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A triptolide composite preparation for treating osteoarthritis by joint intracavity injection

A technology of triptolide and triptolide, which is applied in the field of triptolide compound preparations, can solve the problems of low local absorption rate, poor tissue permeability, skin irritation, etc., and achieve reduced dosage, significant therapeutic effect, and reduced Toxic effects

Inactive Publication Date: 2006-11-22
THE FIRST AFFILIATED HOSPITAL OF THIRD MILITARY MEDICAL UNIVERSITY OF PLA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to its large molecular weight and insolubility in water, the tissue permeability of the drug is poor, the local absorption rate is low, and it has a certain stimulating effect on the skin, so the therapeutic effect is relatively poor.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Embodiment 1: the selection of compound preparation proportioning:

[0029] Experiments have shown that the concentration of triptolide at 1 × 10 -4 mg / ml~5×10 -2 There is a therapeutic effect in the mg / ml range, and the higher the concentration, the better the effect, but the upper limit concentration may begin to appear toxic side effects; the addition of hyaluronic acid or chitosan or its derivative solution can reduce toxic side effects. Tests have shown that the concentration is 5×10 -2 The optimum volume ratio of mg / ml triptolide solution to hyaluronic acid or chitosan or its derivative solution is 1:7~9; the concentration is 1×10 -4 The optimum volume ratio of mg / ml triptolide solution to hyaluronic acid or chitosan or its derivative solution is 1:1-2.

[0030] In addition, it is necessary to determine the concentration and optimal volume ratio of triptolide and hyaluronic acid or chitosan or its derivatives solution according to the degree of osteoarthritis l...

Embodiment 2

[0031] Example 2 Preparation method 1:

[0032] At room temperature, each mg of triptolide was first dissolved in 1ml of absolute ethanol, then dissolved in 0.5ml of dimethyl sulfoxide, and diluted with normal saline to a corresponding concentration of 5×10 -3mg / ml, after filtering through a double-layer filter membrane of 0.22 μm, it is uniformly mixed with carboxymethyl chitosan solution in a volume ratio of 1:9, wherein the preparation process of carboxymethyl chitosan solution is: every 10g of carboxymethyl chitosan Base chitosan was dissolved in 1 liter of distilled water, and sterilized by high temperature and high pressure (115°C). Chitosan can also be oligochitosan, hydroxychitosan and the like.

[0033] Preparation method 2:

[0034] At room temperature, each mg of triptolide was first dissolved in 1ml of absolute ethanol, then dissolved in 0.5ml of dimethyl sulfoxide, and diluted with normal saline to a corresponding concentration of 5×10 -3 mg / ml, after filtering...

Embodiment 3

[0035] Embodiment 3 Animal experiments related to curative effect

[0036] The compound preparation obtained in the preparation method 1 in Example 2 was used to observe the curative effect on Japanese big-eared white rabbits. The rabbit osteoarthritis model was made by injecting type II collagenase into the knee joint cavity, and the compound preparation obtained in the preparation method 1 in Example 2 was used for treatment, 0.4ml / time for each knee joint, 1 time / week, 4 times in total . The observations are as follows:

[0037] 1) After 4 weeks of treatment, the body position of the animals basically returned to normal when resting, and the body weight growth trend was greater than that of the normal saline injection group, the hyaluronic acid alone and the same dose of triptolide alone.

[0038] 2) The degree of degeneration of articular cartilage in general observation and histomorphology was milder than that in the normal saline group, hyaluronic acid alone and tripto...

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PUM

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Abstract

The present invention relates to one kind of compound triptolide alcohol preparation for being injected into articular cavity to treat osteoarthritis. It includes triptolide alcohol solution of 1*10<-4> to 5*10<-2> mg / ml concentration and gel liquid mixed in the volume ratio of 1 to 1-9. It has medicine slow releasing effect, and this can prolong the action period of medicine, reduce consumption of triptolide alcohol and lower the toxic side effect of the medicine. It can inhibit the further development of osteoarthritis in early and middle phase, improve the environment inside the joint and promote the regeneration and repair of articular cartilage to reach the aim of cure osteoarthritis.

Description

Technical field: [0001] The invention relates to an injection preparation for treating osteoarthritis, in particular to a triptolide compound preparation for intra-articular injection for treating osteoarthritis. technical background: [0002] Osteoarthritis (Osteoarthritis) is the most common chronic osteoarthritis characterized by joint cartilage degeneration and secondary bone hyperplasia, which can be divided into primary and secondary. Osteoarthritis is the second leading cause of long-term disability after cardiovascular disease in people over the age of 50. Disease surveys show that the prevalence rate of osteoarthritis in my country is about 10%, and the prevalence rate of the elderly over 60 years old is as high as 50%, and its prevalence rate rises linearly with the increase of age; the incidence rate in rural areas is 9.6%, compared to 49% among urban retirees. In recent years, there have been a lot of studies on the drug treatment of osteoarthritis, and new drug...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K31/585A61K47/36A61P19/02
Inventor 戴刚张卫东杨柳
Owner THE FIRST AFFILIATED HOSPITAL OF THIRD MILITARY MEDICAL UNIVERSITY OF PLA
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