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Long-acting sustained-release pellet and preparation method thereof

A slow-release pellet and long-acting technology, which is applied in the preparation of the preparation, in the field of long-acting trimetazidine hydrochloride sustained-release pellets, can solve the problems of different drug content in the pellets, affecting the stability of the therapeutic effect, etc. Achieve the effect of maintaining stable blood drug concentration, low production cost, and uniform size

Inactive Publication Date: 2014-02-12
AC PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The pellets of this invention patent contain two kinds of pellets: immediate-release pellets and sustained-release pellets. Due to the inconsistency of the wrapping materials and wrapping thicknesses of the instant-release pellets and the sustained-release pellets, there are differences in bulk density and volume size, which will inevitably lead to The drug content of the pellets is different, which affects the stability of the therapeutic effect
[0009] These sustained-release preparations are convenient for patients to use to a certain extent, but due to gastric emptying and normal metabolism of the human body, the time that oral sustained-release preparations stay in the body after taking is generally less than 10h, which has also led to existing oral sustained-release preparations. Need to be taken at least twice a day to ensure adequate blood levels

Method used

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  • Long-acting sustained-release pellet and preparation method thereof
  • Long-acting sustained-release pellet and preparation method thereof
  • Long-acting sustained-release pellet and preparation method thereof

Examples

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preparation example Construction

[0154] The method for preparing the above-mentioned long-acting trimetazidine hydrochloride sustained-release pellets includes preparing a pill-containing core, directly coating the sustained-release coating layer on the pill-containing core, or first coating the isolation coating layer on the pill-containing core, and then The preparation method of coating sustained-release coating layer containing pill core comprises the following steps:

[0155] 1) Sieving: sieve the active ingredients, fillers, binders, and glidants, and set aside;

[0156] 2) Mixing: Accurately weigh the sieved active ingredients, fillers, binders, and glidants and place them in a mixer and mix them evenly;

[0157] 3) Preparation of pellets: extrude-spheronize the mixture and wetting agent to obtain a soft material, dry at 30°C to 80°C, and sieve to obtain a pellet core containing medicine.

[0158] A long-acting trimetazidine hydrochloride sustained-release oral preparation, the preparation is a disper...

Embodiment 1

[0169] A kind of trimetazidine hydrochloride sustained-release pellets, comprising the following components:

[0170] Contains pill core:

[0171] Trimetazidine Hydrochloride (active ingredient) 85.00g

[0172] Hypromellose (binder) 30.00g

[0173] Calcium hydrogen phosphate (filler) 120.00g

[0174] Microcrystalline cellulose (filler) 200.00g

[0175] Talc powder (glidant) 15.00g

[0176] Extended Release Coating:

[0177] Surelease (sustained release coating material) 15.75g

[0178] Talc powder (anti-sticking agent) 2.25g

[0179] Triethyl citrate (plasticizer) 1.13g

[0180] Acryl (porogen) 0.68g

[0181] Carbomer (gastrointestinal adhesion agent) 1.80g

[0182]The method for preparing the above-mentioned trimetazidine hydrochloride sustained-release pellets is as follows:

[0183] A. Preparation of drug-containing pellet cores:

[0184] 1) Screening: Active ingredients, fillers, binders and glidants are passed through a 40-mesh sieve for later use;

[0185] 2)...

Embodiment 2

[0193] A kind of trimetazidine hydrochloride sustained-release pellets, comprising the following components:

[0194] Contains pill core:

[0195] Trimetazidine Hydrochloride 80.00g

[0196] Povidone (Binder) 20.00g

[0197] Pregelatinized starch (filler) 280.00g

[0198] Lactose (filler) 50.00g

[0199] Talc powder (glidant) 20.0g

[0200] Isolation coating:

[0201] Polyvinyl alcohol (isolation coating material) 13.50g

[0202] Talc powder (anti-sticking agent) 6.30g

[0203] Dimethyl phthalate (plasticizer) 2.70g

[0204] Extended Release Coating:

[0205] Surelease (sustained release coating material) 27.00g

[0206] Magnesium stearate (anti-adhesive agent) 2.25g

[0207] Polycarboxyethylene Pentaerythritol Ester (Gastrointestinal Adhesive) 13.50g

[0208] The method for preparing the above-mentioned trimetazidine hydrochloride sustained-release pellets is as follows:

[0209] A. Preparation of drug-containing pellet cores:

[0210] 1) Screening: Active ingred...

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Abstract

The invention discloses a long-acting sustained-release pellet and a preparation method thereof. The long-acting trimetazidine hydrochloride sustained-release pellet comprises a drug-containing core and a sustained-release coating layer from inside to outside sequentially, wherein an optional isolation coating layer is arranged between the drug-containing core and the sustained-release coating layer; the isolation coating layer accounts for 0-15 percent of the mass of the drug-containing core, and the sustained-release coating layer accounts for 5-30 percent of the mass of the drug-containing core; a gastrointestinal adhesive is contained in the sustained-release coating layer. According to the trimetazidine hydrochloride sustained-release pellet, the prescription is meticulously designed, the drug-containing core is uniformly coated by utilizing the sustained-release coating material, so that slow and uniform drug release of the drug-containing core can be maintained, the active component releasing speed can be reduced, the time for reaching the peak can be postponed, the pellet can be constantly and stably released in 24 hours, the blood concentration stability can be maintained, and the phenomenon of insufficient blood concentration in morning ischemia can be avoided. The administration frequency can be reduced to once a day, and the compliance of patients can be improved.

Description

technical field [0001] The invention relates to a sustained-release preparation, in particular to a long-acting trimetazidine hydrochloride sustained-release pellet with a sustained-release time of up to 24 hours. The invention also relates to a preparation method of the preparation. Background technique [0002] Trimetazidine Dihydrochloride (TMZ), as a new class of effective drugs for the prevention and treatment of angina pectoris, has been widely used in many countries and regions, and has a good effect on the treatment of angina pectoris. The ordinary tablet of trimetazidine hydrochloride entered my country in 2000, and now the product has been listed in the National Essential Drug List. [0003] Trimetazidine hydrochloride is 1-(2,3,4-trimethylphenyl)piperazine dihydrochloride, with a molecular weight of 339.3 and a molecular formula of C 14 h 22 N 2 o 3· 2HCl, very soluble in water. The absorption rate of trimetazidine hydrochloride in the body is fast, and the ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K9/22A61K9/52A61K31/495A61P9/10
CPCA61K9/5026A61K9/5036A61K9/5047A61K9/5073A61K31/495A61P9/10
Inventor 刘锋周伟杰赖树挺
Owner AC PHARMA CO LTD
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