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Carvedilol solid self-emulsifying sustained release tablets and preparing method thereof

A self-emulsifying, sustained-release tablet technology, applied in the field of medicine, can solve the problems of low solubility of carvedilol, serious liver first-pass effect, poor bioavailability, etc., and achieve good application prospects, poor bioavailability, and equipment undemanding effects

Inactive Publication Date: 2017-08-18
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Aiming at the problems of low solubility of carvedilol, poor bioavailability, and severe first-pass effect of the liver, the present invention designs a solid self-emulsifying sustained-release tablet of carvedilol. The present invention provides a drug-loaded hollow mesoporous A method for preparing carvedilol solid self-emulsifying sustained-release tablets with silicon oxide as a solid carrier, the specific preparation process is as follows:

Method used

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  • Carvedilol solid self-emulsifying sustained release tablets and preparing method thereof
  • Carvedilol solid self-emulsifying sustained release tablets and preparing method thereof
  • Carvedilol solid self-emulsifying sustained release tablets and preparing method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0022] Example 1: Preparation of hollow mesoporous silica

[0023] (1) Accurately weigh 0.9g of cetyltrimethylammonium bromide, dissolve it in 180ml / 300ml ethanol aqueous solution, stir magnetically until it is completely dissolved, add 8ml of ammonia water, stir magnetically for one hour, mix well, and then add positive Tetraethyl silicate was added dropwise at a rate of 1ml / min, stirred and reacted for 6h, and a white emulsion was obtained. Filter and wash to obtain mesoporous silica containing cetyltrimethylammonium bromide.

[0024] (2) Take 0.5 g of the above-mentioned mesoporous silica and put it into 150 ml of deionized water, etch at a high temperature of 90 ° C for 72 hours, filter and wash to obtain hollow mesoporous silica containing cetyltrimethylammonium bromide, take 0.5 g of the above hollow mesoporous silica was refluxed in the acidic alcohol solution for 3 hours to remove cetyltrimethylammonium bromide, refluxed twice, filtered and washed to obtain hollow mes...

Embodiment 2

[0025] Example 2: Preparation of hollow mesoporous silica

[0026] This example is basically the same as Example 1, except that the amount of cetyltrimethylammonium bromide is 0.7g, the amount of ammonia water is 4ml, the reaction is stirred for 12h, and 0.3g of mesoporous silica is taken into High-temperature etching in 200ml deionized water, the temperature is 60°C, and the etching time is 48h.

Embodiment 3

[0027] Embodiment 3: Preparation of carvedilol solid self-emulsifying granules

[0028] According to the ratio of 3:3:4 oil phase: emulsifier: co-emulsifier, measure a total of 100 microliters of liquid self-emulsification, vortex and oscillate evenly, and use drug-loaded hollow mesoporous silica to absorb liquid self-emulsification , to obtain carvedilol solid self-emulsifying granules.

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Abstract

The invention discloses a method for preparing carvedilol solid self-emulsifying sustained release tablets. The method comprises the steps of synthesizing hollow mesoporous silica with a uniform particles size and an obvious hollow structure; conducting liquid self-emulsifying with the drug-loaded hollow mesoporous silica as a solid carrier, so that carvedilol solid self-emulsifying particles are obtained; finally, evenly mixing the carvedilol solid self-emulsifying particles with proper auxiliary materials for wet granulation, and conducting tabletting to obtain the carvedilol solid self-emulsifying sustained release tablets. The preparing process is simple, operation is easy, and the cost is low. The prepared carvedilol solid self-emulsifying sustained release tablets have an obvious slow release effect and broad application prospects.

Description

technical field [0001] The invention relates to a carvedilol solid self-emulsifying sustained-release tablet and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Carvedilol (CAR) is a new type of vasodilator drug, clinically used to treat mild to moderate essential hypertension, ischemic heart disease and congestive heart failure. Carvedilol has strong lipophilicity, poor dissolution rate, and first-pass effect in the liver, which lead to low bioavailability of carvedilol. In order to overcome these shortcomings, it is necessary to improve its bioavailability by means of pharmacy, such as carvedilol cyclodextrin inclusion complex, carvedilol physical dispersion, carvedilol self-microemulsification and other preparation means. Therefore, it is of great significance to develop methods that can improve the bioavailability of drugs. [0003] Hollow mesoporous silica is a silica nanoparticle with a core-shell structure wi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/22A61K31/403A61K47/04A61P9/12A61P9/04A61P9/10
CPCA61K9/0002A61K9/2009A61K9/2054A61K9/2077A61K31/403
Inventor 王柏李田田
Owner CHINA PHARM UNIV
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