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Aprindine hydrochloride medicinal composition and medicinal use thereof

A technology of aplindine hydrochloride and its composition, which is applied in the field of pharmaceutical composition of aplindine hydrochloride, can solve the problems that have not yet been reported on the sedation and tranquilization of aplindine hydrochloride, and achieve outstanding substantive features, sedative Strong calming effect

Inactive Publication Date: 2016-09-07
徐玉仙
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] So far, there has been no report on the correlation between aplinidine hydrochloride and its pharmaceutical composition and sedation and tranquilization

Method used

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  • Aprindine hydrochloride medicinal composition and medicinal use thereof
  • Aprindine hydrochloride medicinal composition and medicinal use thereof
  • Aprindine hydrochloride medicinal composition and medicinal use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Example 1: Compound (I) Separation Preparation and Structure Confirmation

[0022] 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.

[0023] Separation method: (a) Grind the dried tuber root (2kg) of Pseudostellariae Pseudostellariae, extract with 80% ethanol under heat reflux (15L×3 times), combine the extracts, concentrate until there is 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) In the step (a), the n-butanol extract is removed with a D101 type macroporous resin, and first eluted with 10% ethanol for 8 column volumes, then with 70% ethanol for 1...

Embodiment 2

[0026] Embodiment 2: pharmacological action

[0027] 1. Materials and methods

[0028] 1.1 Animals

[0029] Kunming mice, weighing 18-25 g, were bred and provided by the Laboratory Animal Laboratory of China Pharmaceutical University.

[0030]1.2 Reagents and samples

[0031] Apulin hydrochloride 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.

[0032] 1.3 Mouse grouping and model preparation

[0033] The mice were randomly divided into 4 groups, 12 in each group, respectively the model control group, the aplinidine hydrochloride group (40 mg·kg -1 ), compound (I) group (40mg·kg -1 ), aplindine hydrochloride and compound (I) composition group [20mg·kg -1 Aplindine hydrochloride+20mg·kg -1 Compound (I)], orally administered by gavage.

[0034] 1.4 Pentobarbital Sodium Subthreshold Hypnotic Dose Determination

[0035] 1 hour after intragas...

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Abstract

The invention discloses an aprindine hydrochloride medicinal composition and a medicinal use thereof. The aprindine hydrochloride medicinal composition contains aprindine hydrochloride and a novel-structured natural product compound (I) separated from dry root tuber of Radix Pseudostellariae. Aprindine hydrochloride and the compound (I) respectively act to promote mind tranquilizing; and aprindine hydrochloride and the compound (I) are combined to realize an enhanced mind tranquilizing effect, have synergism, and can be used to develop mind tranquilizing medicines. Compared with medicinal compositions in the prior art, the medicinal composition disclosed in the invention has protruding substantive characteristics and substantial progress.

Description

technical field [0001] The invention belongs to the field of biomedicine and relates to a new application of aplindine hydrochloride, in particular to a pharmaceutical composition of aplindine hydrochloride and its medical application. Background technique [0002] The chemical name of aplindine hydrochloride is N,N'-diethyl-N'-2-indanyl-N'-phenyl-1,3-propanediamine monohydrochloride. [0003] Aplindine hydrochloride is a class Ib-antiarrhythmic drug that inhibits the response of the cell membrane to Na + permeability, but does not promote K + Outflow can slow down the conduction of various parts of the cardiac conduction system, reduce membrane reactivity, increase the excitation threshold, prolong the effective adaptation period of the atrium, atrioventricular node, His-Purkinje system and ventricle, and block the forward direction of the bypass pathway. and reverse conduction. [0004] So far, there is no report on the correlation between aplindine hydrochloride and it...

Claims

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Application Information

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IPC IPC(8): C07D471/20A61K31/439A61P25/20A61K31/136
CPCC07D471/20A61K31/136A61K31/439A61K2300/00
Inventor 徐玉仙
Owner 徐玉仙
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