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Pharmaceutical composition of acedapsone and application thereof in orthopedics

A technology of dapsone and its composition, applied in the field of pharmaceutical composition and its application in orthopedics, can solve the problems of many drug side effects, high price, and application of dapsone and its pharmaceutical composition, etc. To achieve the effect of improving the therapeutic effect

Inactive Publication Date: 2016-07-06
李晨露
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there are many drugs for the clinical treatment of osteoporosis. Western medicine mainly includes preparations that inhibit bone resorption and preparations that stimulate bone formation. The short-term curative effect is satisfactory, but the long-term effect is not sure. Moreover, the drugs have many side effects and are expensive.
[0006] There is no application of dapsone and its pharmaceutical composition in orthopedics

Method used

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  • Pharmaceutical composition of acedapsone and application thereof in orthopedics
  • Pharmaceutical composition of acedapsone and application thereof in orthopedics
  • Pharmaceutical composition of acedapsone and application thereof in orthopedics

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] Example 1: Compound (I) Separation Preparation and Structure Confirmation

[0019] Sources of reagents: ethanol, petroleum ether, ethyl acetate, n-butanol, and dichloromethane were of analytical grade, purchased from Shanghai Lingfeng Chemical Reagent Co., Ltd. Methanol, of analytical grade, were purchased from Jiangsu Hanbang Chemical Reagent Co., Ltd.

[0020] Separation method: (a) Grind the dried root (2kg) of pokeweed, extract with 75% ethanol under heat reflux (20L×3 times), combine the extracts, concentrate until no alcohol smell (4L), and then use petroleum ether (4L ×3 times), ethyl acetate (4L×3 times) and water-saturated n-butanol (4L×3 times) were extracted to obtain petroleum ether extract, ethyl acetate extract and n-butanol extract respectively; (b) In the step (a), the n-butanol extract is removed with AB-8 macroporous resin, first eluted with 8% ethanol for 6 column volumes, then with 70% ethanol for 8 column volumes, and collected 70% eluate , concent...

Embodiment 2

[0023] Example 2: Therapeutic effect on bone destructive diseases

[0024] 1. Materials and Instruments

[0025] SD male rats (4 weeks old) were purchased from the Animal Experiment Center of Nanjing University, clean grade, weighing 150 g. Dapsone was purchased from China Institute for the Control of Pharmaceutical and Biological Products. Compound (I) was self-made according to the method of Example 1, and the HPLC normalized purity was greater than 98%. 1α,25(OH) 2 D. 3 Purchased from Plymouth Biological Research Laboratories, UK. α-MEM medium was purchased from GIBCOBRL, USA. SolubleRANKL was purchased from PeprotecScience, UK. Tartrate-resistant acid phosphatase (TRAP) kit was purchased from Sigma, USA. Dextran gel was purchased from Shanghai Ruji Technology Development Co., Ltd. Standard fetal bovine serum was purchased from Shandong Yinxiang Weiye Biological Co., Ltd. Penicillin sodium for injection was purchased from North China Pharmaceutical Co., Ltd. Strep...

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Abstract

The invention discloses a pharmaceutical composition of dapsone and its application in orthopedics. The pharmaceutical composition of dapsone provided by the invention contains dapsone and a kind of dried root of pokeweed The isolated natural product compound (I) with a novel structure, when dapsone and the natural product compound (I) act alone, have a general therapeutic effect on bone-destructive diseases; The therapeutic effect of the invention is significantly improved, and can be developed into a drug for treating bone destructive diseases, and has outstanding substantive characteristics and significant progress compared with the prior art.

Description

technical field [0001] The invention belongs to the field of biomedicine and relates to a new application of dapsone, in particular to a pharmaceutical composition of dapsone and its application in orthopedics. Background technique [0002] The chemical name of dapsone is 4,4'-sulfonylbis(acetanilide). Its molecular formula: C 16 h 16 N 2 o 4 S, molecular weight: 332.38. [0003] Dapsone is a sulfone bacteriostatic agent, which is slowly decomposed into dapsone or monoacetyl dapsone in the body to play an anti-leprosy effect. For the prevention of leprosy and those who cannot take sulfone drugs orally. This product has a long-acting effect and can last for 60-75 days after one injection. [0004] Osteoclasts are cells with bone erosion function. They have various shapes, usually in the shape of fried eggs, long strips, etc., and pseudopodia can be seen. They are larger than ordinary cells and contain several to dozens of nuclei. Osteoclasts and osteoblasts play a maj...

Claims

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Application Information

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IPC IPC(8): C07D491/22A61K31/4375A61K31/167A61P19/08A61P19/10A61P1/02
CPCC07D491/22A61K31/167A61K31/4375
Inventor 李晨露
Owner 李晨露