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A kind of solid pharmaceutical composition containing trimetazidine or its salt and its preparation method

A composition and drug technology, applied in the field of trimetazidine solid pharmaceutical compositions, can solve the problems of poor particle fluidity, unfavorable patients, increase in impurities and the like

Active Publication Date: 2021-07-02
JIANGSU HENGRUI MEDICINE CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, we have found in actual research that due to the strong hygroscopicity of polyoxyethylene, using polyoxyethylene alone as the sustained-release framework material will also cause poor particle fluidity due to the hygroscopicity of the framework material, resulting in content uniformity of the finished tablet. Unqualified, in addition, the hygroscopicity of polyoxyethylene will make the stability of sustained-release tablets worse, and the impurities will increase rapidly during storage, and too many impurities will cause increased side effects of the drug, which is not conducive to providing patients with safer drugs. drug

Method used

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  • A kind of solid pharmaceutical composition containing trimetazidine or its salt and its preparation method
  • A kind of solid pharmaceutical composition containing trimetazidine or its salt and its preparation method
  • A kind of solid pharmaceutical composition containing trimetazidine or its salt and its preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] With trimetazidine hydrochloride, calcium hydrogen phosphate, povidone K30, according to the ratio in table 1, adopt the high-speed shearing wet granulation process, carry out granulation with purified water, dry processing then, dry granule (moisture is less than 2 %) for dry sizing, adding the prescribed amount of sustained-release matrix material and lubricant, mixing with a rotary blender, and compressing the obtained blended granules into tablets.

[0043] Table 1

[0044]

[0045] After the end of the blending, the blended granules with different prescriptions were taken to investigate the fluidity of the granules. During the tableting process, adjust the tableting parameters to ensure consistent tableting pressure, and investigate the hardness of the tablets made of granules prepared with different prescriptions under the same pressure conditions. After the tablet compression was completed, 10 tablets were randomly selected from the tablets of each prescripti...

Embodiment 2

[0051] Trimetazidine hydrochloride, calcium hydrogen phosphate, povidone K30, according to the ratio in table 3, adopt the high-speed shearing wet granulation process, carry out granulation with purified water, dry processing then, dry granule (moisture is less than 2%) ) for dry sizing, adding the prescribed amount of slow-release matrix material and lubricant, and mixing with a rotary blender. The resulting blended granules were compressed into tablets.

[0052] table 3

[0053]

[0054]

[0055] It can be seen from the measurement results of the angle of repose of the blended granules of each prescription in Table 3 that the preparation of the present invention is used, and the ratio of hydroxypropyl methylcellulose to polyoxyethylene in the prescription is within the range of 1:3 and 1:0.3 At the same time, the mixed granules of the prescription all showed excellent fluidity, and the content uniformity of the final tablet was all small, all of which could reach the ...

Embodiment 3

[0066] Trimetazidine hydrochloride, calcium hydrogen phosphate, povidone K30, according to the ratio in table 6, adopt the high-speed shearing wet granulation process, carry out granulation with purified water, dry processing then, dry granule (moisture is less than 2%) ) for dry sizing, adding the prescribed amount of slow-release matrix material and lubricant, and mixing with a rotary blender. The resulting blended granules were compressed into tablets. Wherein prescription C adopts the preparation method and prescription in the patent CN1166408C.

[0067] Table 6

[0068]

[0069] During the tablet compression process, prescription C and prescription D were respectively compressed into tablets with different hardness (see Table 7 for details), and the dissolution rates of tablets with different hardness were measured according to the aforementioned dissolution test method.

[0070] Table 7

[0071]

[0072] The trimetazidine hydrochloride sustained-release tablet o...

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Abstract

The invention relates to a solid pharmaceutical composition containing trimetazidine or a salt thereof and a preparation method thereof. Specifically, the solid pharmaceutical composition of the present invention contains trimetazidine or a pharmaceutically acceptable salt or a solvate thereof as an active ingredient, and two or more sustained-release matrix materials. The solid pharmaceutical composition of the present invention has the characteristics of gentle release over a long period of time.

Description

technical field [0001] The invention relates to a trimetazidine solid pharmaceutical composition capable of slow and stable release and a preparation method thereof. The composition is used for preventive treatment of angina pectoris attacks. Background technique [0002] Trimetazidine, whose chemical name is 1-(2,3,4-trimethoxybenzyl)piperazine, has the following structure: [0003] [0004] Normal myocardial energy (ATP) supply 60% to 70% from free fatty acid β oxidation, 20% to 25% from glucose oxidation, 5% to 10% from glycolysis. The oxygen consumption of free fatty acid oxidation to produce the same amount of ATP is higher than that of glucose oxidation, and high levels of free fatty acid oxidation can significantly inhibit the rate of glucose oxidation. During myocardial ischemia, the sympathetic nerve is excited, and the level of catecholamines increases, which in turn leads to an increase in the level of free fatty acids in the blood; the oxidation of free fatty...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/20A61K31/495A61K47/38A61K47/10A61P9/10
CPCA61K9/2031A61K9/2054A61K9/2095A61K31/495A61P9/10
Inventor 郭辰宁潘凯刘凯莫志荣
Owner JIANGSU HENGRUI MEDICINE CO LTD
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