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Trimetazidine dihydrochloride sustained release tablet and preparation method thereof

A technology of trimetazidine hydrochloride and sustained-release tablets, which can be applied to pharmaceutical formulations, medical preparations without active ingredients, and medical preparations containing active ingredients, etc. problems, to achieve the effect of simple steps, improved compliance, and process stability

Active Publication Date: 2012-09-19
QILU PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This method increases the residue of organic solvents in the tablet, which is not environmentally friendly and increases the cost, and the early release is faster

Method used

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  • Trimetazidine dihydrochloride sustained release tablet and preparation method thereof
  • Trimetazidine dihydrochloride sustained release tablet and preparation method thereof
  • Trimetazidine dihydrochloride sustained release tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] Example 1 The prescription composition of trimetazidine hydrochloride sustained-release tablets is:

[0053] Raw materials

g / 100 pieces

Trimetazidine hydrochloride

3.5

Kollidon SR

7.0

Ethyl cellulose

1.75

Microcrystalline Cellulose PH101

5.1625

Magnesium stearate

0.0875

[0054] Preparation method: mix the prescription amount of trimetazidine hydrochloride with microcrystalline cellulose PH101, then mix it with Kollidon SR and ethyl cellulose uniformly, add magnesium stearate and mix and press tablets, the hardness measured is 9-10kg / mm 2 , The release degree is shown in Table 5 and figure 1 Shown.

[0055] The stability of the trimetazidine hydrochloride sustained-release tablets obtained in Example 1 was studied. It was investigated under the conditions of (40±2)°C and relative humidity (75±5)%, 0 days, 1, 2, 3 And the stability of 6 months, the experiment proves that the sustained-release tablet prepared by using the mixture of Kollidon SR an...

Embodiment 2

[0058] Example 2 The prescription composition of trimetazidine hydrochloride sustained-release tablets is:

[0059] Raw materials

[0060] The preparation method: the prescription amount of trimetazidine hydrochloride is mixed with lactose, starch and ethyl cellulose, granulated with an aqueous solution of povidone, dried, and granulated. The prepared granules are mixed with Kollidon SR evenly, magnesium stearate is added and mixed, and then compressed, the hardness measured is 9-10kg / mm 2 , The measured release rate is shown in Table 2.

[0061] Table 2 Investigation of release

[0062] Time (hour)

[0063] By investigating the release profile of the trimetazidine hydrochloride sustained-release tablet obtained in Example 2, it was found that although the water-soluble filler would accelerate the release of the drug, the sustained-release time still meets the requirements.

Embodiment 3

[0064] Example 3 The prescription composition of trimetazidine hydrochloride sustained-release tablets is:

[0065] Raw materials

[0066] The preparation method: mix the prescription amount of trimetazidine hydrochloride with microcrystalline cellulose and ethyl cellulose uniformly, then granulate with a hydroxypropyl cellulose aqueous solution, dry, and sizing. The prepared granules are mixed with Kollidon SR evenly, magnesium stearate is added and mixed, and then compressed, the hardness measured is 9-10kg / mm 2 .

[0067] The sample obtained in Example 3 was placed in two different media with a pH of 1.2 hydrochloric acid buffer solution and water, and the release rate was measured as shown in Table 3 and figure 2 Shown.

[0068] Table 3 Investigation of release rate in different media

[0069] Time (hour)

[0070] By investigating the release curve of the trimetazidine hydrochloride sustained-release tablets obtained in Example 3, it is found that the pH environment has a...

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Abstract

The invention belongs to the field of medicinal preparations and particularly relates to a trimetazidine dihydrochloride sustained release tablet and a preparation method thereof. The trimetazidine dihydrochloride sustained release tablet takes polyvinyl acetate and mixture of povidone mixture and ethyl cellulose as sustained-release matrix materials and also contains a filling agent, a lubricating agent and other accessories. The release degree of the trimetazidine dihydrochloride sustained release tablet is not influenced by the granularity of raw material; the mixed sustained-release matrix material can be used for controlling the initial burst release of the trimetazidine dihydrochloride at earlier stage; the in vitro release of the sustained release tablet is not influenced by a pH environment; and meanwhile, the administration times of the medicament is reduced to two times from three times of general tablets, so that the administration adaptability of patients is improved. According to the preparation method of the trimetazidine dihydrochloride sustained release tablet, direct tabletting or granulation tabletting through a water-soluble solvent wet method can be adopted; and the preparation process is simple, and thus the trimetazidine dihydrochloride sustained release tablet can be continuously and stably produced in batch.

Description

Technical field [0001] The invention belongs to the field of pharmaceutical preparations, and specifically relates to a trimetazidine hydrochloride sustained-release tablet and a preparation method thereof. Background technique [0002] The chemical name of Trimetazidine is 1-(2,3,4-trimethoxybenzyl)piperazine. It is the first 3-ketoacyl-CoA thiolase inhibitor (3-KAT). It can inhibit the oxidation of fatty acids (FFA), stimulate the oxidation of glucose, and have a protective effect against myocardial ischemic cells to a certain extent. In recent years, trimetazidine hydrochloride has been widely used in the preventive treatment of angina pectoris and the auxiliary symptomatic treatment of vertigo and tinnitus. [0003] Trimetazidine is rapidly absorbed after oral administration, and its half-life is relatively short [t 1 / 2 =(6.0±1.4)h], the concentration of trimetazidine can be stable within 24h, and the concentration can remain relatively unchanged during the administration peri...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/22A61K31/495A61K47/38A61K47/32A61P9/10A61P1/08A61P27/16
Inventor 王晶翼王婧璨杨清敏李长军李颖张明会
Owner QILU PHARMA
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