Pharmaceutical composition of bezafibrate and application thereof to rheumatoid arthritis

A bezafibrate and rheumatoid technology, applied in the field of biomedicine, can solve the problems that have not been reported related to bezafibrate rheumatoid arthritis, etc., and achieve the goal of highlighting substantive features, improving effects, and making significant progress Effect

Inactive Publication Date: 2016-11-16
赵吉永
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] There is no report on the relationship between bezafibrate and the treatment of rheumatoid arthritis

Method used

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  • Pharmaceutical composition of bezafibrate and application thereof to rheumatoid arthritis
  • Pharmaceutical composition of bezafibrate and application thereof to rheumatoid arthritis
  • Pharmaceutical composition of bezafibrate and application thereof to rheumatoid arthritis

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Example 1: Compound (I) Separation Preparation and Structure Confirmation

[0020] Separation method: (a) crush the dried flower buds (2kg) of cloves, extract with 80% ethanol under heat reflux (15L × 3 times), combine the extracts, concentrate until no alcohol smell (3L), and then use petroleum ether (3L× 3 times), ethyl acetate (3L × 3 times) and water-saturated n-butanol (3L × 3 times) were extracted to obtain petroleum ether extract, ethyl acetate extract and n-butanol extract respectively; (b) step (a) The ethyl acetate extract in (a) was removed with D101 type macroporous resin, first eluted with 20% ethanol for 12 column volumes, then with 80% ethanol for 15 column volumes, collected 80% eluate, and subtracted Concentrate under pressure to obtain 80% ethanol elution concentrate; (c) in step (b), 80% ethanol elution concentrate is separated with normal phase silica gel, and the volume ratio is 80:1 (10 column volumes), 40:1 successively (8 column volumes), 20:1 (...

Embodiment 2

[0024] Embodiment 2: pharmacological action

[0025] 1. Materials and methods

[0026] 1.1 Animals

[0027] Male Wistar rats (provided by the Animal Experiment Center of Tongji Medical College, Huazhong University of Science and Technology) with a body weight of about 120 g were selected.

[0028] 1.2 Reagents and samples

[0029] Bezafibrate was purchased from China National Institute for the Control of Pharmaceutical and Biological Products. Compound (I) is self-made, and the preparation method is shown in Example 1. Type Ⅱ collagen (Sigma, USA), incomplete Freund's adjuvant (Sigma), and RPMI-1640 (GIBCO).

[0030] 1.3 Instruments

[0031] American Nurie CO 2 Incubator (NU4750 type), Japanese Olympian inverted fluorescence microscope (CKX41 type), American Beckman Coulter flow cytometer (EPICSXL type), Japanese transmission electron microscope (Hitachi H-7500 type).

[0032] 1.4 Rat model preparation and cell grouping

[0033] Preparation of CIA Rat Model Dissolve ty...

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PUM

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Abstract

The invention discloses a pharmaceutical composition of bezafibrate and application thereof to rheumatoid arthritis. The pharmaceutical composition of bezafibrate provided by the invention contains bezafibrate and a natural compound (I) with novel structure and isolated from the dried clove buds; when bezafibrate and the compound (I) are combined for action, the synovial cells arrest in a G1 phase of a cell cycle, thereby inhibiting the proliferation of synovial cells for the treatment of rheumatoid arthritis. The treatment effect of the pharmaceutical composition is better than the individual effect of bezafibrate or compound (I). The composition of bezafibrate and compound (I) can be developed into drugs for the treatment of rheumatoid arthritis. Compared with the prior art, the invention has prominent substantive features and obvious progress.

Description

technical field [0001] The invention belongs to the field of biomedicine and relates to a new application of bezafibrate, in particular to a pharmaceutical composition of bezafibrate and its application in rheumatoid arthritis. Background technique [0002] Bezafibrate belongs to the class of fibrates. It was launched in the market for the first time in the 1970s. It has undergone a large number of clinical application tests and large-scale systematic clinical trials around the world. It has been confirmed that it can significantly reduce triglycerides, increase High-density lipoprotein levels can delay the progression of coronary atherosclerotic lesions and reduce the risk of coronary heart disease events. There are two mechanisms for its blood lipid-lowering effect. One is that this product can increase the activity of lipoprotein lipase and liver lipase, promote the catabolism of very low-density lipoprotein, and reduce the level of triglyceride in plasma; The secretion ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/365A61K31/192C07D307/93A61P19/02A61P29/00
CPCA61K31/192A61K31/365A61K36/61C07D307/93A61K2300/00A61P19/02A61P29/00
Inventor 不公告发明人
Owner 赵吉永
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