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Pharmaceutical composition containing tacrolimus and preparation methods thereof

a tacrolimus and composition technology, applied in the field of pharmaceutical technology, can solve the problems of insufficient absorption rate in the body, reduced drug bioavailability, incomplete dissolution of tacrolimus, etc., and achieve the effect of shortening operation procedures and reducing hazards to operators and the environmen

Inactive Publication Date: 2017-03-16
SOLIPHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The present invention is about a new way to make tacrolimus, which is a drug used to prevent rejection in transplant patients. The new method uses a different solvent that is safer and easier to handle. The experiments showed that adding a certain substance called crystallization inhibitor hydroxypropyl methylcellulose to the tacrolimus can prevent the drug from crystallizing in the body, which could cause low blood levels and ineffectiveness. Overall, this invention makes it safer and more effective to make tacrolimus for medical use.

Problems solved by technology

When orally administered, tacrolimus in formulations can't be rapidly released, which leads to insufficient absorption rate in the body and thus causes lower drug bioavailability.
The tacrolimus products prepared by the methods disclosed in other documents as discussed above have the problems of crystallization of tacrolimus in the dissolution medium or in vivo causing incomplete dissolution of tacrolimus and low drug plasma concentration and low drug efficacy.

Method used

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  • Pharmaceutical composition containing tacrolimus and preparation methods thereof

Examples

Experimental program
Comparison scheme
Effect test

preparation example 1

[0030]The capsule formulations containing tacrolimus were prepared by reference to the preparation process in example 11 of the patent document CN1820759A. The process is specified as follows:

[0031]Place 1 g of tacrolimus and 5 g of hydroxypropyl methylcellulose (E3) in a beaker, add 25 ml of anhydrous ethanol and 25 ml of dichloromethane, stir to dissolve completely, rotary evaporate the solvents for 25 minutes in a 50° C. water bath until dryness, freeze and dry the mixture for 24 h, take the solids out of the drier, grind, pass the solids through a 80-mesh sieve and obtain tacrolimus solid dispersion.

[0032]Encapsulate the tacrolimus solid dispersion with the strength of 1 mg of tacrolimus.

example 1

[0033]A formula of tacrolimus capsules is shown in the following table:

Percentage ofNamePer capsule (mg)component (%)Tacrolimus11.7Lactose1.62.7Hydroxypropyl methylcellulose11.7Cross-linked sodium0.40.7carboxymethylcelluloseLactose (Additional)5591.7Magnesium stearate11.7(Additional)Ethanol2.5N / ATotal60100.0

[0034]Preparation procedures are as follows:

[0035](1) preparing solution: weighing 24 g of tacrolimus and dissolving the tacrolimus in 60 g of ethanol;

[0036](2) preparing premixed excipients: mixing 24 g of hydroxypropyl methylcellulose, 4.8 g of cross-linked sodium carboxymethylcellulose and 38.4 g of lactose homogeneously using a wet granulating machine;

[0037](3) preparing soft materials: mixing the solution obtained in procedure (1) and premixed excipients obtained in procedure (2) using a wet granulating machine and obtaining soft materials;

[0038](4) drying the soft materials in a vacuum oven at 50° C.;

[0039](5) granulating by forcing the soft materials obtained in procedure ...

example 2

[0040]A formula of tacrolimus capsules is shown in the following table:

Percentage ofNamePer capsule (mg)component (%)Tacrolimus11.7Lactose0.61.0Hydroxypropyl methylcellulose2.54.2Cross-linked sodium0.40.7CarboxymethylcelluloseLactose (additional)54.590.8Magnesium stearate11.7(additional)Ethanol2.5N / ATotal60100.0

[0041]Preparation procedures of the capsules are the same as those of Example 1.

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Abstract

Disclosed are a pharmaceutical composition comprising tacrolimus and a preparation method thereof.

Description

FIELD OF THE INVENTION[0001]The invention relates to the field of pharmaceuticals technology. Specifically, the present invention relates to a pharmaceutical composition containing tacrolimus and methods for preparing the composition.BACKGROUND[0002]Tacrolimus, also named FK506, is a macrolide pharmaceutical compound with the molecular formula C44H69NO12 H2O and molecular weight 882.05, having the chemical structural formula shown below:[0003]Tacrolimus has expanded indications. It was initially used as graft rejection inhibitor for organ transplant patients. Later it was developed as ointment formulations for treating atopic dermatitis, and was further used as therapeutic agents for other inflammatory skin diseases. Currently, the dosage forms of tacrolimus are capsules, extended release capsules, ointment and so on.[0004]The solubility of tacrolimus in water is extremely low and is only 1 to 2 μg / ml. When orally administered, tacrolimus in formulations can't be rapidly released, w...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K47/38A61K47/26A61K47/12A61K31/436
CPCA61K47/26A61K31/436A61K47/38A61K47/12A61K9/48A61K9/1652A61P37/06
Inventor SHENG, XIAOXIATANG, YONG
Owner SOLIPHARMA
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