Back to results
US 6,773,714 B2Granted
Polymeric delivery formulations of leuprolide with improved efficacy
AssigneeAtrix Laboratories, Inc.
InventorsRichard L. Dunn, John Steven Garrett, Harish Ravivarapu, Bhagya L. Chandrashekar
Life of this patent
Estimating the term…
Abstract
The present invention is directed to a flowable composition that is suitable for use as a controlled release implant. The flowable composition includes a biodegradable thermoplastic polyester that is at least substantially insoluble in aqueous medium or body fluid. The flowable composition also includes a biocompatible polar aprotic solvent. The biocompatible polar aprotic solvent is miscible to dispersible in aqueous medium or body fluid. The flowable composition also includes leuprolide acetate.
Claims47
A flowable composition suitable for use as a controlled release implant, the composition comprising:
- (a) a biodegradable thermoplastic homopolymer of lactide, glycolide, or caprolactone, or a copolymer of any combination of lactide, glycolide and caprolactone, wherein the homopolymer or copolymer includes a monofunctional alcohol or a diol residue, is without a carboxylic acid terminus and is at least substantially insoluble in aqueous medium or body fluid;
- (b) a biocompatible polar aprotic solvent selected from the group consisting of an amide, an ester, a carbonate, a ketone, an ether, and a sulfonyl;
- wherein the biocompatible polar aprotic solvent is miscible to dispersible in aqueous medium or body fluid;
- and
- (c) leuprolide acetate.
2 more elements
A method for forming a flowable composition for use as a controlled release implant, comprising the step of mixing, in any order:
- (a) a biodegradable thermoplastic homopolymer of lactide, glycolide, or caprolactone, or a copolymer of any combination of lactide, glycolide and caprolactone, wherein the homopolymer or copolymer includes a monofunctional alcohol or a diol residue, is without a carboxylic acid terminus and is at least substantially insoluble in aqueous medium or body fluid;
- (b) a biocompatible polar aprotic solvent selected from the group consisting of an amide, an ester, a carbonate, a ketone, an ether, and a sulfonyl;
- wherein the biocompatible polar aprotic solvent is miscible to dispersible in aqueous medium or body fluid;
- and
- (c) leuprolide acetate;
- wherein the mixing is performed for a sufficient period of time effective to form the flowable composition for use as a controlled release implant.
3 more elements
A biodegradable implant formed in situ, in a patient, by the steps comprising:
- (a) injecting a composition within the body of the patient;
- and
- (b) allowing the biocompatible polar aprotic solvent to dissipate to produce a solid biodegradable implant, wherein the composition comprises an effective amount of a biodegradable thermoplastic homopolymer of lactide, glycolide, or caprolactone, or a copolymer of any combination of lactide, glycolide and caprolactone, wherein the homopolymer or copolymer includes a monofunctional alcohol or a diol residue, is without a carboxylic acid terminus and is at least substantially insoluble in aqueous medium or body fluid;
- an effective amount of a biocompatible polar aprotic solvent selected from the group consisting of an amide, an ester, a carbonate, a ketone, an ether, and a sulfonyl, wherein the biocompatible polar aprotic solvent is miscible to dispersible in aqueous medium or body fluid;
- and an effective amount of leuprolide acetate.
2 more elements
A method of forming a biodegradable implant in situ, in a living patient, comprising the steps of:
- (a) injecting a flowable composition within the body of a patient;
- and
- (b) allowing the biocompatible polar aprotic solvent to dissipate to produce a solid biodegradable implant, wherein the flowable composition comprises an effective amount of a biodegradable thermoplastic homopolymer of lactide, glycolide, or caprolactone, or a copolymer of any combination of lactide, glycolide and caprolactone, wherein the homopolymer or copolymer includes a monofunctional alcohol or a dial residue, is without a carboxylic acid terminus and is at least substantially insoluble in aqueous medium or body fluid;
- an effective amount of a biocompatible polar aprotic solvent selected from the group consisting of an amide, an ester, a carbonate, a ketone, an ether, and a sulfonyl;
- wherein the biocompatible polar aprotic solvent is miscible to dispersible in aqueous medium or body fluid;
- and an effective amount of leuprolide acetate.
3 more elements
A kit comprising:
- (a) a first container comprising a composition comprising a biodegradable thermoplastic homopolymer of lactide, glycolide, or caprolactone, or a copolymer of any combination of lactide, glycolide and caprolactone, wherein the homopolymer or copolymer includes a monofunctional alcohol or a diol residue, is without a carboxylic acid terminus and is at least substantially insoluble in aqueous medium or body fluid and a biocompatible polar aprotic solvent selected from the group consisting of an amide, an ester, a carbonate, a ketone, an ether, and a sulfonyl;
- wherein the biocompatible polar aprotic solvent is miscible to dispersible in aqueous medium or body fluid;
- and
- (b) a second container comprising leuprolide acetate.
1 more element
A solid implant comprising:
- (a) a biocompatible thermoplastic homopolymer of lactide, glycolide, or caprolactone, or a copolymer of any combination of lactide, glycolide and caprolactone, wherein the homopolymer or copolymer includes a monofunctional alcohol or a diol residue, is without a carboxylic acid terminus and is at least substantially insoluble in aqueous medium or body fluid;
- and
- (b) leuprolide acetate;
- wherein
- the solid implant has a solid or gelatinous microporous matrix, the matrix being a core surrounded by a skin.
2 more elements
A flowable composition suitable for use as a controlled release implant, the composition comprising:
- (a) a biodegradable thermoplastic copolymer of lactide dimer and glycolide dimer wherein the copolymer includes a single lactic or glycolic acid residue and is at least substantially insoluble in aqueous medium or body fluid;
- (b) a biocompatible polar aprotic solvent selected from the group consisting of an amide, an ester, a carbonate, a ketone, an ether, and a sulfonyl;
- wherein the biocompatible polar aprotic solvent is miscible to dispersible in aqueous medium or body fluid;
- and
- (c) leuprolide acetate.
2 more elements
Dependencies are inferred from the claim text.