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A complex emulsion method for the preparation of metoprolol succinate sustained-release pellets

A technology of metoprolol succinate and sustained-release pellets, which is applied in the field of multi-phase emulsion method, can solve the problems of emulsion instability, inhomogeneity, easy aggregation, etc., and achieve easy control of release speed, obvious sustained-release effect, capsule smooth wall effect

Active Publication Date: 2017-12-19
邸蓉
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] At present, the domestic preparation of metoprolol succinate sustained-release pellets is basically prepared by fluidized bed coating. During the fluidized bed coating process, it is easy to make the pellets stick together, the particle size is uneven, and the thickness of the coating film is not easy to control, which makes it difficult to control the sustained release effect of the drug; the emulsified solvent diffusion method only uses a single sodium lauryl sulfate The emulsification effect is not good, the emulsion is unstable, and it is easy to agglomerate in actual operation, resulting in large and uneven product particles, and the reproducibility of drug sustained release effect is not good

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] (1) Preparation of capsule material solution: under stirring, 0.8 g of cellulose acetate and 2 g of ethyl cellulose were dissolved in 8 g of methyl acetate to form a transparent solution;

[0019] (2) Preparation of capsule core solution: under stirring, add 2 grams of metoprolol succinate powder to 10 grams of pure water, and dissolve into a transparent solution;

[0020] (3) Preparation of protective colloid solution: under stirring, add 4 grams of hydroxypropyl cellulose and 2 grams of polyvinyl alcohol to 500 grams of pure water at 80 ° C to dissolve, slowly cool down to room temperature to form a uniform and transparent solution, and set aside ;

[0021] (4) under high-speed shearing and stirring, add 1 gram of sorbitan laurate to the capsule material solution, and then slowly and evenly add the capsule core solution to make a uniform water-in-oil emulsion;

[0022] (5) Slowly add the above-mentioned water-in-oil emulsion into the protective colloid solution under...

Embodiment 2

[0026] (1) Preparation of capsule material solution: under stirring, 1.2 grams of cellulose acetate and 4 grams of ethyl cellulose were dissolved in 10 grams of methyl acetate to form a transparent solution;

[0027] (2) Preparation of capsule core solution: under stirring, add 4 grams of metoprolol succinate powder to 10 grams of pure water, and dissolve into a transparent solution;

[0028] (3) Preparation of protective colloid solution: under stirring, add 6 grams of hydroxypropyl cellulose and 4 grams of polyvinyl alcohol to 500 grams of pure water at 80 ° C to dissolve, slowly cool down to room temperature to form a uniform and transparent solution, and set aside ;

[0029] (4) under high-speed shearing and stirring, add 1 gram of sorbitan laurate to the capsule material solution, and then slowly and evenly add the capsule core solution to make a uniform water-in-oil emulsion;

[0030] (5) Slowly add the above-mentioned water-in-oil emulsion into the protective colloid s...

Embodiment 3

[0034] (1) Preparation of capsule material solution: under stirring, 1.0 g of cellulose acetate and 3 g of ethyl cellulose were dissolved in 10 g of methyl acetate to form a transparent solution;

[0035] (2) Preparation of capsule core solution: under stirring, add 3 grams of metoprolol succinate powder to 10 grams of pure water, and dissolve into a transparent solution;

[0036] (3) Preparation of protective colloid solution: under stirring, add 6 grams of hydroxypropyl cellulose and 3 grams of polyvinyl alcohol to 500 grams of pure water at 80 ° C to dissolve, slowly cool down to room temperature to form a transparent solution, and set aside;

[0037] (4) under high-speed shearing and stirring, add 1 gram of sorbitan laurate to the capsule material solution, and then slowly and evenly add the capsule core solution to make a uniform water-in-oil emulsion;

[0038] (5) Slowly add the above-mentioned water-in-oil emulsion into the protective colloid solution under stirring to ...

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Abstract

The invention relates to a multiphase emulsion method for preparing metoprolol succinate sustained-release pellets. The preparation steps are as follows: preparation of capsule material solution, preparation of capsule core solution, preparation of protective colloid solution, adding Sorbitan laurate, and then slowly and evenly add the capsule core solution to make a uniform water-in-oil emulsion, slowly add the above water-in-oil emulsion to the protective colloid solution to make a uniform multi-phase emulsion , slowly heating, filtering, vacuum drying, and sieving to make pellets. The present invention adopts the mixture of cellulose acetate and ethyl cellulose as the capsule material, so that the slow-release effect of the medicine is more obvious, and the release speed of the medicine is easier to control; sorbitan laurate is used as the emulsifier , using hydroxypropyl cellulose as a dispersant, polyvinyl alcohol as an emulsion protective colloid, and sorbitan laurate as an emulsifier, the emulsion is relatively stable, the product particles are uniform, and the surface of the capsule wall is smooth.

Description

technical field [0001] The invention relates to a complex phase emulsion method for preparing metoprolol succinate sustained-release pellets. Background technique [0002] At present, the domestic preparation of metoprolol succinate sustained-release pellets is basically prepared by the method of fluidized bed coating. This preparation method is easy to make the pellets stick together during the fluidized bed coating process, and the particle size Inhomogeneous, the thickness of the coating film is not easy to control, resulting in the slow release effect of the drug is not easy to control; the emulsification solvent diffusion method only uses a single surfactant of sodium lauryl sulfate for emulsification, the effect is not good, the emulsion is unstable, In actual operation, it is easy to agglomerate, resulting in large and uneven product particles, and the reproducibility of drug sustained release effect is not good. Contents of the invention [0003] The present inven...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/50A61K47/38A61K47/32A61K47/14A61K31/138
Inventor 邸蓉刘传荣
Owner 邸蓉
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