EP0442671A2
Expired / Lapsed
EP
⏱️ 0.0 years remaining
Prolonged release microcapsules
Assignee: Takeda Pharmaceutical Co Ltd
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Filing: 1991-02-11
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Granted: —
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Expires: 2011-02-11
Abstract
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, the molar composition ratio of lactic acid/glycolic acid being 80/20 to 100/0, subjecting said water-in oil emulsion to microencapsulation.
Inventors
- 👤 Hiroaki Okada
- 👤 Yayoi Inoue
- 👤 Yasuaki 77-42 Koaza-Tanita Ogawa
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-10-25 22:17
CPC Classifications
A; A61; A61K; A61K38/00; A61K38/04; A61K38/06; A61K38/066; A61K38/08; A61K38/09; A61K9/00; A61K9/14; A61K9/16; A61K9/1605; A61K9/1629; A61K9/1641; A61K9/1647
Claims Analysis
Total Claims: 23
Claim 1
Independent Claim
82 words
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 phase containing an about 20 to 70% (w/w) of said polypeptide and an oil phase containing a copolymer or homopolymer having a weight-average molecular weight of 7,000 to 30,000, the molar composition ratio of lactic acid/glycolic acid being 80/20 to 100/0, and then subjecting said water-in oil emulsion to microencapsulation.
Claim 2
Dependent Claim
28 words
The microcapsule according to claim 1, wherein said water-in-oil emulsion is dispersed in an aqueous phase and then subjecting the resulting water/oil/water ternary emulsion to an in-water drying.
Claim 3
Dependent Claim
28 words
The microcapsule according to claim 1, wherein said polypeptide comprises having amino acid residues of two or more and a molecular weight of about 200 to about 100,000.
Claim 4
Dependent Claim
32 words
The microcapsule according to claim 1, wherein said polypeptide is lutenizing hormone-releasing hormone (LH-RH) and an analogous substance of LH-RH which is water-soluble and has a molecular weight of 1,000 or more.
Claim 5
Dependent Claim
12 words
The microcapsule according to claim 1, wherein said polypeptide is (pyr)Glu-His-Trp-Ser-Tyr-D-Leu-Leu-Arg-ProNHC₂H₅ (TAP-144).
Claim 6
Dependent Claim
13 words
The microcapsule according to claim 1, wherein said polypeptide is thyrotropin-releasing hormone (TRH).
Claim 7
Dependent Claim
19 words
The microcapsule according to claim 1, wherein the molar composition ratio of lactic acid/glycolic acid is 90/10 to 100/0.
Claim 8
Dependent Claim
22 words
The microcapsule according to claim 1, wherein said homopolymer is a poly-lactic acid having a weight-average molecular weight of 7,000 to 25,000.
Claim 9
Dependent Claim
20 words
The microcapsule according to claim 1, wherein said inner aqueous phase contains a 25 to 65% (w/w) of said polypeptide.
Claim 10
Dependent Claim
20 words
The microcapsule according to claim 1, wherein said inner aqueous phase contains a 35 to 60% (w/w) of said polypeptide.
Claim 11
Dependent Claim
19 words
The microcapsule according to claim 1, wherein said inner aqueous phase is prepared without adding a drug retaining substance.
Claim 12
Dependent Claim
89 words
A process for preparing a microcapsule designed for zero order release of a physiologically active polypeptide over a period of at least two months, which comprises preparing a water-in-oil emulsion comprising an inner aqueous phase containing an about 20 to 70% (w/w) of the said polypeptide and an oil phase containing a copolymer or homopolymer having a weight-average molecular weight of 7,000 to 30,000, the molar composition ratio of lactic acid/glycolic acid being 80/20 to 100/0, and then subjecting said water-in-oil emulsion to an in-water drying or phase-separation method.
Claim 13
Dependent Claim
28 words
The process according to claim 12, wherein said water-in-oil emulsion is dispersed in an aqueous phase and then subjecting the resulting water/oil/water ternary emulsion to an in-water drying.
Claim 14
Dependent Claim
24 words
The process according to claim 12, wherein the said water-in-oil emulsion is dispersed in an aqueous phase containing polyvinyl alcohol as an emlusifying agent.
Claim 15
Dependent Claim
29 words
The process according to claim 12, wherein said polypeptide comprises having amino acid residues of two or more and a weight-average molecular weight of about 200 to about 100,000.
Claim 16
Dependent Claim
32 words
The process according to claim 12, wherein said polypeptide is lutenizing hormone-releasing hormone (LH-RH) and an analogous substance of LH-RH which is water-soluble and has a molecular weight of 1,000 or more.
Claim 17
Dependent Claim
12 words
The method according to claim 12, wherein said polypeptide is (pyr)Glu-His-Trp-Ser-Tyr-D-Leu-Leu-Arg-ProNHC₂H₅ (TAP-144).
Claim 18
Dependent Claim
12 words
The process according to claim 12, said polypeptide is thyrotropin-releasing hormone (TRH).
Claim 19
Dependent Claim
19 words
The process according to claim 12, wherein the molar composition ratio of lactic acid/glycolic acid is 90/10 to 100/0.
Claim 20
Dependent Claim
22 words
The process according to claim 12, wherein said homopolymer is a poly-lactic acid having a weight-average molecular weight of 7,000 to 25,000.
Claim 21
Dependent Claim
20 words
The process according to claim 12, wherein said inner aqueous phase contains a 25 to 65% (w/w) of said polypeptide.
Claim 22
Dependent Claim
20 words
The process according to claim 12, wherein said inner aqueous phase contains a 35 to 60% (w/w) of said polypeptide.
Claim 23
Dependent Claim
19 words
The process according to claim 12, wherein said inner aqueous phase is prepared without adding a drug retaining substance.
References Cited (Backward Citations)
No citation records indexed.
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