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Composition of ciclosporin micro-emulsion soft capsules and preparation method thereof

A cyclosporine and soft capsule technology, applied in the field of cyclosporine microemulsion soft capsules, can solve the problems of low bioavailability, liver toxicity, kidney toxicity, etc., and achieve the effect of improving bioavailability and reducing disparity

Inactive Publication Date: 2018-02-27
温州中壹技术研究院有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] When making cyclosporine microemulsified soft capsules, because it has significant hydrophobicity and is almost insoluble in water, it is rarely absorbed by the body after oral administration, and its bioavailability is very low (30% or lower), and there are It is reported that the absorption of cyclosporine microemulsion soft capsules varies greatly in different human bodies, and serious side effects such as nephrotoxicity and hepatotoxicity will appear when administered for a long time

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0017] A composition of cyclosporine microemulsion soft capsules, the composition of said cyclosporine microemulsion soft capsules by weight is as follows: 5 parts of cyclosporine A, 3 parts of phosphatidylcholine, 7 parts of surfactants, poly 36 parts of oxyethylene hydrogenated castor oil, 11 parts of Span 80, 10 parts of sorbitan, and 11 parts of medium-chain fatty acid triglycerides.

[0018] Phosphatidylcholine has a purity of 25%.

[0019] The ratio of sorbitan, polyoxyethylene hydrogenated castor oil, surfactant and cyclosporin A is 2:3:8:1.

[0020] The surfactant is an alkyl glucoside.

[0021] The present invention also proposes a preparation method of the composition of cyclosporine microemulsified soft capsules, comprising the following steps:

[0022] S1. Stir the composition, weigh 5 parts of cyclosporine A, 3 parts of phosphatidylcholine, 7 parts of absolute ethanol, 36 parts of polyoxyethylene hydrogenated castor oil, 11 parts of Span 80 and 11 parts of mediu...

Embodiment 2

[0025] A composition of cyclosporine microemulsion soft capsules, the composition of said cyclosporine microemulsion soft capsules according to weight is as follows: 9 parts of cyclosporine A, 8 parts of phosphatidylcholine, 12 parts of surfactants, poly 47 parts of oxyethylene hydrogenated castor oil, 19 parts of Span 80, 16 parts of sorbitan, and 19 parts of medium-chain fatty acid triglycerides.

[0026] Phosphatidylcholine has a purity of 46%.

[0027] The ratio of sorbitan, polyoxyethylene hydrogenated castor oil, surfactant and cyclosporin A is 2:3:8:1.

[0028] The surfactant is an alkyl glucoside.

[0029] The present invention also proposes a preparation method of the composition of cyclosporine microemulsified soft capsules, comprising the following steps:

[0030] S1. Stir the composition, weigh 9 parts of cyclosporin A, 8 parts of phosphatidylcholine, 12 parts of surfactant, 47 parts of polyoxyethylene hydrogenated castor oil, 19 parts of Span 80, 16 parts of sor...

Embodiment 3

[0033] A composition of cyclosporine microemulsion soft capsules, the composition of said cyclosporine microemulsion soft capsules by weight is as follows: 15 parts of cyclosporine A, 14 parts of phosphatidylcholine, 20 parts of surfactants, poly 59 parts of oxyethylene hydrogenated castor oil, 8021 parts of Span, 24 parts of sorbitan, and 22 parts of medium-chain fatty acid triglycerides.

[0034] Phosphatidylcholine has a purity of 79%.

[0035] The ratio of sorbitan, polyoxyethylene hydrogenated castor oil, surfactant and cyclosporin A is 2:3:8:1.

[0036] The surfactant is an alkyl glucoside.

[0037] The present invention also proposes a preparation method of the composition of cyclosporine microemulsified soft capsules, comprising the following steps:

[0038] S1. Stir the composition, weigh 15 parts of cyclosporin A, 14 parts of phosphatidylcholine, 20 parts of surfactant, 59 parts of polyoxyethylene hydrogenated castor oil, 21 parts of Span 80, 24 parts of sorbitan a...

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Abstract

The invention relates to the technical field of ciclosporin micro-emulsion soft capsules and in particular relates to a composition of ciclosporin micro-emulsion soft capsules and a preparation methodthereof. The ciclosporin micro-emulsion soft capsules comprise the following compositions in parts by weight: 5-18 parts of ciclosporin A, 3-20 parts of phosphatidylcholine, 7-26 parts of a surfactant, 36-74 parts of polyoxyethylene hydrogenated castor oil, 11-26 parts of Span 80, 10-30 parts of sorbitan and 11-28 parts of medium-chain triglycerides. According to the composition of ciclosporin micro-emulsion soft capsules disclosed by the invention, due to the addition of the surfactant, the polyoxyethylene hydrogenated castor oil and the sorbitan, dissolution of water-insoluble drugs is promoted, the bioavailability of the drugs is improved, and disparity of the bioavailability among individuals and other poor properties are reduced, so that clinical curative effects of the ciclosporin micro-emulsion soft capsules are increased, and renal toxicity, hepatotoxicity and other severe side effects in clinical application of ciclosporin are decreased.

Description

technical field [0001] The invention relates to the technical field of cyclosporin microemulsion soft capsules, in particular to a composition of cyclosporine microemulsion soft capsules and a preparation method thereof. Background technique [0002] When making cyclosporine microemulsified soft capsules, because it has significant hydrophobicity and is almost insoluble in water, it is rarely absorbed by the body after oral administration, and its bioavailability is very low (30% or lower), and there are It is reported that the absorption of cyclosporine microemulsion soft capsules varies greatly among individuals, and severe side effects such as nephrotoxicity and hepatotoxicity may occur when administered for a long time. Contents of the invention [0003] The purpose of the present invention is to solve the shortcomings of nephrotoxicity and hepatotoxicity in the prior art, and propose a composition of cyclosporine microemulsified soft capsules and a preparation method ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/48A61K38/13A61K47/44A61K47/26
CPCA61K9/4808A61K9/4858A61K38/13
Inventor 郑利方
Owner 温州中壹技术研究院有限公司
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