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|Title:||Prolonged release microcapsules|
|Abstract:||This invention provides a microcapsule designed for zero order release of a physiologically active polypeptide over a period of at least two months, which is produced by preparing a water-in-oil emulsion comprising an inner aqueous layer containing about 20 to 70% (w/w) of said polypeptide and an oil layer containing a copolymer or homopolymer having a weight-average molecular weight of 7,000 to 30,000, wherein the composition ratio of lactic acid/glycolic acid in the copolymer or homopolymer is 80/10 to 100/0, and then subjecting said water-in oil emulsion to microencapsulation.|
|Inventor(s):||Okada; Hiroaki (Suita, JP), Inoue; Yayoi (Kyoto, JP), Ogawa; Yasuaki (Otokuni, JP)|
|Assignee:||Takeda Chemical Industries, Ltd. (Osaka, JP)|
1. A microcapsule exhibiting zero order release of (pyr)Glu-His-Trp-Ser-Tyr-D-Leu-Leu-Arg-ProNHC.sub.2 H.sub.5 for a period of at least two months upon administration, which is
produced by preparing a water-in-oil emulsion comprising an inner aqueous phase free from a drug retaining substance containing 35 to 60% (W/W) of (pyr)Glu-His-Trp-Ser-Tyr-D-Leu-Leu-Arg-ProNHC.sub.2 H.sub.5, and an oil phase containing a homopolymer of
lactic acid having a weight-average molecular weight of 14,100 to 18,200 and a dispersion degree (ratio of weight-average molecular weight to number-average molecular weight) of 1.5 to 2.5, as the material for forming an outer wall of the microcapsule
and then subjecting said water-in-oil emulsion to microencapsulation.
2. A microcapsule according to claim 1, which exhibits zero order release for a period of at least three months upon administration.
3. A microcapsule according to claim 1, wherein the concentration of homopolymer in the oil phase is from 2 to 60% by weight.