Microemulsion pre-concentrate composition containing cyclosporine and pharmaceutical formulation including a microemulsion pre-concentrate composition containing cyclosporine

摘要

"COMPOSITION OF PRECONCENTRATE OF MICROEMULSION CONTAINING CYCLOSPORIN AND PHARMACEUTICAL FORMULATION INCLUDING A COMPOSITION OF PRECONCENTRATE OF MICROEMULSION CONTAINING CYCLOSPORIN". The present invention relates to a microemulsion pre-concentrate composition that includes (1) cyclosporine as an active component; (2) alkyl ester of polycarboxylic acid and / or carboxylic acid ester of polyols as a lipophilic solvent; (3) oil; and (4) surfactant. The composition according to the present invention is characterized by the fact that it dissolves in an external phase such as water, artificial gastric fluid and artificial intestinal fluid, controlling the mixing ratio of its components to obtain the microemulsion form of the internal phase with a diameter of 10nm or less. The composition according to the present invention can be formulated in the dosage form of a soft capsule, a hard capsule sealed with a gelatin strip on the conjugate part, or a liquid preparation for oral administration. Especially, in the case where the composition according to the present invention is formulated in a soft capsule, the resulting capsule does not present disadvantages of the prior art such as the reactivity of the hydrophilic solvent with the gelatin envelope of the soft capsule and the volatility of the hydrophilic solvent. Unlike existing patents that use a hydrophilic solvent as an essential component of their compositions, the present invention does not use any hydrophilic solvent.