EP0166596A2
Expired / Lapsed
EP
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Biodegradable amphipathic copolymers
Assignee: Imperial Chemical Industries Ltd
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Filing: 1985-06-24
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Granted: —
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Expires: 2005-06-24
Abstract
Abstract A pharmaceutically or veterinarily acceptable amphipathic, non-cross linked linear, branched or graft block copolymer, which has a minimum weight average molelcular-weight of 1000, in which the hydrophobic component is biodegradable or hydrolytically unstable under normal physiological conditions, and the hydrophilic component may or may not be biodegradable or hydrolytically unstable under such conditions, and which copolymer is self-dispersible in water; together with mixtures of such a copolymer and a drug, which may be water-soluble or water-insoluble, which mixtures are self-dispersible in water; and processes for the manufacture of such copolymers and such mixtures.
Inventors
- 👤 Jeffrey Richard Churchill
- 👤 Francis Gowland Hutchinson
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-10-23 10:53
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/48; A61K9/50; A61K9/51; A61K9/5107; A61K9/513; A61K9/5146; A61K9/5153; A61K9/10; A61K9/107; A61K9/1075; A61K9/14; A61K9/141; A61K9/146; C; C08; C08G; C08G63/00; C08G63/02; C08G63/06; C08G63/08; C08G63/66; C08G63/664; Y; Y10; Y10S; Y10S977/00; Y10S977/70; Y10S977/734; Y10S977/735; Y10S977/737; Y10S977/738; Y10S977/773; Y10S977/775; Y10S977/788; Y10S977/795; Y10S977/797; Y10S977/798; Y10S977/799; Y10S977/801; Y10S977/84; Y10S977/849; Y10S977/86; Y10S977/868; Y10S977/869; Y10S977/895; Y10S977/902; Y10S977/904; Y10S977/905; Y10S977/915
Claims Analysis
Total Claims: 12
Claim 1
Independent Claim
66 words
A pharmaceutically or veterinarily acceptable amphipathic, non-cross-linked linear, branched or graft block copolymer, which has a minimum weight average molecular weight of 1000, in which the hydrophobic component is biodegradable or hydrolytically unstable under normal physiological conditions, and the hydrophilic component may or may not be biodegradable or hydrolytically unstable under such conditions, characterised in that it is self-dispersible in water to form a stable dispersion.
Claim 2
Dependent Claim
66 words
A pharmaceutically or veterinarily acceptable amphipathic, non-cross-linked linear, branched or graft block copolymer, which has a minimum weight average molecular weight of 1000, in which the hydrophobic component is biodegradable or hydrolytically unstable under normal physiological conditions, and the hydrophilic component may or may not be biodegradable or hydrolytically unstable under such conditions, characterised in that it is self-dispersible in water to form a stable dispersion.
Claim 3
Dependent Claim
29 words
A copolymer as claimed in claim 1 which either has a large proportion of hydrophile to hydrophobe or has a hydrophobe weight average molecular weight of less than 5000.
Claim 4
Dependent Claim
75 words
A process for the manufacture of a self-dispersible copolymer as defined in claim 1, which comprises freeze-drying a frozen stable aqueous dispersion of a pharmaceutically or veterinarily acceptable amphipathic, non-cross-linked linear, branched or graft block copolymer, which has a minimum weight average molecular weight of 1000, in which the hydrophobic component is biodegradable or hydrolytically unstable under such conditions, and the hydrophilic component may or may not be biodegradable or hydrolytically unstable under such conditions.
Claim 5
Dependent Claim
97 words
A process for the manufacture of a frozen aqueous dispersion of a pharmaceutically or veterinarily acceptable amphipathic, non-cross-linked linear, branched or graft block copolymer, which has a minimum weight average moleculare weight of 1000, in which the hydrophobic component is biodegradable or hydrolytically unstable and the hydrophobic component may or may not be biodegradable or hydrolytically unstable, which comprises dissolving such a copolymer in the non-self-dispersible form in a water-miscible solvent which either has a low boiling point or is freeze-driable, vigorously agitating said solution while an excess of water is added, and freezing the resulting dispersion.
Claim 6
Dependent Claim
97 words
A process for the manufacture of a frozen aqueous dispersion of a pharmaceutically or veterinarily acceptable amphipathic, non-cross-linked linear, branched or graft block copolymer, which has a minimum weight average moleculare weight of 1000, in which the hydrophobic component is biodegradable or hydrolytically unstable and the hydrophobic component may or may not be biodegradable or hydrolytically unstable, which comprises dissolving such a copolymer in the non-self-dispersible form in a water-miscible solvent which either has a low boiling point or is freeze-driable, vigorously agitating said solution while an excess of water is added, and freezing the resulting dispersion.
Claim 7
Dependent Claim
51 words
A solid, copolymer/drug powder material comprising up to 99% by weight of a drug, the remainder being a pharmaceutically or veterinarily acceptable amphipathic, non-cross-linked linear, branched or graft block copolymer as claimed in claim 1 characterised in that said solid, powder material is self-dispersible in water to form a stable dispersion.
Claim 8
Dependent Claim
85 words
A copolymer/drug powder material as claimed in claim 5 wherein the drug is water-soluble and is selected from oxytocin, vasopressin, adrenocorticotrophic hormone (ACTH), epidermal growth factor (EGF), transforming growth factor antagonists, prolactin, luliberin or luteinizing hormone releasing hormone (LH-RH), LH-RH agonists or antagonists, growth hormone, growth hormone releasing factor, insulin, somatostatin, bombesin antagonists, glucagon, interferon, gastrin, tetragastrin, pentagastrin, urogastrone, secretin, calcitonin, enkephalins, endorphins, angiotensins, renin, bradykinin, bacitracins, polymyxins, colistins, tyrocidin, gramicidines and synthetic analogues and modifications and pharmaceutically-active fragments thereof, monoclonal antibodies and soluble vaccines.
Claim 9
Dependent Claim
30 words
A process for the manufacture of a solid, copolymer/drug powder material as claimed in claim 5, characterised by freeze-drying a frozen, stable aqueous dispersion of the copolymer and the drug.
Claim 10
Dependent Claim
62 words
A process for the manufacture of a frozen, stable aqueous dispersion of a copolymer and a water-soluble drug, as defined in claim 7, characterised by dispersing a self-dispersible copolymer, as claimed in claim 1, in water, buffering the dispersion to physiological or neutral pH, mixing the buffered dispersion with an aqueous solution of the water-soluble drug, and freezing the resulting copolymer/drug dispersion.
Claim 11
Dependent Claim
63 words
A process for the manufacture of a frozen, stable aqueous dispersion of a copolymer and a water-insoluble drug, as defined in claim 7, characterised by dissolving the drug and the self-dispersible copolymer in a minimum amount of a water-miscible organic solvent, slowly adding an excess of water to the vigorously agitated solution of produce a fine, stable dispersion, and then freezing the dispersion.
Claim 12
Dependent Claim
90 words
A process for the manufacture of a frozen, stable aqueous dispersion of a copolymer and a drug, as defined in claim 7, characterised by dissolving the copolymer, in its non-self-dispersible form, in a water-miscible, organic solvent, slowly adding an excess of water to the vigorously agitated solution, adding a solution of the drug, either in water if the drug is water-soluble, or in a water-miscible solvent or in a mixture thereof with water if the drug is water-insoluble, to the copolymer dispersion, and then freezing the copolymer/drug dispersion so obtained.
References Cited (Backward Citations)
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