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Drug composition of bisoprolol fumarate and pharmaceutical application thereof

A technology of bisoprolol fumarate and its composition, which is applied in the directions of drug combinations, medical preparations containing active ingredients, pharmaceutical formulas, etc., and can solve the related reports on bisoprolol fumarate and its pharmaceutical composition that have not yet been seen and other issues, to achieve the effect of highlighting substantive characteristics, good effect, and significant progress

Inactive Publication Date: 2016-08-24
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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 bisoprolol fumarate and its pharmaceutical composition and anti-inflammatory and cough-relieving effects

Method used

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  • Drug composition of bisoprolol fumarate and pharmaceutical application thereof
  • Drug composition of bisoprolol fumarate and pharmaceutical application thereof
  • Drug composition of bisoprolol fumarate and pharmaceutical application 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 loquat leaves (2kg), extract them under reflux with 75% ethanol (20L×3 times), combine the extracts, concentrate until there is no alcohol smell (4L), and then use petroleum ether (4L×3 times) 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) step (a) Use D101 type macroporous resin to remove impurities from the n-butanol extract in (a), first elute with 15% ethanol for 6 column volumes, then use 70% ethanol for 10 column volumes,...

Embodiment 2

[0026] Embodiment 2: pharmacological action

[0027] 1. Materials and methods

[0028] 1.1 Drugs and reagents

[0029] Bisoprolol fumarate 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. Glacial acetic acid is produced by Guangxi Nanning Chemical Reagent Factory; xylene is produced by China National Pharmaceutical Group Shanghai Chemical Reagent Company; Aspirin tablets (100mg / tablet) were produced by Bayer Pharmaceutical Company; Guilong Kechuanning Capsules were produced by Shanxi Guilong Pharmaceutical Co., Ltd.; Juhong Granules were produced by Nanchang Kangzhengde Pharmaceutical Co., Ltd.

[0030] 1.2 Experimental animals

[0031] 90 Kunming mice, weighing (20±2) g, male and female, 60 Wistar rats, weighing (200±20) g, male and female, were provided by Hubei Experimental Animal Center.

[0032] 1.3 Equipment

[0033] 1. 80-2 type centrifuge, pro...

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PUM

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Abstract

The invention discloses a drug composition of bisoprolol fumarate and a pharmaceutical application thereof. The drug composition of the bisoprolol fumarate contains the bisoprolol fumarate and a novel-structured natural product compound (I) separated from dried loquat leaves, wherein a compound of the bisoprolol fumarate and the compound (I) has obvious anti-inflammation and cough-reliving effects which is better than the independent anti-inflammation and cough-reliving effects of the bisoprolol fumarate or the compound (I), and can be developed into an anti-inflammation and cough-reliving drug. Compared with the prior art, the drug composition has prominent substantive features and remarkable progress.

Description

technical field [0001] The invention belongs to the field of biomedicine and relates to a new application of bisoprolol fumarate, in particular to a pharmaceutical composition of bisoprolol fumarate and its application in anti-inflammatory and cough-relieving. Background technique [0002] Bisoprolol fumarate is a β-receptor blocker, which has a high affinity for β1-receptors of bronchial and vascular smooth muscle, thereby dilating blood vessels and lowering blood pressure. It is suitable for hypertension, coronary heart disease, and moderate to severe chronic stable heart failure. [0003] Bisoprolol fumarate is a highly selective β1-adrenoceptor antagonist without intrinsic sympathomimetic and membrane stabilizing activity. Bisoprolol fumarate has high affinity to β1-receptors of bronchial and vascular smooth muscle, but only low affinity to β2-receptors of bronchial and vascular smooth muscle and regulation of metabolism. Therefore, bisoprolol fumarate generally does n...

Claims

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Application Information

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IPC IPC(8): C07D311/94A61K31/352A61P29/00A61P11/14A61K31/138
CPCA61K31/138A61K31/352C07D311/94A61K2300/00
Inventor 徐挺
Owner 徐挺
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