Cyclosporin A dispersion solid and its preparation method

A solid dispersion, cyclosporine technology, applied in the directions of cyclic peptide components, bulk delivery, pill delivery, etc., can solve the problems of inability to prepare, low solubility of cyclosporine A, almost insoluble, etc.

Inactive Publication Date: 2005-01-05
FUDAN UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Cyclosporine A has very little solubility in water, is almost insoluble, and has low bioavailability, so it cannot be directly prepared into qualified oral preparations from raw materials

Method used

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  • Cyclosporin A dispersion solid and its preparation method
  • Cyclosporin A dispersion solid and its preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Take 1g of cyclosporin A and 8g of polyoxyethylene (40) stearate and put them in a beaker, add 15ml of absolute ethanol, stir to dissolve completely. In a 40°C water bath, evaporate the solvent 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 (at room temperature), take it out, grind it, and pass it through an 80-mesh sieve to obtain the product. The solid dispersion of the invention has a cumulative dissolution rate of 94.40±1.51% (n=6) in 60 minutes in vitro.

Embodiment 2

[0034]Take 1g of cyclosporin A and 8g of povidone K-29 / 32 in a beaker, add 20ml of absolute ethanol, stir to dissolve completely. In a 40°C water bath, evaporate the solvent 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 (50°C), take it out, grind it, and pass it through an 80-mesh sieve to obtain the product. The solid dispersion of the invention has an in vitro cumulative dissolution rate of 55.79±11.92% (n=6) within 60 minutes.

Embodiment 3

[0036] Take 1 g of cyclosporine A and 10 g of poloxamer 407 and put them in a beaker, add 25 ml of absolute ethanol, stir to dissolve completely. In a 40°C water bath, evaporate the solvent 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 (40°C), take it out, grind it, and pass it through an 80-mesh sieve to obtain the product. The solid dispersion of the invention has a 60-minute cumulative dissolution rate in vitro of 91.83±5.19% (n=6).

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Abstract

A dispersing solid (capsule, tablet, particle, suppository and dripping pill) of cyclosporin A is prepared from cyclosporin A and carrier by solvent method, solvent fusion method, etc. It has high solubility of easy absorption.

Description

technical field [0001] The invention belongs to the field of chemical pharmacy, and in particular relates to a compound cyclosporin A solid dispersion and a preparation method thereof. technical background [0002] Cyclosporin A (English name: Cyclosporine A, Cyclosporin A) its chemical name is cyclo[[(E)-(2S,3R,4R)-3-hydroxy-4-methyl-2-(methylamino)-6 -octenyl]-L-2aminobutyryl-N-methylglycyl-N-methyl-L-leucyl-L-valyl-N-methyl-L-leucyl-L -alanyl-D-alanyl-N-methyl-L-leucyl-N-methyl-L-leucyl-N-methyl-L-valyl], formula C 62 h 111 N 11 o 12 ; Molecular weight: 1202.63, with the following chemical structure, [0003] [0004] Cyclosporin A is a lipophilic cyclic polypeptide extracted from the fungus (Tolypocladium Inflatum Gams) in 1772. It consists of 11 amino acids and is insoluble in water with a melting point of 148-151°C. In 1976, it was discovered that cyclosporin A has immunosuppressive effect and is a powerful immunosuppressant. It was used in kidney transplant p...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/02A61K9/14A61K9/16A61K9/20A61K38/13A61P37/02A61P37/06
Inventor 柳晨裴元英林富源冯明发
Owner FUDAN UNIV
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