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Preparation method of trimetazidine hydrochloride slow release microcapsules

A technology of trimetazidine hydrochloride and sustained-release microcapsules, which is applied in the field of preparation of trimetazidine hydrochloride sustained-release microcapsules, can solve the problems of high frequency of administration, short duration of drug effect, low bioavailability, etc. Achieve the effects of improved bioavailability, long duration of drug effect, and simple preparation steps

Inactive Publication Date: 2016-07-20
袁春华
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The technical problem to be solved by the present invention: for trimetazidine hydrochloride is very soluble in water, the duration of drug effect after use is short, the frequency of administration is high, the bioavailability is low, and the amount of lubricant used in the preparation process is too much The dissolution of the agent is slow, and if it is too little, the solution will stick to the disadvantages of the pressing process. A method is provided to mix chitosan, starch, sodium carbonate, etc., mix with isoamylase, adjust the pH with hydrochloric acid solution, filter to obtain the filtrate, squeeze Crushed and sieved after pressing, mixed with polyglutamic acid and distilled water to obtain a mixed solution, then mixed with dietary fiber and sodium alginate to obtain a wall material solution, mixed with a mixed solution prepared from trimetazidine hydrochloride and mannitol solution , spray calcium chloride solution, leave standstill, dry, wash, freeze-dry and make the method for trimetazidine hydrochloride sustained-release microcapsules

Method used

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Examples

Experimental program
Comparison scheme
Effect test

example 1

[0016] First, in parts by weight, take 30 parts of chitosan, 25 parts of starch, 35 parts of deionized water and 15 parts of sodium carbonate, put them into a container, heat the container to 50°C, stir at 150r / min for 40min, and then Add starch mass 18% isoamylase to the container, adjust the pH to 5.5 with a mass fraction of 15% hydrochloric acid solution, continue to stir for 1 hour, filter, and collect the filtrate; then put the above-mentioned filtrate into an extruder, Squeeze down for 10 minutes, put the extruded product into a pulverizer and crush it, pass through a 200-mesh sieve, mix the sieved particles and polyglutamic acid at a mass ratio of 3:1, add distilled water to the mixture, and stir until the mixture is completely dissolved , stop adding distilled water to obtain a mixed solution; then pour the above-mentioned mixed solution into the reaction kettle, and then add dietary fiber such as starch and sodium alginate with a starch quality of 10% to the above-ment...

example 2

[0019] First, in parts by weight, take 33 parts of chitosan, 28 parts of starch, 38 parts of deionized water and 18 parts of sodium carbonate, put them into a container, heat the container to 55°C, stir at 150r / min for 45min, and then Add 21% isoamylase of starch mass into the container, adjust the pH to 5.5 with a hydrochloric acid solution with a mass fraction of 15%, continue to stir for 2 hours and then filter to collect the filtrate; then put the above-mentioned filtrate into an extruder, Squeeze down for 13 minutes, put the extruded product into a pulverizer and crush it, pass through a 200-mesh sieve, mix the sieved particles and polyglutamic acid at a mass ratio of 3:1, add distilled water to the mixture, and stir until the mixture is completely dissolved , stop adding distilled water to obtain a mixed solution; then pour the above-mentioned mixed solution into the reaction kettle, and then add dietary fiber such as starch and sodium alginate with a starch quality of 13...

example 3

[0022]First, in parts by weight, take 35 parts of chitosan, 30 parts of starch, 40 parts of deionized water and 20 parts of sodium carbonate, put them into a container, heat the container to 60°C, stir at 150r / min for 50min, and then Add starch mass 24% isoamylase to the container, adjust the pH to 5.5 with a mass fraction of 15% hydrochloric acid solution, continue to stir for 2 hours, filter, and collect the filtrate; then put the above-mentioned filtrate into an extruder, Squeeze down for 15 minutes, put the extruded product into a pulverizer and crush it, pass through a 200-mesh sieve, mix the sieved particles and polyglutamic acid at a mass ratio of 3:1, add distilled water to the mixture, and stir until the mixture is completely dissolved , stop adding distilled water to obtain a mixed solution; then pour the above-mentioned mixed solution into the reaction kettle, and then add dietary fiber such as starch and sodium alginate with a starch quality of 13% to the above-ment...

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Abstract

The invention discloses a preparation method of trimetazidine hydrochloride slow release microcapsules, and belongs to the technical field of medicine preparation. The preparation method comprises the following steps: mixing chitosan, starches and sodium carbonate to obtain a mixture, mixing the mixture with isoamylase, adjusting the pH with an acidic solution, filtering to obtain filtrates, squeezing the filtrates, smashing and screening the filtrates, mixing the filtrates with polyglutamic acid and distilled water to obtain a mixed solution, mixing the mixed solution with dietary fibers and sodium alga acid, discharging a material which is a wall material solution, mixing the wall material solution with a mixed solution prepared from trimetazidine hydrochloride and a mannitol solution, spraying a calcium chloride solution, and stewing, drying, washing and freeze-drying products to obtain the trimetazidine hydrochloride slow release microcapsules. The preparation method has the benefits that the preparation steps are simple, and the solutions difficultly get sticky in the preparation process; the solubility of the obtained product in water is reduced by 23.3 percent or above; after being used, the trimetazidine hydrochloride slow release microcapsules can last for a long time, the administration frequency is reduced by 15 to 20 percent, and the biological utilization rate is increased by 20 to 30 percent.

Description

technical field [0001] The invention relates to a preparation method of trimetazidine hydrochloride sustained-release microcapsules, belonging to the technical field of medicine preparation. Background technique [0002] Preparation of Trimetazidine Hydrochloride Sustained-release Tablets Trimetazidine Hydrochloride and auxiliary materials were sieved separately. Weigh the prescribed amount of trimetazidine hydrochloride, lactose, dextrin, microcrystalline cellulose and hypromellose K4M, and sieve to mix them evenly. Add an appropriate amount of 2% polyvinylpyrrolidone ethanol solution to the fine powder of raw materials and auxiliary materials, and mix well to make a soft material. Sieve to make wet granules, dry them, sieve them into 18-mesh sieves, add micro-powder silica gel, and press into tablets. Trimetazidine hydrochloride is an anti-ischemic drug. It selectively inhibits 3-ketoacyl-CoA thiolase, reduces free fatty acid metabolism and increases glucose oxidation, ...

Claims

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Application Information

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IPC IPC(8): A61K9/50A61K47/36A61K31/495A61P9/10A61P1/08A61P27/16
CPCA61K9/5036A61K9/5089A61K31/495
Inventor 袁春华盛海丰宋奇
Owner 袁春华
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