EP0202065A2
Expired / Lapsed
EP
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Polymer, production and use thereof
Assignee: Takeda Pharmaceutical Co Ltd
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Filing: 1986-05-06
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Granted: —
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Expires: 2006-05-06
Abstract
Abstract The present invention provides a biodegradable high molecular polymer characterized in that the content of water-soluble low molecular compounds, as calculated on the assumption that each of said compounds is a monobasic acid, is less than 0.01 mole per 100 grams of said high molecular polymer.The thus-obtained high molecular polymer has good aging stability and can be used advantageously as an excipient for pharmaceutical preparations.
Inventors
- 👤 Masaki Yamamoto
- 👤 Hiroaki Okada
- 👤 Yasuaki Ogawa
- 👤 Tsutomu Miyagawa
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-10-23 13:16
CPC Classifications
C; C08; C08G; C08G63/00; C08G63/02; C08G63/06; A; A61; A61K; A61K9/00; A61K9/14; A61K9/16; A61K9/1605; A61K9/1629; A61K9/1641; A61K9/1647; A61K9/48; A61K9/50; A61K9/5005; A61K9/5021; A61K9/5031; B; B01; B01J; B01J13/00; B01J13/02; B01J13/06; B01J13/12; B01J13/125
Claims Analysis
Total Claims: 34
Claim 1
Independent Claim
42 words
A biodegradable high molecular polymer characterized in that the content of water-soluble low molecular compounds, as calculated on the assumption that each of said compounds is a monobasic acid, is less than 0.01 mole per 100 grams of said high molecular polymer.
Claim 2
Dependent Claim
42 words
A biodegradable high molecular polymer characterized in that the content of water-soluble low molecular compounds, as calculated on the assumption that each of said compounds is a monobasic acid, is less than 0.01 mole per 100 grams of said high molecular polymer.
Claim 3
Dependent Claim
31 words
The biodegradable high molecular polymer according to claim 1, wherein the biodegradable high molecular polymer is a copolymer or homopolymer having a weight average molecular weigh of about 2,000 to 50,000.
Claim 4
Dependent Claim
33 words
The biodegradable high molecular polymer according to claim 1, wherein the high molecular polymer is a copolymer of about 50-100 mole percent of lactic acid and about 50-0 mole percent of glycolic acid.
Claim 5
Dependent Claim
41 words
The biodegradable high molecular polymer according to claim 3, wherein the high molecular polymer has an inherent viscosity of about 0.05-0.5 dl/g as determined with a 0.5 weight percent chloroform solution thereof and a weight average molecular weight of about 5,000-35,000.
Claim 6
Independent Claim
104 words
A method of producing a biodegradable high molecular polymer characterized in that the content of water-soluble low molecular compounds, as calculated on the assumption that each of said compounds is a monobasic acid, is less than 0.01 mole per 100 arams of said high molecular polymer, which method comprises removing water-soluble low molecular compounds from a biodegradable high molecular polymer containing not less than 0.01 mole of water-soluble low molecular compounds per 100 grams thereof, as calculated on the assumption that each of said compounds is a monobasic acid, using water or a mixture of water and an organic solvent readily soluble in water.
Claim 7
Independent Claim
104 words
A method of producing a biodegradable high molecular polymer characterized in that the content of water-soluble low molecular compounds, as calculated on the assumption that each of said compounds is a monobasic acid, is less than 0.01 mole per 100 arams of said high molecular polymer, which method comprises removing water-soluble low molecular compounds from a biodegradable high molecular polymer containing not less than 0.01 mole of water-soluble low molecular compounds per 100 grams thereof, as calculated on the assumption that each of said compounds is a monobasic acid, using water or a mixture of water and an organic solvent readily soluble in water.
Claim 8
Dependent Claim
31 words
The method according to claim 5, wherein the organic solvent readily soluble in water is a member selected from the group consisting of acetone, methanol, ethanol, tetrahydrofuran, acetonitrile and ethyl acetate.
Claim 9
Dependent Claim
16 words
The method according to claim 6, wherein the organic solvent readily soluble in water is ethanol.
