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 with inactive ingredients, and medical preparations containing active ingredients, etc. The production process is complex, the drug release stability is greatly affected, and the PEO gel strength is not high. It can solve the problems of adjuvant adhesion equipment, excellent quality stability, and suitable for process production.

Inactive Publication Date: 2013-01-23
AC PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0013] 2. Polyethylene oxide (Poly Ethylene Oxide, PEO) is used as the skeleton of the tablet core to control the release, but the strength of the gel formed by PEO is not high, which has a great impact on the stability of drug release; at the same time, the glass transition temperature of PEO is 65°C-67°C , the thermal stability is not good, and the drying temperature should not be too high, which may cause problems in the tablet preparation process. During the storage process, due to oxidation, PEO will also generate free radicals, which will lead to the degradation of excipients and active compounds, which is not conducive to Long-term storage of products
[0014] 3. The production process of sustained-release pellets or sustained-release film-coated tablets is relatively complicated, requiring expensive production equipment, large investment and high cost

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
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Effect test

Embodiment 1

[0053] A trimetazidine hydrochloride sustained-release tablet, comprising the following components (calculated in 1000 tablets):

[0054]

[0055] The method for preparing the above-mentioned trimetazidine hydrochloride sustained-release tablet comprises the following steps:

[0056] (1), grinding and sieving: grind trimetazidine hydrochloride into fine powder, get trimetazidine hydrochloride fine powder, hydroxypropyl methylcellulose (12000mPa s-21000mPa s), povidone, phosphoric acid Calcium hydrogen is passed through a 40-mesh sieve, and micronized silica gel and stearic acid are passed through an 80-mesh sieve;

[0057] (2), Weighing: Accurately weigh 35.00g of trimetazidine hydrochloride, 48.00g of hydroxypropyl methylcellulose (12000mPa s-21000mPa s), 12.00g of povidone, 103.60g of calcium hydrogen phosphate, and micronized silica gel 0.40g, stearic acid 2.00g, Opadry (film coating material is hypromellose) 10.00g for subsequent use;

[0058] (3), mixing: mix the wei...

Embodiment 2

[0064] A trimetazidine hydrochloride sustained-release tablet, comprising the following components (calculated in 1000 tablets):

[0065]

[0066] The method for preparing the above-mentioned trimetazidine hydrochloride sustained-release tablet comprises the following steps:

[0067] (1), grinding and sieving: grind trimetazidine hydrochloride into fine powder, get trimetazidine hydrochloride fine powder, hypromellose (80000mPa s-120000mPa s), povidone, micro Crystalline cellulose is passed through a 40-mesh sieve, and micronized silica gel and magnesium stearate are passed through an 80-mesh sieve;

[0068] (2), weighing: Accurately weigh 35.00g of trimetazidine hydrochloride, 40.00g of hydroxypropylmethylcellulose (80000mPa s-120000mPa s), 16.00g of povidone, 107.60g of microcrystalline cellulose, micropowder 0.40g of silica gel, 2.00g of magnesium stearate, 10.00g of Opadry (film coating material is hypromellose) for later use;

[0069] (3), mixing: put the weighed tri...

Embodiment 3

[0075] A trimetazidine hydrochloride sustained-release tablet, comprising the following components (calculated in 1000 tablets):

[0076]

[0077]

[0078] The method for preparing the above-mentioned trimetazidine hydrochloride sustained-release tablet comprises the following steps:

[0079] (1), grinding and sieving: grind trimetazidine hydrochloride into fine powder, take trimetazidine hydrochloride fine powder, glyceryl behenate, hydroxypropyl methylcellulose, povidone, pregelatinized starch Cross 40 mesh sieves, get micropowder silica gel and magnesium stearate and cross 80 mesh sieves;

[0080] (2), weighing: Accurately weigh 35.00g of trimetazidine hydrochloride, 30.00g of glyceryl behenate, 16.00g of hydroxypropyl methylcellulose (3000mPa s-5600mPa s), 10.00g of povidone, Pregelatinized starch 117.60g, micropowder silica gel 0.40g, magnesium stearate 2.00g. Opadry (film coating material is hydroxypropyl methylcellulose) 10.00g spare;

[0081] (3), mixing: the ...

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Abstract

The invention discloses a trimetazidine dihydrochloride sustained-release tablet and a preparation method thereof. The trimetazidine dihydrochloride sustained-release tablet comprises the following constituents in percentage by mass: 5-60% of trimetazidine dihydrochloride, 10-25% of sustained-release framework material, 1-8% of adhesive, 20-80% of filler, 0.1-5% of glidant and 0.2-3% of lubricant. According to the trimetazidine dihydrochloride sustained-release tablet, medicine can be slowly and uniformly released by adding the sustained-release framework material, so as to achieve regulation and control for a release speed, reduce the peak-valley ratio of the medicine, improve the efficacy, reduce the toxic and side effects of the medicine, reduce daily medicine-taking times and enhance the compliance of the patient on the medicine. The preparation method of the trimetazidine dihydrochloride sustained-release tablet disclosed by the invention is simple in process, does not need specially process production equipment, and is low in cost and good for batch amplification and industrialized production for products.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a novel sustained-release tablet of trimetazidine hydrochloride, a novel antiangina pectoris drug, and a preparation method thereof. Background technique [0002] Trimetazidine hydrochloride is 1-(2,3,4-trimethylphenyl)piperazine dihydrochloride, molecular formula C 14 h 22 N 2 o 3 · 2HCl, its molecular weight is 339.3, easily soluble in water. [0003] Trimetazidine hydrochloride is different from traditional therapeutic drugs such as nitrate esters, β-receptor blockers and calcium ion antagonists in chemical structure and pharmacological action. It does not depend on the rate of the heart or the drop of blood pressure. It has anti-epinephrine, norepinephrine and vasopressin effects, can reduce vascular resistance, increase coronary blood flow and peripheral blood flow, and promote myocardial metabolism and myocardial energy production. At the same time, it can re...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/22A61K9/28A61K31/495A61K47/38A61K47/36A61K47/26A61K47/14A61K47/32A61P9/10
Inventor 刘锋王世刚曹付春周伟杰莫华丝
Owner AC PHARMA CO LTD
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