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Isradipine pharmaceutical composition with improved bioavailability

A technology of isradipine and its composition, which is applied in the field of isradipine pharmaceutical preparations, can solve the problems of poor solubility, low bioavailability of active ingredients, low water solubility, etc.

Inactive Publication Date: 2017-11-03
HEFEI HUAFANG PHARMA SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But the water solubility of isradipine medicine is low (dissolubility is poor), causes the bioavailability of active ingredient to be low, not only there is certain difficulty in the pharmaceutical preparation of medical field, and because isradipine medicine bioavailability is low, causes its In clinical application, the curative effect is not satisfactory and needs to be solved

Method used

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  • Isradipine pharmaceutical composition with improved bioavailability
  • Isradipine pharmaceutical composition with improved bioavailability

Examples

Experimental program
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Effect test

experiment example 1

[0030] Twelve healthy Beagle dogs were selected and randomly divided into three groups, 4 dogs in each group, which were fed with normal group, seaweed (containing Fe3+ ions) group and vitamin C group respectively. During the test period, Beagle dogs were fasted overnight without water (feeding deionized water) for at least 12 hours, collected venous blood, separated plasma, and used it as a 0-hour blood drug concentration sample. Then began to feed according to the experimental grouping. The dogs in the normal group were not fed food, the dogs in the laver group were fed with 100ml of laver soup, and the dogs in the vitamin C group were fed with 0.1g of vitamin C tablets (1 tablet, 0.1g / tablet). After 30 minutes, each dog was fed with isradipine tablet 5 mg (2 tablets, 2.5 mg / tablet). After administration, blood samples were collected at 0.25h, 0.5h, 1h, 1.5h, 2h, 3h, 4h, 5h, 6h, 8h, 10h, 12h, and 24h, placed in anticoagulant tubes containing EDTA, and centrifuged at 3000r / mi...

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Abstract

The invention discloses an isradipine pharmaceutical composition with improved bioavailability. The invention firstly provides a method for improving the bioavailability of an isradipine medicament, which comprises the step: using an effective amount of isradipine medicament in combination with an antioxidant or a metal ion complexing agent. The invention still further provides a pharmaceutical composition with improved bioavailability and taking the isradipine medicament as an active ingredient, and the pharmaceutical composition contains antioxidants. The antioxidants comprise, but not limited to, free radical absorbers, metal ion chelators, oxygen scavengers, peroxide decomposers or enzyme antioxidants.

Description

technical field [0001] The invention relates to an isradipine pharmaceutical composition, in particular to an isradipine pharmaceutical composition with improved bioavailability, and belongs to the field of isradipine pharmaceutical preparations. Background technique [0002] Isradipine is a new type of dihydropyridine calcium channel blocker. It achieves the purpose of lowering blood pressure by dilating blood vessels, reducing peripheral vascular resistance, increasing coronary blood flow, and improving myocardial oxygen supply. The drug was developed by the Swiss company Sandoz, and was first introduced to the market by the British Ciba-Geigy company in February 1989. [0003] The drug isradipine is a compound known to be very effective in the treatment of hypertension and coronary heart disease, among other applications. But the water solubility of isradipine medicine is low (dissolubility is poor), causes the bioavailability of active ingredient to be low, not only th...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4439A61K45/06A61K31/375A61P9/12
CPCA61K31/375A61K31/4439A61K45/06A61K2300/00
Inventor 高永好何勇张亮亮吴宗好
Owner HEFEI HUAFANG PHARMA SCI & TECH
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