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Tacrolimus pharmaceutical composition and preparation method thereof

A technology for tacrolimus and composition, applied in the field of tacrolimus pharmaceutical composition and its preparation, can solve the problems of volatile ethanol, hardening and cracking of capsule shell, etc. less demanding effects

Active Publication Date: 2015-08-19
FUJIAN KERUI PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In the patent CN100515413C, ethanol is used as a solvent to prepare tacrolimus capsules, which improves the safety of the finished product and the production process, but high-concentration ethanol is volatile, and there are certain requirements for operating time and ambient temperature during the scale-up production process
At the same time, during the long-term storage process, the ethanol in the capsule will absorb water and cause the capsule shell to harden and crack, so the residual amount of ethanol in the finished product must be strictly controlled

Method used

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  • Tacrolimus pharmaceutical composition and preparation method thereof
  • Tacrolimus pharmaceutical composition and preparation method thereof

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preparation example Construction

[0027] The preparation method of the tacrolimus pharmaceutical composition is as follows: dissolving tacrolimus in ethanol, adding hypromellose to make it uniformly dispersed, then adding purified water, and stirring to make the hypromellose completely After swelling, add croscarmellose sodium and lactose in sequence, stir evenly, granulate, sieve, and then dry under reduced pressure at 40°C and pressure>0.09MPa for 24 hours to obtain the product.

[0028] In order to make the content of the present invention easier to understand, the technical solutions of the present invention will be further described below in conjunction with specific embodiments, but the present invention is not limited thereto.

Embodiment 1

[0030] Tacrolimus 0.5 g,

[0031] Ethanol 0.5 g,

[0032] Hypromellose 0.5 g,

[0033] Croscarmellose Sodium 1.5 g,

[0034] Lactose 50 g,

[0035] Purified water 0.5 g.

[0036] The preparation method of the tacrolimus pharmaceutical composition is as follows: dissolving tacrolimus in ethanol, adding hypromellose to make it uniformly dispersed, then adding purified water, and stirring to make the hypromellose completely After swelling, add croscarmellose sodium and lactose in turn, stir evenly, granulate, pass through a 60-mesh sieve, and place in a vacuum oven at 40°C and pressure>0.09MPa to dry under reduced pressure for 24 hours to obtain the product.

Embodiment 2

[0038] Tacrolimus 1 g,

[0039] Ethanol 3 g,

[0040] Hypromellose 5 g,

[0041] Croscarmellose Sodium 2.5 g,

[0042] Lactose 100 g,

[0043] Purified water 15 g,

[0044] Adequate flow aid.

[0045] The preparation method of the tacrolimus capsule is as follows: dissolving tacrolimus in ethanol, adding hypromellose to make it uniformly dispersed, adding purified water, stirring, and completely swelling the hypromellose , add croscarmellose sodium and lactose in turn, stir evenly, granulate, pass through a 60-mesh sieve, place in a vacuum oven at 40°C with a pressure >0.09MPa and dry under reduced pressure for 24 hours, pass through a 40-mesh sieve for granulation, An appropriate amount of glidant is added, and the capsule is filled to obtain the product.

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Abstract

The invention discloses a tacrolimus pharmaceutical composition and a preparation method thereof. The tacrolimus pharmaceutical composition is prepared from the following raw materials in parts by weight: 0.5-1 part of tacrolimus, 0.5-3 parts of ethanol, 0.5-10 parts of hydroxypropyl methylcellulose, 0.5-5 parts of croscarmellose sodium, 50-100 parts of lactose, and 0.5-15 parts of purified water. The security risk and the unsteady quality problem easily occurring due to use of a toxic organic solvent or high-concentration ethanol in original preparation of a tacrolimus preparation are solved; and the tacrolimus pharmaceutical composition is simple in preparation process, low in equipment operation requirement and easy in industrial production.

Description

technical field [0001] The invention belongs to the field of medicines, and in particular relates to a tacrolimus pharmaceutical composition and a preparation method thereof. Background technique [0002] Tacrolimus (tacrolimus, FK506) is a white crystal or crystalline powder, insoluble in water, easily soluble in ethanol, is a new type of potent immunosuppressive macrolide antibiotics. Clinically, it is mainly used for anti-transplant rejection, and can also be used for the treatment of autoimmune diseases such as systemic lupus erythematosus and rheumatoid arthritis. [0003] At present, in the existing tacrolimus capsules, tacrolimus is made into a solid dispersion, and then other pharmaceutical excipients are added to make capsules. Patent JP62277321 is to dissolve tacrolimus in a certain amount of ethanol to obtain a clear solution, then add hydroxypropylmethylcellulose and mix evenly, immediately add a certain amount of dichloromethane and stir evenly, so that the hyd...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/48A61K9/20A61K31/436A61K47/38A61P37/06A61P37/02
Inventor 王娟魏宗有肖丽华连云阳
Owner FUJIAN KERUI PHARMA
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