Polymeric delivery formulations of leuprolide with improved efficacy
AssigneeAtrix Laboratories, Inc.
InventorsRichard L. Dunn, John Steven Garrett, Harish Ravivarapu, Bhagya L Chandrashekar
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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.
Claims49
A flowable composition suitable for use as a controlled release implant, the composition comprising:
- (a) a biodegradable thermoplastic polyester that 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) uncomplexed leuprolide acetate that is the only source of leuprolide in the composition.
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 polyester that 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) uncomplexed leuprolide acetate that is the only source of leuprolide for the composition;
- wherein the mixing is performed for a sufficient period of time effective to form the flowable composition for use as a controlled release implant.
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 polyester that 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 uncomplexed leuprolide acetate that is the only source of leuprolide in the composition.
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 polyester that 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 uncomplexed leuprolide acetate that is the only source of leuprolide in the composition.
A kit comprising:
- (a) a first container comprising a composition comprising a biodegradable thermoplastic polyester that 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 uncomplexed leuprolide acetate that is the only source of leuprolide in the composition.
A solid implant comprising:
- (a) a biocompatible thermoplastic polyester that is at least substantially insoluble in aqueous medium or body fluid;
- and
- (b) uncomplexed leuprolide acetate that is the only source of leuprolide in the implant;
- wherein
- the solid implant has a solid or gelatinous microporous matrix, the matrix being a core surrounded by a skin.
A flowable composition suitable for use as a controlled release implant, the composition comprising:
- (a) a biodegradable thermoplastic polyester that 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;
- and
- (c) uncomplexed leuprolide acetate that is the only source of leuprolide in the composition.
Dependencies are inferred from the claim text.