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Claims for Patent: 4,917,893

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Claims for Patent: 4,917,893

Title: Prolonged release microcapsules
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:07/103,117
Patent Claims: 1. A spherical microcapsule for an injectable preparation, having an average diameter of 2-200 .mu.m, the spherical microcapsule comprising particles of a mixture of a biologically active polypeptide and a drug-retaining substance selected from the group consisting of gelatin, albumin, pectin and agar, the weight ratio of the drug-retaining substance to the biologically active polypeptide being in the range of about 2.5/1 through about 1/1, the particles being dispersed in a spherical microcapsule matrix composed of a lactic acid-glycolic acid polymer having a monomer ratio within the range of about 78/22 to 50/50 and an average molecular weight within the range of about 5,000-100,000.

2. The microcapsule according to claim 1, wherein the biologically active polypetide is luteninizing hormone releasing hormone or its derivative.

3. The microcapsule according to claim 2, wherein the luteinizing hormone releasing hormone or its derivative is a polypeptide of the formula:

wherein R.sub.1 is His, Tyr, Trp or p-NH.sub.2 -Phe; R.sub.2 is Tyr or Phe; R.sub.3 is Gly or D-amino acid residue which may have a protective group; R.sub.4 is Leu, Ile or Nle and R.sub.5 is Gly-NH-R.sub.6 or NHR.sub.6, wherein R.sub.6 is hydrogen or lower alkyl which may be substituted by hydroxyl.

4. The microcapsule according to claim 3, wherein R.sub.1 is His, R.sub.2 Tyr, R.sub.3 is D-Leu, R.sub.4 is Leu and R.sub.5 is NHCH.sub.2 CH.sub.3.

5. The microcapsule according to claim 3, wherein R.sub.1 is His, R.sub.2 is Tyr, R.sub.3 is D-Ala protected with naphthyl, R.sub.4 is Leu and R.sub.5 is Gly-NH.sub.2.

6. The microcapsule according to claim 1, wherein the drug retaining substance is gelatin.

7. The microcapsule according to claim 1, wherein the lactic acid-glycolic acid polymer is a copolymer having a monomer molar ratio of 78/22.

8. An injectable preparation comprising a therapeutically effective amount of spherical microcapsules according to claim 1 and a pharmaceutically acceptable vehicle, the preparation providing release of the polypeptide to a patient over a period of at least two weeks after administration.
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