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Claims for Patent: 5,643,607

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Claims for Patent: 5,643,607

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-gun, JP)
Assignee: Takeda Chemical Industries, Ltd. (Osaka, JP)
Application Number:08/458,679
Patent Claims: 1. A microcapsule exhibiting zero order release of luteinizing hormone-releasing hormone (LH-RH) analog 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 the LH-RH analog, 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.

4. A microcapsule according to claim 1, wherein the LH-RH analog is water-soluble and has a molecular weight of 1,000 or more.

5. A process for preparing a microcapsule exhibiting zero order release of luteinizing hormone-releasing hormone (LH-RH) analog for a period of at least two months upon administration, which comprises preparing a water-in-oil emulsion comprising an inner aqueous phase free from a drug retaining substance containing 35 to 60% (W/W) of the LH-RH analog, 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 in-water drying or phase-separation.

6. A process according to claim 5, wherein the water-in-oil emulsion is dispersed in an aqueous phase and the resulting water/oil/water ternary emulsion is subjected to in-water drying.

7. A process according to claim 5, wherein the water-in-oil emulsion is dispersed in an aqueous phase containing polyvinyl alcohol as an emulsifying agent.

8. A process according to claim 5, wherein the LH-RH analog is water-soluble and has a molecular weight of 1,000 or more.

9. A process according to claim 5, wherein the LH-RH analog is (pyr)Glu-His-Trp-Ser-Tyr-D-Leu-Leu-Arg-ProNHC.sub.2 H.sub.5.
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