrocyte marshalling but the double-core chondrocyte is not seen in the cartilage layers attenuation.
The scorching pathology table of integrals of rabbit knee
*With model group contrast, P＜0.05,
*With the tetrahydropyrimidine list with comparing P＜0.05.
Therefore, tetrahydropyrimidine separately or associating hyaluronate sodium, meticortelone, neostigmine use and can significantly improve the osteoarthritis pathological symptom, wherein tetrahydropyrimidine and hyaluronate sodium, meticortelone are united the use curative effect and are better than tetrahydropyrimidine and use separately.
Claims (9)
1. the application of tetrahydropyrimidine in the medicine of preparation treatment of arthritis.
2. application according to claim 1 is characterized in that: the effective dose of described tetrahydropyrimidine is the 0.1-100mg/kg body weight.
3. application according to claim 2 is characterized in that: the effective dose of described tetrahydropyrimidine is the 8-50mg/kg body weight.
4. application according to claim 1 is characterized in that: be that tetrahydropyrimidine is made the intraarticular injection preparation.
5. application according to claim 1 is characterized in that: described tetrahydropyrimidine uses separately in the medicine of preparation treatment of arthritis.
6. application according to claim 1 is characterized in that: described tetrahydropyrimidine is united use with hormone medicine in the medicine of preparation treatment of arthritis.
7. application according to claim 6 is characterized in that: described hormone medicine comprises prednisone, meticortelone, dexamethasone.
8. application according to claim 1 is characterized in that: described tetrahydropyrimidine in the medicine of preparation treatment of arthritis with arthritis treatment medicine hyaluronate sodium, chondroitin sulfate, chitosan, methotrexate, somatostatin, diclofenac sodium, oxychloroquine, sulfasalazine in a kind of or appoint several uses of uniting.
9. application according to claim 1 is characterized in that: described tetrahydropyrimidine in the medicine of preparation treatment of arthritis with analgesics morphine, neostigmine, tramadol in a kind of or appoint several uses of uniting.
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2009100146290A CN101491526A (en) | 2009-03-03 | 2009-03-03 | Use of tetrahydropyridines in preparing medicine for treating arthritis |
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| CNA2009100146290A CN101491526A (en) | 2009-03-03 | 2009-03-03 | Use of tetrahydropyridines in preparing medicine for treating arthritis |
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Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102210682A (en) * | 2011-04-29 | 2011-10-12 | 山东弘立医学动物实验研究有限公司 | Application of tetrahydropyrimidine and derivatives thereof in preparing medicament for treating cystitis |
| CN102228445A (en) * | 2011-06-30 | 2011-11-02 | 山东弘立医学动物实验研究有限公司 | Freeze-dried powder of ectoine or ectoine derivative for injection |
| CN102258520A (en) * | 2011-04-29 | 2011-11-30 | 济南环肽医药科技有限公司 | Medicinal composition for preventing or treating cystitis caused by chemotherapy |
| CN108778250A (en) * | 2016-03-07 | 2018-11-09 | 乌尔萨法姆药物有限责任公司 | Ophthalmic composition |
-
2009
- 2009-03-03 CN CNA2009100146290A patent/CN101491526A/en active Pending
Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102210682A (en) * | 2011-04-29 | 2011-10-12 | 山东弘立医学动物实验研究有限公司 | Application of tetrahydropyrimidine and derivatives thereof in preparing medicament for treating cystitis |
| CN102258520A (en) * | 2011-04-29 | 2011-11-30 | 济南环肽医药科技有限公司 | Medicinal composition for preventing or treating cystitis caused by chemotherapy |
| CN102210682B (en) * | 2011-04-29 | 2012-08-01 | 山东弘立医学动物实验研究有限公司 | Application of tetrahydropyrimidine and derivatives thereof in preparing medicament for treating cystitis |
| CN102258520B (en) * | 2011-04-29 | 2012-10-03 | 济南环肽医药科技有限公司 | Medicinal composition for preventing or treating cystitis caused by chemotherapy |
| CN102228445A (en) * | 2011-06-30 | 2011-11-02 | 山东弘立医学动物实验研究有限公司 | Freeze-dried powder of ectoine or ectoine derivative for injection |
| CN108778250A (en) * | 2016-03-07 | 2018-11-09 | 乌尔萨法姆药物有限责任公司 | Ophthalmic composition |
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Open date: 20090729 |