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Bevantolol hydrochloride sustained release preparation

A technology of bevanolol hydrochloride and preparation, applied in the field of pharmaceutical preparations, can solve the problems of short plasma half-life and the like

Active Publication Date: 2009-11-18
北京化药科创医药科技发展有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The existing oral dosage forms are ordinary tablets or capsules, but because of the short plasma half-life of bevanolol in the body, it needs to be taken several times a day to better maintain its blood concentration

Method used

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  • Bevantolol hydrochloride sustained release preparation
  • Bevantolol hydrochloride sustained release preparation
  • Bevantolol hydrochloride sustained release preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1     Embodiment 2    Embodiment 3

[0037]Bevanolol hydrochloride 100 50 100

[0038] Xanthan gum 102.9 60 133.3

[0039] HPMC K4M 17.1 15 16.7

[0040] Stearic acid 15 24 9

[0041] Microcrystalline cellulose 62 145 39

[0042] Magnesium stearate 3 6 2

[0043] Preparation process: the above-mentioned slow-release matrix xanthan gum, HPMC K 4M Disperse and dissolve with a sufficient amount of water respectively, add the prescribed amount of bevanolol hydrochloride and stearic acid into the aqueous solution of the sustained-release matrix, stir well, and form a uniform solution or dispersion, which is used as a spray-drying material liquid, and then sprayed Spray granulation is carried out in the dryer, the inlet temperature of the spray dryer is 125°C, the outlet temperature is 90°C, the feed rate is 8ml / min, the atomizer pressure is 125kpa, the particles are collected in the cyclone separator, and the average of the obtained particles is The particle size is 36.7 μm, for use;

[0044] The prepared bevano...

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Abstract

The invention relates to a bevantolol hydrochloride sustained release preparation, which contains an effective dose of raw medicaments of bevantolol hydrochloride, a sustained release matrix and other excipients, wherein the component of the sustained release matrix is the combination of HPMC K4M and xanthan gum. The bevantolol hydrochloride sustained release preparation is mainly prepared by preparing the raw medicaments into sustained release particles first and then preparing the particles into various required dosage forms. The bevantolol hydrochloride sustained release preparation can be released evenly and slowly within 24 hours.

Description

technical field [0001] The invention relates to a bevanolol hydrochloride sustained-release preparation and a preparation method thereof, belonging to the field of pharmaceutical preparations. Background technique [0002] β-blockers are the first-line drugs for the treatment of hypertension. Long-term treatment of hypertension with non-selective β-receptor blockers can cause dyslipidemia. Among selective β-receptor blockers, antihypertensive drugs that have little effect on blood lipids will receive more and more attention. Bevantolol (bevantolol) is a relatively new fat-soluble selective β1-receptor blocker developed by the Warner-Lambert Company of the United States. It has no intrinsic sympathomimetic activity because it can block α-receptors and calcium ions channels, and thus have a mild vasodilator effect. The bioavailability of bevanolol is 60%, the peak time is about 1-2 hours, and the plasma half-life is about 1.5 hours, and its metabolite 4-hydroxyl bevanolol h...

Claims

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Application Information

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IPC IPC(8): A61K31/138A61K47/36A61K47/38A61K9/16A61P9/12
Inventor 关屹闫冬
Owner 北京化药科创医药科技发展有限公司
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