Anti-arthritis medicine composition

An anti-arthritis and composition technology, applied in the field of medicine, can solve the problems of little effect, achieve the effects of reducing toxic side effects, high heart safety, and improving therapeutic effect

Active Publication Date: 2020-08-25
香港浸会大学深圳研究院
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, attempts to develop COX-2 inhibitors through chemical synthesis or modification have met with little success

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Embodiment 1: the preparation of pharmaceutical composition (for research in vitro)

[0041] Take scopoletin 1.9216g, add dimethyl sulfoxide (DMSO) 5mL, mix and set aside, as the mother solution of scopoletin (2M). Take 3.7237g of syringin, add 5mL of DMSO, and mix well for later use as the mother solution of syringin (2M). Preparation of scopoletin and syringin in different ratios of substances for in vitro studies:

[0042] (1) 1:0

[0043] Dilute scopoletin mother solution with DMEM medium to 12.5, 25, 50, 100, 150, 200 μM;

[0044] (2) 0:1

[0045] Dilute syringin mother solution with DMEM medium to 12.5, 25, 50, 100, 150, 200 μM;

[0046] (3) 1:1

[0047] Scopoletin and syringin mother liquor were mixed at a ratio of 1:1 to obtain a mixture, and the solute concentration of the mixture was diluted with medium to 12.5, 25, 50, 100, 150, 200 μM;

[0048] (4)1:5

[0049] Scopoletin and syringin mother liquor were mixed at a ratio of 1:5 to obtain a mixture, and ...

Embodiment 2

[0052] Example 2: Preparation of pharmaceutical composition (for in vivo studies)

[0053] Different mass ratios of scopoletin and syringin were prepared for in vivo studies:

[0054] (1) 1:0

[0055] Take scopoletin 10g, add 5% CMC-Na 50mL, dilute to 200mg / mL solution;

[0056] (2) 0:1

[0057] Take 10g of syringin, add 5% CMC-Na 50mL, and dilute to 200mg / mL solution;

[0058] (3) 1:1

[0059] Take 5 g each of scopoletin and syringin, add 50 mL of 5% CMC-Na, and dilute to a 200 mg / mL solution.

Embodiment 3

[0060] Embodiment 3: the in vitro myocardial safety test of pharmaceutical composition

[0061]Cardiomyocytes H9c2 were seeded in 96-well plates (5000 cells / well). After 24 hours, the cells were congested, and different ratios of scopoletin and syringin (1:0, 0:1, 1:1, 1:1) were added. 5, 1:9; the concentration of each ratio is 12.5, 25, 50, 100, 200 μM) / celecoxib (12.5, 25, 50, 100, 200 μM) and incubated for 24 hours. Using the culture medium as a negative control and celecoxib as a positive control, the cell survival rate is detected by the MTT method, and then the cytotoxic effect of the pharmaceutical composition is evaluated.

[0062] Dissolve 30 mg of MTT powder in 6 mL of phosphate-buffered saline (PBS) in the dark, add 10 μL to each well, and incubate in the incubator for 2 h in the dark. Then centrifuge (1000rpm, 10min), carefully suck off the supernatant, add 100μL DMSO to each well, and place on a shaker for 10min at low speed to fully dissolve the crystals. The a...

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Abstract

The invention discloses an anti-arthritis medicine composition. Scopoletin and syringin are prepared at a mass ratio of 1: 1 to obtain the medicine composition. The anti-arthritis medicine compositionhas good cardiac safety, a good in vitro and vivo COX-2 inhibition function and a good in vivo anti-arthritis function. The composition performs a certain synergy function on the aspects of safety and curative activity. The composition has a certain meaning for eliminating a situation that a chemical synthesis medicine in an existing anti-arthritis medicine generally has cardiotoxicity.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to an anti-arthritic pharmaceutical composition. Background technique [0002] Arthritis is a chronic joint disease that can cause progressive joint damage and systemic complications, resulting in heavy social and economic burdens. The most common types of arthritis include rheumatoid arthritis (RA) and osteoarthritis (OA). RA is an autoimmune disease in which the joints are attacked by the body's own immune system, with a global prevalence of about 1% and can appear at any age. OA is a degenerative joint disease caused by the wear and tear of cartilage, affecting approximately 10% of the population over the age of 60 and ranking fifth among all forms of disability worldwide. Common symptoms of RA and OA include joint swelling due to soft tissue inflammation and pain during or after exercise, especially morning stiffness and loss of mobility. The etiology of RA and O...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/352A61K31/7034A61P19/02
CPCA61K31/352A61K31/7034A61P19/02A61K2300/00
Inventor 易涛陈绮蕾陈虎彪祝琳江滔吴亮叶桦珍
Owner 香港浸会大学深圳研究院
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