Claim 10
Dependent Claim
27 words
The method according to claim 5, wherein the ratio of the mixture of water and organic solvent readily soluble in water (v/v) is about 100/0 to 100/100.
Claim 11
Dependent Claim
26 words
The method according to claim 5, wherein the biodegradable high molecular polymer containing the water-soluble low molecular compounds is in advance dissolved in a organic solvent.
Claim 12
Dependent Claim
20 words
The method according to claim 5, wherein the removal of the water soluble low molecular compounds is conducted under stirring.
Claim 13
Dependent Claim
26 words
The method according to claim 5, wherein the removal of the water soluble low molecular compounds is conducted at a temperature of about 0° to 90°C.
Claim 14
Dependent Claim
64 words
The method according to claim 9, wherein the biodegradable high molecular polymer containing water-soluble low molecular compounds is dissolved in a 3 to 20 times amount (w/v) of an organic solvent, then the solution is poured into water under stirring at a temperature about 20° to 70°C to remove the trace amount of water soluble low molecular compounds from the biodegradable high molecular polymer.
Claim 15
Dependent Claim
60 words
A microcapsule for injectable sustained release which contains an effective amount of an ingredient and a biodegradable high molecular polymer characterized in that the content of water-soluble low molecular compounds, as calculated on the assumption that each of said compounds is a monobasic acid, is less than 0.01 mole per 100 grams of said high molecular polymer as an excipient.
Claim 16
Dependent Claim
60 words
A microcapsule for injectable sustained release which contains an effective amount of an ingredient and a biodegradable high molecular polymer characterized in that the content of water-soluble low molecular compounds, as calculated on the assumption that each of said compounds is a monobasic acid, is less than 0.01 mole per 100 grams of said high molecular polymer as an excipient.
Claim 17
Dependent Claim
13 words
The microcapsule according to claim 13, wherein the ingredient is a water-soluble peptide.
Claim 18
Independent Claim
136 words
A method for producing a microcapsule for injectable sustained release which contains an effective amount of an ingredient and a biodegradable high molecular polymer characterized in that the content of water-soluble low molecular compounds, as calculated on the assumption that each of said compounds is a monobasic acid, is less than 0.01 mole per 100 grams of said high molecular polymer as an excipient, which comprises preparing a w/o emulsion with a solution containing the ingredient serving as an inner water phase and a solution containing the biodegradable high molecular polymer serving as an oil phase, dispersing said emulsion in a water phase to give a (w/o)/w emulsion, and subjecting the thus obtained emulsion to a third aqueous phase to give a (w/o)/w ternary phase emulsion, and then the solvent in the oil phase is desorbed.
Claim 19
Independent Claim
136 words
A method for producing a microcapsule for injectable sustained release which contains an effective amount of an ingredient and a biodegradable high molecular polymer characterized in that the content of water-soluble low molecular compounds, as calculated on the assumption that each of said compounds is a monobasic acid, is less than 0.01 mole per 100 grams of said high molecular polymer as an excipient, which comprises preparing a w/o emulsion with a solution containing the ingredient serving as an inner water phase and a solution containing the biodegradable high molecular polymer serving as an oil phase, dispersing said emulsion in a water phase to give a (w/o)/w emulsion, and subjecting the thus obtained emulsion to a third aqueous phase to give a (w/o)/w ternary phase emulsion, and then the solvent in the oil phase is desorbed.
Claim 20
Independent Claim
104 words
A method of producing a biodegradable high molecular polymer characterized in that the content of water-soluble low molecular compounds, as calculated on the assumption that each of said compounds is a monobasic acid, is less than 0.01 mole per 100 grams of said high molecular polymer, which method comprises removing water-soluble low molecular compounds from a biodegradable high molecular polymer containing not less than 0.01 mole of water-soluble low molecular compounds per 100 grams thereof, as calculated on the assumption that each of said compounds is a monobasic acid, using water or a mixture of water and an organic solvent readily soluble in water.
