Self-micro emulsifying soft capsule of cyclosporine A and method of producing the same

Abstract

The invention relates to a self micro emulsifying soft capsule with cyclosporin A and the preparing method. The preparing method comprises the following steps: heating and dissolving cyclosporin A, absolute ethyl alcohol, methyl ethylene glycol, polyoxyethylene hydrogenated castor oil, span 80 and medium chain fatty acid triglyceride in the homogenized emulsified pan; making soft capsule; and getting the product by treating the surface with alcohol and drying. The disintegrated self micro emulsifying soft capsule is dispersed into the transparent microemulsion, and the determined result indicates that the grain diameter of microemulsion is uniform. The invention has the easy getting solvent, the low price and the simple technology, which is fit for the large scale industry production, overcomes the low bioavailability of cyclosporin A , reduces the enormous difference of bioavailability among the individual, improves the digestion of the water-insoluble medicine, and improves bioavailability of the medicine.

Description

technical field [0001] The invention relates to a self-microemulsifying soft capsule of cyclosporine A and a preparation method thereof, in particular to a self-microemulsifying soft capsule containing cyclosporine A. Background technique [0002] Cyclosporine A (CrclosporineA, CyA) is a metabolite of fungi, a high-level peptide compound composed of 11 amino acids, and is a white needle-like crystal. Because it is significantly hydrophobic and almost insoluble in water, it is rarely absorbed by the body after oral administration, and its bioavailability is very low (30% or less). And it has been reported that the absorption varies greatly between human bodies by 4-60%, and severe side effects such as nephrotoxicity and hepatotoxicity will appear when administered for a long time. [0003] Cyclosporin A is a new type of high-efficiency immunosuppressant, which was first developed by the Swiss Sandoz Pharmaceutical Company. In 1983, the US Food and Drug Administration (FDA) a...

AI Technical Summary

Problems solved by technology

Although some improvements have been made in the formulation process of these two patents and some other patents, they all have similar defects, that is, there are many components in the formulation, which will cause complicated preparation process and corresponding increase in product cost.