Tacrolimus solid dispersion and its preparing method

A technology of solid dispersion and tacrolimus, which is used in medical preparations containing active ingredients, pharmaceutical formulas, organic active ingredients, etc.

Inactive Publication Date: 2006-08-23
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There is no self-developed oral solid dosage form of tacrolimus in China, and the price of imported oral capsules (1mg/capsule) is as...

Method used

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  • Tacrolimus solid dispersion and its preparing method
  • Tacrolimus solid dispersion and its preparing method
  • Tacrolimus solid dispersion and its preparing method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Take 1g of tacrolimus and 5g of povidone K-29 / 32 into a beaker, add 25mL of absolute ethanol and 25mL of dichloromethane, stir to completely dissolve. In a water bath at 50°C, evaporate with a rotary evaporator for 25 minutes to evaporate the solvent. Transfer to a vacuum drying oven to continue drying for 24 hours (room temperature), take it out, grind, and pass through an 80-mesh sieve to get it. The cumulative in vitro dissolution percentage of the solid dispersion in 45 minutes of the invention is 92.48±1.53% (n=6).

Embodiment 2

[0032] Take 1g of tacrolimus and 10g of povidone K-29 / 32 into a beaker, add 25mL of absolute ethanol and 25mL of dichloromethane, stir to completely dissolve. In a 50°C water bath, evaporate with a rotary evaporator for 25 minutes, and evaporate the solvent to dryness. Transfer to a vacuum drying oven to continue drying for 24 hours (room temperature), take it out, grind, and pass through an 80-mesh sieve to get it. The cumulative in vitro dissolution percentage of the solid dispersion in 45 minutes of the invention is 104.01±5.86% (n=6).

Embodiment 3

[0034]Take 1g of tacrolimus and 5g of hypromellose E3 into a beaker, add 25mL of absolute ethanol and 25mL of dichloromethane, stir to completely dissolve. In a 50°C water bath, evaporate with a rotary evaporator for 25 minutes, and evaporate the solvent to dryness. Transfer to a vacuum drying oven to continue drying for 24 hours (room temperature), take it out, grind, and pass through an 80-mesh sieve to get it. The cumulative in vitro dissolution percentage of the solid dispersion in 45 minutes of the invention is 103.20±3.28% (n=6).

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PUM

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Abstract

The present invention belongs to the field of chemical medicine preparing technology, and is especially solid Tacrolimus dispersion as one kind of immunodepressant and its preparation process. The present invention adopts Tacrolimus as active medicine component, and prepares the solid Tacrolimus dispersion through adding carrier material, solvent process, solvent-fusing process and freeze drying process, and the solid Tacrolimus dispersion is further prepared into capasule. The present invention has raised medicine solubility, 5-500 times raised solubility in water compared with Tacrolimus, raised leaching speed and increased absorption of the medicine inside body.

Description

Technical field [0001] The invention belongs to the field of chemical pharmacy, and specifically relates to a compound tacrolimus solid dispersion and a preparation method thereof. technical background [0002] Tacrolimus (English name: Tacrolimus) its chemical name is [3S-[3R * [E(1S * , 3S * , 4S * )], 4S * , 5R * , 8S * , 9E * , 12R * , 14R * , 15S * , 16R * , 18S * , 19S * , 26aR * ]]-5,6,8,11,12,13,14,15,16,17,18,19,24,25,26a-hexa-decylhydro-5,19-dihydroxy-3-[2- (4-Hydroxy-3-methoxycyclohexyl)-1-methylvinyl]-14,16-dimethoxy-4,10,12,18-tetramethyl8-(2-propenyl)-15 ,19-Epoxy-3H-pyrido[2,1-c][1,4]oxaazacyclotriyne-1,7,20,21(4H,23H)-tetraketone. Molecular formula C 44 H 69 NO 12 , Molecular weight: 804.03, with the following chemical structure: [0003] [0004] Tacrolimus is a 23-ring macrolide antibiotic (erythromycin family) isolated from the fermentation product of a strain of Streptomyces in the soil of Tsukuba region, Japan in 1979. It has poor water solubility and is ea...

Claims

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Application Information

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IPC IPC(8): A61K31/7048A61K9/48A61P37/06
Inventor 顾希平裴元英
Owner FUDAN UNIV
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