Isradipine controlled-release tablet and preparation method and application thereof

A technology of isradipine and controlled-release tablets, which is applied in the directions of pharmaceutical formulations, medical preparations containing active ingredients, and pill delivery to achieve the effect of delaying the release time.

Active Publication Date: 2012-09-26
CHONGQING CONQUER PHARML
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] In order to solve the problem of time-selected release of drugs for the treatment of cardiovascular diseases, the invention provides a time-delayed controlled-release tablet that combines a tablet core sustained-release matrix with a controlled-release coating; the existence of the controlled-release coating not only Causes drug release time lag and can affect the release kinetics of the inner chip

Method used

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  • Isradipine controlled-release tablet and preparation method and application thereof
  • Isradipine controlled-release tablet and preparation method and application thereof
  • Isradipine controlled-release tablet and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] The preparation of embodiment 1 isradipine controlled release tablet

[0021] The prescription for the controlled-release tablet core is: isradipine 20mg, phosphatidylcholine 40mg, HPMC K15M 40mg, EC 100cp30mg, PVP K3020mg; the prescription for the controlled-release coating is: HPMC K15M 37.5mg, EC 0.01Pa·s 112.5mg, PVP K3060mg, MCC 90mg. Mix isradipine, phosphatidylcholine, ethyl cellulose, hydroxypropyl methyl cellulose and polyvinylpyrrolidine evenly, wet granulate, dry, add magnesium stearate and press into tablets to make a controlled-release tablet core; The hydroxypropyl methylcellulose, ethylcellulose, polyvinylpyrrolidone and microcrystalline cellulose in the controlled-release coating raw materials are wet-granulated, dried, and mixed with magnesium stearate to obtain a coating mixture; Half of the mixture is put into the die, the controlled-release tablet core is placed in the center of the die, and the other half of the coating mixture is put into the tabl...

Embodiment 2

[0022] The in vitro release comparison of embodiment 2 isradipine controlled-release tablet and controlled-release tablet core

[0023] Get the isradipine controlled-release tablet and controlled-release tablet core that embodiment provides, the device that passes through Chinese Pharmacopoeia 2010 edition dissolution test method first method, with distilled water 900mL as dissolution medium, rotating speed is 10Or min -1 , the temperature is (37±0.5) ℃, operate according to the law, take 5mL of the solution at 1, 2, 3, 4, 5, 6, 8, 10, 12 and 14h, filter, and add 5mL of water immediately. Part of the sample solution was diluted with distilled water, and then the ultraviolet absorbance was measured at 236nm, and the drug release percentage at different time points was calculated by the standard curve.

[0024] The most critical index in delayed-release controlled-release tablets is the release time lag (T lag ), the drug release time lag can be determined by the following meth...

Embodiment 3

[0028] The influence of embodiment 3 different controlled-release coatings on the release behavior of isradipine controlled-release tablets

[0029] The controlled-release tablet core prescription of the isradipine controlled-release tablet provided in 1 was fixed, and the influence of the type, specification, dosage and compression pressure of the polymer in the controlled-release coating on the drug release behavior was separately investigated.

[0030] The dosage of hydroxypropyl methylcellulose (HPMC): according to the preparation method of isradipine controlled-release tablets, the coating layers containing 5%, 7.5%, 10%, 12.5%, 15%, 17.5%, and 20% HPMCK4M were prepared respectively. Ladipine controlled-release tablets and determination of drug release curve;

[0031] Hydroxypropylmethylcellulose (HPMC) viscosity: according to the preparation method of isradipine controlled-release tablets, HPMC (E50, K4M, K15M, K100M) with different viscosities were used to prepare israd...

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Abstract

The invention discloses an isradipine controlled-release tablet. The controlled-release tablet consists of an isradipine-containing controlled-release tablet core and a controlled-release coat. The invention provides an isradipine controlled-release tablet capable of delaying the release time, and solves the problem of obvious time dependence of the drug administration for cardiovascular diseases; and meanwhile, phosphatidylcholine is added to the tablet, thus the controlled-release tablet has a certain treatment effect on diabetic nephropathy.

Description

technical field [0001] The invention relates to a pharmaceutical preparation, more specifically to an isradipine controlled-release tablet, a preparation method and an application thereof. technical background [0002] Isradipine (also known as: isradipine, iradipine), chemical name: isopropylmethyl(±)-4-(4-benzofurazanyl)-1,4-dihydro-2,6 -Dimethyl-3,6-pyridinedicarboxylate. It is a new type of dihydropyridine calcium channel blocker. Like other dihydropyridine drugs, it can effectively and selectively inhibit the contraction caused by depolarization by blocking the influx of transmembrane calcium ions. And in the myocardium and function on vascular smooth muscle. This product has a strong vasodilator effect, but no heart inhibitory effect, and almost does not cause reflex tachycardia. Clinical and animal experiments have proved that the drug has obvious antihypertensive and anti-atherosclerotic effects. By maintaining or restoring the blood flow under the left ventricula...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/28A61K9/36A61K31/4439A61P3/10A61P13/12
Inventor 梅勇罗磊何远东马贵勇姜艳红杨莉贺代琼李小林
Owner CHONGQING CONQUER PHARML
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