Injectable Flowable Composition Comprising Buprenorphine
AssigneeRB Pharmaceuticals Limited
InventorsRichard L. Norton, Andrew Watkins, Mingxing Zhou
Life of this patent
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Abstract
The present invention is directed to a buprenorphine sustained release delivery system capable of delivering buprenorphine, a metabolite, or a prodrug thereof for a duration of about 14 days to about 3 months. The buprenorphine sustained release delivery system includes a flowable composition and a solid implant for the sustained release of buprenorphine, a metabolite, or a prodrug thereof. The implant is produced from the flowable composition. The buprenorphine sustained release delivery system provides in situ 1-month and 3-month release profiles characterized by an exceptionally high bioavailability and minimal risk of permanent tissue damage and typically no risk of muscle necrosis.
Claims31
An injectable flowable composition comprising:
- at least one biodegradable thermoplastic polymer that is at least substantially insoluble in body fluid;
- a biocompatible polar aprotic organic liquid selected from the group consisting of one or more of an amide, an ester, a carbonate, a lactam, an ether, and a sulfonyl, wherein the biocompatible polar aprotic organic liquid has a solubility in aqueous medium or body fluid ranging from insoluble to completely soluble in all proportions;
- and,
- 1 wt % to 30 wt % of buprenorphine, a metabolite, or a prodrug thereof;
- wherein the composition is transformed in situ into a solid implant by contact with water, body fluid or other aqueous medium.
A method of forming a flowable composition for use as a controlled release implant, comprising mixing, in any order:
- a biodegradable thermoplastic polymer that is at least substantially insoluble in aqueous medium or body fluid;
- a biocompatible polar aprotic liquid;
- and
- buprenorphine, a metabolite, or a prodrug thereof;
- 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 kit comprising:
- a first syringe comprising a composition comprising a biodegradable thermoplastic polymer that is at least substantially insoluble in a body fluid and a biocompatible polar aprotic liquid;
- and
- a second syringe comprising buprenorphine, a metabolite, or a prodrug thereof;
- wherein the syringes can be directly connected to each other.
A kit comprising a single syringe comprising a composition comprising a biodegradable thermoplastic polymer that is at least substantially insoluble in a body fluid, a biocompatible polar aprotic liquid and buprenorphine, a metabolite, or a prodrug thereof.
A method for treatment of a patient having a medical condition, comprising administering to the patient an effective amount of buprenorphine, a metabolite, or a prodrug thereof in combination with an at least substantially water-insoluble biodegradable thermoplastic polymer and a biocompatible, polar, aprotic organic liquid to provide a biodegradable implant.
Dependencies are inferred from the claim text.