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

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 ...

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