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Tacrolimus sustained-release tablet composition capable of rapid disintegration

A technology for a composition and a disintegrant, applied in the field of medicine, can solve problems such as technical difficulties, and achieve the effects of low labor intensity and simple operation

Active Publication Date: 2020-06-23
HANGZHOU ZHONGMEI HUADONG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] The purpose of the present invention is to provide a method for preparing a tablet pharmaceutical composition with the performance of delaying drug release, and overcome the inherent technical difficulties or product defects of existing sustained-release tablets or sustained-release capsules

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0105] Embodiment 1: preparation tablet pharmaceutical composition

[0106] Formula (dosage per 100mg tablet):

[0107] Tacrolimus: 2mg,

[0108] Ethyl cellulose: 0.6×API (indicates that the amount of EC is 0.6 times the weight of API, that is, 1.2mg, which is the meaning in this article),

[0109] Microcrystalline cellulose (water-insoluble diluent): 20mg,

[0110] Mannitol (water-soluble diluent): the balance amount makes the total amount of the pharmaceutical composition reach 100mg,

[0111] Crospovidone (disintegrant): 5mg,

[0112] Colloidal silicon dioxide (glidant): 2mg,

[0113] Magnesium stearate (lubricant): 1mg,

[0114] Aspartame (flavor): 0mg.

[0115] Preparation method:

[0116] (1) The water-insoluble diluent is crushed into a powder capable of passing through a 80-mesh sieve at least, and the remaining materials are respectively crushed into a powder capable of passing through a 65-mesh sieve at least;

[0117] (2) Add the active drug and ethyl cell...

Embodiment 2

[0120] Embodiment 2: preparation tablet pharmaceutical composition

[0121] Formula (dosage per 100mg tablet):

[0122] Tacrolimus: 1mg,

[0123] Ethyl cellulose: 0.65×API,

[0124] Microcrystalline cellulose (water-insoluble diluent): 25mg,

[0125] Mannitol (water-soluble diluent): the balance amount makes the total amount of the pharmaceutical composition reach 100mg,

[0126] Croscarmellose sodium (disintegrant): 6mg,

[0127] Colloidal silicon dioxide (glidant): 3mg,

[0128] Magnesium stearate (lubricant): 1 mg.

[0129] Preparation method:

[0130] (1) The water-insoluble diluent is crushed into a powder capable of passing through a 80-mesh sieve at least, and the remaining materials are respectively crushed into a powder capable of passing through a 65-mesh sieve at least;

[0131] (2) Add the active drug and ethyl cellulose to ethanol in an amount sufficient to dissolve the two, stir to dissolve; mix the drug solution with the pre-prepared colloidal solution;...

Embodiment 3

[0133] Embodiment 3: preparation tablet pharmaceutical composition

[0134] Formula (dosage per 100mg tablet):

[0135] Tacrolimus: 5mg,

[0136] Ethyl cellulose: 0.8×API,

[0137] Microcrystalline cellulose (water-insoluble diluent): 15mg,

[0138] Mannitol (water-soluble diluent): the balance amount makes the total amount of the pharmaceutical composition reach 100mg,

[0139] Croscarmellose sodium (disintegrant): 4mg,

[0140] Colloidal silicon dioxide (glidant): 2mg,

[0141] Magnesium stearate (lubricant): 2 mg.

[0142] Preparation method:

[0143] (1) The water-insoluble diluent is crushed into a powder capable of passing through a 80-mesh sieve at least, and the remaining materials are respectively crushed into a powder capable of passing through a 65-mesh sieve at least;

[0144] (2) Add the active drug and ethyl cellulose to ethanol in an amount sufficient to dissolve the two, stir to dissolve; mix the drug solution with the pre-prepared colloidal solution; ...

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Abstract

The invention relates to a tacrolimus slow-release tablet composition capable of being quickly disintegrated, in particular to a medicine composition which is in a tablet form. The composition includes tacrolimus, ethyecellulose, colloid, water-insoluble diluent, water-soluble diluent, disintegrating agent, fluid auxiliary and lubricating agent. The tablet can be quickly disintegrated; meanwhile,after fine particles formed after the tablet is quickly disintegrated enter the gastrointestinal tract, active medicine tacrolimus can be slowly released, and shows the unique features of quick disintegrating and slow release. Besides, the dissolution performance of the tablet under an acid condition basically has no difference from the dissolution performance of the tablet under a weak acid condition. The invention further relates to a preparing method of the tablet composition and clinical treatment application of the tablet composition, as immunosuppression, in preventing graft rejection reactions after a liver or kidney transplantation operation, and treating the graft rejection reactions which cannot be controlled by other immunosuppression drugs after the liver or kidney transplantation operation.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to tablet pharmaceutical compositions in solid form and their preparation methods. In particular, the present invention relates to a tablet capable of rapid disintegration, and the fine particles formed after the rapid disintegration of the tablet can slowly release the active drug tacrolimus after entering the gastrointestinal tract, presenting a unique rapid disintegration solution, slow release characteristics. A tablet pharmaceutical composition with immunosuppressive effect, rapid disintegration and sustained release performance can be prepared by the method of the invention. Background technique [0002] The preparation industry products are the products closest to the application of clinical patients in the field of medical technology, and the tablet is the most classic, most widely used and most convenient pharmaceutical dosage form in the preparation industry. Base. [00...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/20A61K47/38A61K31/436A61P37/06
CPCA61K9/0056A61K9/2054A61K9/2095A61K31/436A61P37/06
Inventor 韩敏刘玉艳傅立峰
Owner HANGZHOU ZHONGMEI HUADONG PHARMA
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