Cyclosporin-containing microemulsion preconcentrate composition

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...

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514937, 514951, A61K 31545

Patent

active

060280670

ABSTRACT:
The present invention relates to a microemulsion preconcentrate composition comprising (1) cyclosporin 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 in that it dissolves in an external phase such as water, artificial gastric fluid and artificial intestinal fluid by controlling the mixing ratio of the components thereby to get the microemulsion form of inner phase diameter of 100 nm or below. The composition according to the present invention can be formulated as the dosage form of a soft capsule, a hard capsule sealed with a gelatin banding at the conjugated portion, or an oral liquid preparation for oral administration. Especially, if the cyclosporin microemulsion preconcentrate comprising cyclosporin, oil, lipophilic solvent and surfactant is formulated in a soft capsule according to the present invention, the resultant capsule removes the disadvantages of the prior arts showing the reactivity of hydrophilic solvent with gelatin shell of soft capsule and the volatility of hydrophilic solvent wherein the hydrophilic solvent was essential component in the composition according to the existing patents.

REFERENCES:
patent: 4388307 (1983-06-01), Cavanak
patent: 5342625 (1994-08-01), Hauer et al.
patent: 5583105 (1996-12-01), Kovacs et al.
patent: 5589455 (1996-12-01), Woo
patent: 5603951 (1997-02-01), Woo
patent: 5639474 (1997-06-01), Woo
patent: 5639724 (1997-06-01), Cavanak
patent: 5891846 (1999-04-01), Ishida et al.

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