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Biodegradable amphipathic copolymers

Assignee: AstraZeneca UK Ltd
•
Filing: 1985-06-21
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Granted: 1988-05-17
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Expires: 2005-06-21
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Abstract

Abstract 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, and which copolymer is self-dispersible in water; together with mixtures of such a copolymer and a drug, which may be water-soluble of water-insoluble, which mixtures are self-dispersible in water; and processes for the manufacture of such copolymers and such mixtures.

Inventors

  • 👤 Jeffrey R. Churchill
  • 👤 Francis G. Hutchinson

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-10-23 13:39
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: 6
Claim 1
Independent Claim 253 words
A pharmaceutically or veterinarily acceptable amphipathic block copolymer, which is self-dispersable in water to form a stable dispersion in water without the addition of any surfactant or other additive and has a minimum weight average molecular weight of 1000, selected from the group consisting of (a) non-cross-linked linear copolymers of the formula A m (BA) n or B m (AB) n ; and (b) non-cross-linked branched or graft block copolymers of the formula AB n or BA n wherein respectively A or B is a backbone polymer with n units of a monomer or polymer B or A respectively grafted onto it; wherein m is 0 or 1; n is an integer; wherein A is a pharmaceutically or veterinarily acceptable hydrophobic polymer which is biodegradable or hydrolytically unstable under normal physiological conditions and is selected from the group consisting of poly(D-, L- and DL-lactic acids); poly(D-, L-, and DL-lactides); polyglycolic acid; polyglycolide; poly-caprolactone; poly(3-hydroxybutyric acid); non-therapeutic hydrophobic polypeptides; polyacetals of the formula: ##STR5## wherein R is a hydrocarbon radical, and n is as previously defined; polycarbonates and polyorthoesters of the formula: ##STR6## wherein R and n are as previously defined; copolymers of the formula: ##STR7## wherein R and n are as previously defined; and copolymers derived from at least two monomers from which the above polymers are derived; and wherein B is a pharmaceutically or veterinarily acceptable hydrophilic polymer selected from the group consisting of polyvinylalcohol, polyvinylpyrrolidone, polyethylene glycol, polyacrylamide, polymethacrylamide, dextran, alginic acid, sodium alginate, gelatine, copolymers thereof, and polyoxyethylene/polyoxypropylene block copolymers.
Claim 2
Dependent Claim 253 words
A pharmaceutically or veterinarily acceptable amphipathic block copolymer, which is self-dispersable in water to form a stable dispersion in water without the addition of any surfactant or other additive and has a minimum weight average molecular weight of 1000, selected from the group consisting of (a) non-cross-linked linear copolymers of the formula A m (BA) n or B m (AB) n ; and (b) non-cross-linked branched or graft block copolymers of the formula AB n or BA n wherein respectively A or B is a backbone polymer with n units of a monomer or polymer B or A respectively grafted onto it; wherein m is 0 or 1; n is an integer; wherein A is a pharmaceutically or veterinarily acceptable hydrophobic polymer which is biodegradable or hydrolytically unstable under normal physiological conditions and is selected from the group consisting of poly(D-, L- and DL-lactic acids); poly(D-, L-, and DL-lactides); polyglycolic acid; polyglycolide; poly-caprolactone; poly(3-hydroxybutyric acid); non-therapeutic hydrophobic polypeptides; polyacetals of the formula: ##STR5## wherein R is a hydrocarbon radical, and n is as previously defined; polycarbonates and polyorthoesters of the formula: ##STR6## wherein R and n are as previously defined; copolymers of the formula: ##STR7## wherein R and n are as previously defined; and copolymers derived from at least two monomers from which the above polymers are derived; and wherein B is a pharmaceutically or veterinarily acceptable hydrophilic polymer selected from the group consisting of polyvinylalcohol, polyvinylpyrrolidone, polyethylene glycol, polyacrylamide, polymethacrylamide, dextran, alginic acid, sodium alginate, gelatine, copolymers thereof, and polyoxyethylene/polyoxypropylene block copolymers.
Claim 3
Dependent Claim 24 words
The amphiphatic copolymer of claim 1 wherein the copolymer is made self-dispersible by including at least 50 (wt) % hydrophilic component in the copolymer.
Claim 4
Dependent Claim 27 words
The amphiphatic copolymer of claim 1 wherein the copolymer is made self-dispersible by maintaining the weight average molecular weight of the hydrophobic component at less than 5000.
Claim 5
Dependent Claim 28 words
The amphiphatic copolymer of claim 1 wherein the copolymer is a graft block copolymer made self-dispersible by maintaining at least 50 (wt) % hydrophilic component in the graft.
Claim 6
Dependent Claim 34 words
The amphiphatic copolymer of claim 1 wherein the weight average molecular weight is at least 5000 and wherein the copolymer is made self-dispersible by a process involving freeze-drying of a dispersion of the copolymer.

References Cited (Backward Citations)

US3651008A Cited
US3887699A Cited
US3773919A Cited
US4018736A Cited
EP0058481A1 Cited
US4526938A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1991-05-17 1991-11-16 1992-05-17 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1995-05-17 1995-11-16 1996-05-17 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1999-05-17 1999-11-16 2000-05-17 $7700.00 Window Closed / Lapsed

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