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Baclofen drug composition and application thereof in bone destructive diseases

A technology of baclofen and a composition, applied to a pharmaceutical composition and its application field in bone destructive diseases, can solve the problems of many drug side effects, high price, and no reports of baclofen bone destructive diseases, etc., To achieve the effect of improving the treatment effect

Inactive Publication Date: 2016-06-08
钱浩
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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 relevant report on baclofen and its pharmaceutical composition and bone destructive diseases

Method used

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  • Baclofen drug composition and application thereof in bone destructive diseases
  • Baclofen drug composition and application thereof in bone destructive diseases
  • Baclofen drug composition and application thereof in bone destructive diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Example 1: Compound (I) Separation Preparation and Structure Confirmation

[0021] 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.

[0022] Separation method: (a) Grind the dried root (2kg) of Burnet, 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 , concentra...

Embodiment 2

[0025] Example 2: Therapeutic effect on bone destructive diseases

[0026] 1. Materials and Instruments

[0027] SD male rats (4 weeks old) were purchased from the Animal Experiment Center of Nanjing University, clean grade, weighing 150 g. Baclofen 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. Stre...

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Abstract

The invention discloses a baclofen drug composition and an application thereof in bone destructive diseases. The baclofen drug composition comprises baclofen and a natural product compound (I), wherein the natural product compound (I) is of a novel structure and is separated from dried roots of garden burnet. The baclofen drug composition has the advantages that when the baclofen and the natural product compound (I) singly act, the effect of treating the bone destructive diseases is weaker; when the baclofen and the natural product compound (I) jointly act, the effect of treating the bone destructive diseases is obviously improved, and the baclofen drug composition can be developed into a drug for treating the bone destructive diseases; compared with the prior art, the outstanding material characteristics and obvious progress are realized.

Description

technical field [0001] The invention belongs to the field of biomedicine and relates to a new application of baclofen, in particular to a pharmaceutical composition of baclofen and its application in bone destructive diseases. Background technique [0002] The Chinese aliases of Baclofen are Baclofen, Beikangfen, Beikefen, Heluxing, Liluxing, Chlorpheniram, Chlorpheniram Butyric Acid, Baclofen (γ-aminobutyric acid analogues), for Skeletal muscle relaxants. The mechanism is still unknown, it may interfere with the release of excitatory neurotransmitters and inhibit the conduction between spinal cord synapses. Baclofen can activate GABAβ receptors, reduce the reflex potential of spinal cord monosynapse or polysynapse and the reflex potential between spinal cord dorsal root and dorsal root, and produce skeletal muscle relaxation. Since the 1970s, it has been widely used in spinal cord in foreign countries. There is no report on the use of this type of drug in patients with tr...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J73/00A61K31/585A61K31/195A61K36/739A61P19/08
CPCC07J73/003A61K31/195A61K31/585A61K2300/00
Inventor 不公告发明人
Owner 钱浩
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