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Slow release tacrolimus pharmaceutical composition

A composition and drug technology, 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

[0109] Embodiment 1: preparation tablet pharmaceutical composition

[0110] Formula (dosage per 100mg tablet):

[0111] Tacrolimus: 2mg,

[0112] 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),

[0113] Microcrystalline cellulose (water-insoluble diluent): 20mg,

[0114] Mannitol (water-soluble diluent): the balance amount makes the total amount of the pharmaceutical composition reach 100mg,

[0115] Crospovidone (disintegrant): 5mg,

[0116] Colloidal silicon dioxide (glidant): 2mg,

[0117] Magnesium stearate (lubricant): 1mg,

[0118] Aspartame (flavor): 0 mg.

[0119] Preparation method:

[0120] (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;

[0121] (2) Add the active drug and ethyl cel...

Embodiment 2

[0124] Embodiment 2: preparation tablet pharmaceutical composition

[0125] Formula (dosage per 100mg tablet):

[0126] Tacrolimus: 1mg,

[0127] Ethyl cellulose: 0.65×API,

[0128] Microcrystalline cellulose (water-insoluble diluent): 25mg,

[0129] Mannitol (water-soluble diluent): the balance amount makes the total amount of the pharmaceutical composition reach 100mg,

[0130] Croscarmellose sodium (disintegrant): 6mg,

[0131] Colloidal silicon dioxide (glidant): 3mg,

[0132] Magnesium stearate (lubricant): 1 mg.

[0133] Preparation method:

[0134] (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;

[0135] (2) Add the active drug and ethyl cellulose to ethanol that is sufficient to dissolve the two, and stir to dissolve; add a water-insoluble diluent to the resulting solution, stir to...

Embodiment 3

[0137] Embodiment 3: preparation tablet pharmaceutical composition

[0138] Formula (dosage per 100mg tablet):

[0139] Tacrolimus: 5mg,

[0140] Ethyl cellulose: 0.8×API,

[0141]Microcrystalline cellulose (water-insoluble diluent): 15mg,

[0142] Mannitol (water-soluble diluent): the balance amount makes the total amount of the pharmaceutical composition reach 100mg,

[0143] Croscarmellose sodium (disintegrant): 4mg,

[0144] Colloidal silicon dioxide (glidant): 2mg,

[0145] Magnesium stearate (lubricant): 2 mg.

[0146] Preparation method:

[0147] (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;

[0148] (2) Add the active drug and ethyl cellulose to ethanol in an amount sufficient to dissolve the two, and stir to dissolve; add a water-insoluble diluent to the resulting solution, stir...

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Abstract

The present invention relates to slow release tacrolimus pharmaceutical composition. It specifically relates to a pharmaceutical composition in the form of a tablet, which comprises: active drug, ethyl cellulose, water-insoluble diluent, water-soluble diluent, disintegrant, glidant and lubricant. The tablet of the present invention can disintegrate rapidly, and the fine particles formed after the rapid disintegration of the tablet can slowly release the active drug tacrolimus after entering the gastrointestinal tract, showing unique characteristics of rapid disintegration and sustained release. The present invention also relates to the preparation method of the pharmaceutical composition, and their immunosuppressive effect for preventing graft rejection after liver or kidney transplantation, and for treating transplantation uncontrollable by other immunosuppressive drugs after liver or kidney transplantation. Application in the clinical treatment of objection rejection.

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): A61K9/22A61K47/38A61K31/436A61P37/06
CPCA61K9/0056A61K9/2054A61K9/2095A61K31/436A61P37/06
Inventor 周屹峰韩敏蒋颖燕
Owner HANGZHOU ZHONGMEI HUADONG PHARMA
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