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EP0058481A1 Expired / Lapsed EP ⏱️ 0.0 years remaining

Continuous release pharmaceutical compositions

Assignee: Syngenta Ltd
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Filing: 1982-01-27
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Granted: —
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Expires: 2002-01-27
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Abstract

Abstract Pharmaceutical compositions, comprising a polylactide and a pharmacologically active, acid stable polypeptide, which when placed in an aqueous physiological environment release the polypeptide at an approximately constant rate in an essentially monophasic manner, with a minimal, or no induction period prior to the release; polylactides suitable for use in said compositions; and a method for the manufacture of such polylactides.

Inventors

  • 👤 Francis Gowland Hutchinson

Bibliographic Details

Application Number —
Jurisdiction EP
Data Source google_patents
Last Synchronized 2026-11-04 11:04
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/0012; A61K9/0019; A61K9/0024; A61K9/14; A61K9/16; A61K9/1605; A61K9/1629; A61K9/1641; A61K9/1647; A61K9/20; A61K9/2004; A61K9/2022; A61K9/2031; A61K9/204; A61K9/70; A61K9/7007; C; C07; C07D; C07D319/00; C07D319/10; C07D319/12; C08; C08G; C08G63/00; C08G63/02; C08G63/06; C08G63/08; Y; Y10; Y10S; Y10S930/00; Y10S930/01; Y10S930/28

Claims Analysis

Total Claims: 12
Claim 1
Independent Claim 59 words
A pharmaceutical composition as claimed in claim 1, 2 or 3 comprising from 0.1 to 50% by weight of a polypeptide of molecular weight 8,000 to 30,000 and from 50 to 99.9% by weight of a polylactide wherein the ratio of glycolide to lactide units is O to 3, and which has an inherent viscosity of less than 0.1.
Claim 2
Dependent Claim 52 words
A pharmaceutical composition as claimed in claim 1, 2 or 3 comprising from 5 to 50% by weight of ICI.118,630 and from 50 to 95% by weight of a polylactide wherein the ratio of glycolide to lactide units is 0.8 to 3, and which has an inherent viscosity of more than 0.5.
Claim 3
Dependent Claim 52 words
A pharmaceutical composition as claimed in claim 1, 2 or 3 comprising from 5 to 50% by weight of ICI.118,630 and from 50 to 95% by weight of a polylactide wherein the ratio of glycolide to lactide units is 0.2 to 3, and which has an inherent viscosity of 0.2 to 0.5.
Claim 4
Dependent Claim 52 words
A pharmaceutical composition as claimed in claim 1, 2 or 3 comprising from 0.1 to 50% by weight of ICI.118,630 and from 50 to 99.9% by weight of a polylactide wherein the ratio of glycolide to lactide units is O to 3, and which has an inherent viscosity of less than 0.2.
Claim 5
Dependent Claim 56 words
A pharmaceutical composition as claimed in claim 1, 2 or 3 comprising from 10 to 50% by weight of epidermal growth factor or urogastrone and from 50 to 90% by weight of a polylactide wherein the ratio of glycolide to lactide units is 0.5 to 3, and which has an inherent viscosity of 0.4 to 0.8.
Claim 6
Dependent Claim 54 words
A pharmaceutical composition as claimed in claim 1, 2 or 3 comprising from 0.1 to 50% by weight of epidermal growth factor or urocastrone and from 50 to 99.9% by weight of a polylactide wherein the ratio of glycolide to lactide units is 0.3, and which has an inherent viscosity of 0.15 to 0.4.
Claim 7
Dependent Claim 132 words
A pharmaceutical composition in the form of a suspension for in injection comprising from 1 to 50 % by weight of a solid formulation, which itself comprises from 0.1 to 50% by weight of an acid-stable polypeptide as herein defined and from 50 to 99.9% by weight of a polylactide hwerein the ratio of glycolide to lactide units is O to 3 and which is either soluble in benzene and has an inherent viscosity (lg./ 100ml. solution in benzene) of less than 0.5 or is insoluble in benzene and has an inherent viscosity (lg./ 100ml. solution in chloroform or dioxan) of less than 4, which solid formulation has been reduced to fine particle size, together with from 50 to 99 % by weight of a liquid carrier suitable for injection into mammals.
Claim 8
Dependent Claim 132 words
A pharmaceutical composition in the form of a suspension for in injection comprising from 1 to 50 % by weight of a solid formulation, which itself comprises from 0.1 to 50% by weight of an acid-stable polypeptide as herein defined and from 50 to 99.9% by weight of a polylactide hwerein the ratio of glycolide to lactide units is O to 3 and which is either soluble in benzene and has an inherent viscosity (lg./ 100ml. solution in benzene) of less than 0.5 or is insoluble in benzene and has an inherent viscosity (lg./ 100ml. solution in chloroform or dioxan) of less than 4, which solid formulation has been reduced to fine particle size, together with from 50 to 99 % by weight of a liquid carrier suitable for injection into mammals.
Claim 9
Dependent Claim 70 words
A heterogeneous copolymer of lactic acid and glycolic acid units comprising from 25 to 100% molar of lactic acid units and from O to 75% molar of glycolic acid units, and which is either soluble in benzene and has an inherent viscosity (Ig./lOOml. solution in benzene) of less than 0.5, or is insoluble in benzene and has an inherent viscosity (1g./100ml. solution in chloroform or dioxan) of less than 4.
Claim 10
Dependent Claim 70 words
A heterogeneous copolymer of lactic acid and glycolic acid units comprising from 25 to 100% molar of lactic acid units and from O to 75% molar of glycolic acid units, and which is either soluble in benzene and has an inherent viscosity (Ig./lOOml. solution in benzene) of less than 0.5, or is insoluble in benzene and has an inherent viscosity (1g./100ml. solution in chloroform or dioxan) of less than 4.
Claim 11
Dependent Claim 34 words
A process for the manufacture of a heterogeneous copolymer as claimed in claim 21 which camprises the ring opening copolymerisation of a mixture of the cyclic dimers of lactic acid and glycoli c acid.
Claim 12
Dependent Claim 17 words
A heterogeneous copolymer as claimed in claim 21 whenever prepared by the process claimed in claim 22.

References Cited (Backward Citations)

US3887699A Cited
US3773919A Cited
US4011312A Cited
GB2008135A Cited
EP0025698A2 Cited

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