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Last Updated: November 22, 2024

Claims for Patent: 5,476,663

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Summary for Patent: 5,476,663

Title:	Prolonged release microcapsule
Abstract:	A microcapsule produced by preparing a water-in-oil emulsion comprising an inner aqueous layer containing said water-soluble drug and a drug retaining substance therefor and an oil layer containing a polymer substance, then thickening or solidifying said inner aqueous layer to a viscosity of not lower than about 5000 centiposes and finally subjecting the resulting emulsion to in water drying gives prolonged release of water-soluble drug.
Inventor(s):	Okada; Hiroaki (Osaka, JP), Ogawa; Yasuaki (Osaka, JP), Yashiki; Takatsuka (Hyogo, JP)
Assignee:	Takeda Chemical Industries, Ltd. (Osaka, JP)
Application Number:	08/228,452
Patent Claims:	1. A prolonged release microcapsule for injection, which comprises particles containing a water-soluble drug, the particles being dispersed in a spherical microcapsule matrix composed of a copolymer of lactic acid and glycolic acid having a comonomer ratio within the range of about 100/0 to 50/50 and an average molecular weight within the range of about 5,000 to 200,000, the spherical microcapsule matrix having an average diameter of 2 to 200 .mu.m, and an excipient selected from the group consisting of mannitol, sorbitol, lactose and glucose, which particles are produced by in-water drying. 2. A microcapsule as claimed in claim 1, wherein the water-soluble drug is a biologically active polypeptide. 3. A microcapsule as claimed in claim 1, wherein the water-soluble drug is a non-polypeptidic drug. 4. A microcapsule as claimed in claim 1, wherein the excipient is mannitol. 5. An injectable preparation comprising a therapeutically effective amount of a prolonged release microcapsule which comprises particles containing a water-soluble drug, the particles being dispersed in a spherical microcapsule matrix composed of a copolymer of lactic acid and glycolic acid having a comonomer ratio within the range of about 100/0 to 50/50 and an average molecular weight within the range of about 5,000 to 200,000, the spherical microcapsule matrix having an average diameter of 2 to 200 .mu.m, and an excipient selected from the group consisting of mannitol, sorbitol, lactose and glucose, which particles are produced by in-water drying. 6. An injectable preparation as claimed in claim 5, wherein the water-soluble drug is a biologically active polypeptide. 7. An injectable preparation as claimed in claim 5, wherein the water-soluble drug is a non-polypeptidic drug. 8. An injectable preparation as claimed in claim 5, wherein the excipient is mannitol.

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