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Pharmaceutical composition of difenidol hydrochloride and application thereof in biological medicines

A technology of diphenidol hydrochloride and a composition is applied to pharmaceutical compositions and the application field in biomedicine, and can solve the problems such as the related reports about diphenidol hydrochloride cholestatic hepatitis and the like, and achieve a therapeutic effect improved effect

Inactive Publication Date: 2016-11-16
胡逸穹
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] So far, there has been no report on the correlation between difenidol hydrochloride and its pharmaceutical composition and cholestatic hepatitis

Method used

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  • Pharmaceutical composition of difenidol hydrochloride and application thereof in biological medicines
  • Pharmaceutical composition of difenidol hydrochloride and application thereof in biological medicines
  • Pharmaceutical composition of difenidol hydrochloride and application thereof in biological medicines

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) Ginseng leaves (2kg) were crushed, extracted with 65% ethanol under heat reflux (20L×3 times), the extracts were combined, concentrated to no alcohol smell (4L), and petroleum ether (4L×3 times) was used successively ), ethyl acetate (4L × 3 times) and water-saturated n-butanol (4L × 3 times) extraction, respectively obtain petroleum ether extract, ethyl acetate extract and n-butanol extract; (b) step (a ) in n-butanol extract with AB-8 type macroporous resin for impurity removal, first elute 12 column volumes with 10% ethanol, then elute 15 column volumes with 70% ethanol, collect 70% elu...

Embodiment 2

[0024] Embodiment 2: pharmacological action

[0025] In this example, α-naphthalene isothiocyanate (α-naphthylisothiocy, ANIT) was used to prepare a rat model of acute cholestatic hepatitis, and the drug was observed to reduce serum alanine aminotransferase (ALT), aspartate aminotransferase (AST), and total bilirubin. (TBIL), direct bilirubin (DBIL), alkaline phosphatase (ALP), and anti-acute cholestatic hepatitis in terms of increasing bile flow.

[0026] 1. Materials and methods

[0027] 1.1 Animals

[0028] Clean-grade male Wistar rats, 200-220 g, were provided by the Experimental Animal Center of the Academy of Military Medical Sciences of the Chinese People's Liberation Army.

[0029] 1.2 Reagents and samples

[0030] Diphenidol hydrochloride was purchased from China Institute for the Control of Pharmaceutical and Biological Products. Compound (I) is self-made, and the preparation method is shown in Example 1. α-Naphthalene isothiocyanate (ANIT, Sigma company) was ma...

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Abstract

The invention discloses a pharmaceutical composition of difenidol hydrochloride and its application in biomedicine. The pharmaceutical composition of difenidol hydrochloride provided by the invention contains difenidol hydrochloride and a natural product with a novel structure Compound (I), difenidol hydrochloride and compound (I) have a therapeutic effect on cholestatic hepatitis when they act alone; when difenidol hydrochloride and compound (I) act in combination, they have a therapeutic effect on cholestatic hepatitis Further improvement can be developed into a drug for treating cholestatic hepatitis, which has outstanding substantive features and remarkable 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 difenidol hydrochloride, in particular to a pharmaceutical composition of difenidol hydrochloride and its application in biomedicine. Background technique [0002] Diphenidol hydrochloride can improve the blood supply of the vertebral artery, regulate the function of the vestibular system, inhibit the vomiting center, and have anti-vertigo and antiemetic effects. [0003] So far, there is no report on the correlation between difenidol hydrochloride and its pharmaceutical composition and cholestatic hepatitis. Contents of the invention [0004] The object of the present invention is to provide a pharmaceutical composition of difenidol hydrochloride, which contains difenidol hydrochloride and a natural product with a novel structure, and difenidol hydrochloride and the natural product can be synergistically treated Cholestatic hepatitis. [0005] Above-mentioned pur...

Claims

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Application Information

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IPC IPC(8): A61K31/4453A61K31/366C07D493/10A61P1/16
CPCA61K31/4453A61K31/366A61K36/258C07D493/10
Inventor 胡逸穹
Owner 胡逸穹
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