Claim 21
Independent Claim
104 words
A method of producing a biodegradable high molecular polymer characterized in that the content of water-soluble low molecular compounds, as calculated on the assumption that each of said compounds is a monobasic acid, is less than 0.01 mole per 100 grams of said high molecular polymer, which method comprises removing water-soluble low molecular compounds from a biodegradable high molecular polymer containing not less than 0.01 mole of water-soluble low molecular compounds per 100 grams thereof, as calculated on the assumption that each of said compounds is a monobasic acid, using water or a mixture of water and an organic solvent readily soluble in water.
Claim 22
Dependent Claim
28 words
The method according to claim 1, wherein the biodegradable high molecular polymer is a copolymer or homopolymer having a weight average molecular weight of about 2,000 to 50,000.
Claim 23
Dependent Claim
30 words
The method according to claim 1, wherein the high molecular polymer is a copolymer of about 50-100 mole percent of lactic acid and about 50-0 mole percent of glycolic acid.
Claim 24
Dependent Claim
38 words
The method according to claim 3, wherein the high molecular polymer has an inherent viscosity of about 0.05-0.5 dl/g as determined with a 0.5 weight percent chloroform solution thereof and a weight average molecular weight of about 5,000-35,000.
Claim 25
Dependent Claim
31 words
The method according to claim 1, wherein the organic solvent readily soluble in water is a member selected from the group consisting of acetone, methanol, ethanol, tetrahydrofuran, acetonitrile and ethyl acetate.
Claim 26
Dependent Claim
16 words
The method according to claim 5, wherein the organic solvent readily soluble in water is ethanol.
Claim 27
Dependent Claim
27 words
The method according to claim 1, wherein the ratio of the mixture of water and organic solvent readily soluble in water (v/v) is about 100/0 to 100/100.
Claim 28
Dependent Claim
26 words
The method according to claim 1, wherein the biodegradable high molecular polymer containing the water-soluble low molecular compounds is in advance dissolved in a organic solvent.
Claim 29
Dependent Claim
21 words
The method according to claim 1, wherein the removal of the water soluble low molecular compounds - is conducted under stirring.
Claim 30
Dependent Claim
26 words
The method according to claim 1, wherein the removal of the water soluble low molecular compounds is conducted at a temperature of about 0° to 90°C.
Claim 31
Dependent Claim
64 words
The method according to claim 8, wherein the biodegradable high molecular polymer containing water-soluble low molecular compounds is dissolved in a 3 to 20 times amount (w/v) of an organic solvent, then the solution is poured into water under stirring at a temperature about 20° to 70°C to remove the trace amount of water soluble low molecular compounds from the biodegradable high molecular polymer.
Claim 32
Independent Claim
136 words
A method for producing a microcapsule for injectable sustained release which contains an effective amount of an ingredient and a. biodegradable high molecular polymer characterized in that the content of water-soluble low molecular compounds, as calculated on the assumption that each of said compounds is a monobasic acid, is less than 0.01 mole per 100 grams of said high molecular polymer as an excipient, which comprises preparing a w/o emulsion with a solution containing the ingredient serving as an inner water phase and a solution containing the biodegradable high molecular polymer serving as an oil phase, dispersing said emulsion in a water phase to give a (w/o)/w emulsion, and subjecting the thus obtained emulsion to a third aqueous phase to give a (w/o)/w ternary phase emulsion, and then the solvent in the oil phase is desorbed.
Claim 33
Independent Claim
136 words
A method for producing a microcapsule for injectable sustained release which contains an effective amount of an ingredient and a. biodegradable high molecular polymer characterized in that the content of water-soluble low molecular compounds, as calculated on the assumption that each of said compounds is a monobasic acid, is less than 0.01 mole per 100 grams of said high molecular polymer as an excipient, which comprises preparing a w/o emulsion with a solution containing the ingredient serving as an inner water phase and a solution containing the biodegradable high molecular polymer serving as an oil phase, dispersing said emulsion in a water phase to give a (w/o)/w emulsion, and subjecting the thus obtained emulsion to a third aqueous phase to give a (w/o)/w ternary phase emulsion, and then the solvent in the oil phase is desorbed.
Claim 34
Dependent Claim
13 words
The microcapsule according to claim 12, wherein the ingredient is an water-soluble peptide.
References Cited (Backward Citations)
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