An oil-in-water buprenorphine formulation including buprenorphine and a surfactant that emulsifies the buprenorphine in oil, wherein the drug release is controlled by varying the oil concentration and/or pH. A buprenorphine aqueous suspension formulation including a free base buprenorphine and a suspension stabilizer. A buprenorphine oil formulation including a buprenorphine salt suspended in a pharmaceutically acceptable oil. Methods of providing sustained release of buprenorphine over a period of time.
- An oil-in- water buprenorphine formulation comprising buprenorphine; and a surfactant that emulsifies said buprenorphine in oil, wherein control of release of said buprenorphine is controlled by varying the oil concentration and/or pH.
- The formulation according to claim 1 wherein said buprenorphine is selected from the group consisting of a free base and a salt.
- The formulation according to claim 1, wherein said surfactant is selected from the group consisting of synthetic non-ionic surfactants, polypropylene polyethylene block copolymers, phosphatides, egg phosphatide, polysorbates, other surfactants acceptable for parenteral administration, and combinations thereof.
- The formulation according to claim 1, wherein said buprenorphine is dissolved in a water immiscible solvent selected from the group consisting of vegetable oil, soybean oil, safflower oil, cottonseed oil, corn oil, sunflower oil, arachis oil, castor oil, olive oil, ester of a medium or long chain fatty acid such as a mono-, di-, or triglyceride, ethyl oleate, isopropyl myristate, polyoxyl hydrogenated castor oil, and combinations thereof.
- The formulation according to claim 1 further comprising glycerol.
- The formulation according to claim 1 further comprising pH adjusting agents selected from the group consisting of sodium hydroxide.
- The formulation according to claim 1 further comprising substances selected from the group consisting of a buffer further selected from the group consisting of sodium citrate and sodium phosphate, and combinations thereof.
- The formulation according to claim 1 further comprising preservatives selected from the group consisting of benzyl alcohol, EDTA, and combinations thereof.
- A buprenorphine aqueous suspension formulation comprising free base buprenorphine and a suspending agent.
- The formulation according to claim 9, wherein said buprenorphine is a free base buprenorphine formed by the addition of an alkali metal salt selected from the group consisting of NaOH to buprenorphine salt.
- The formulation according to claim 9, wherein said suspending agent is selected from the group consisting of polyvinyl pyrrolidone (PVP), sodium carboxymethylcellulose, and dextran.
- The formulation according to claim 9, wherein the composition has a pH of from about 6 to about 8.
- The formulation according to claim 9, wherein said formulation further comprises substances selected from the group consisting of a buffer further selected from the group consisting of sodium citrate and sodium phosphate, and combinations thereof.
- The formulation according to claim 9 further comprising preservatives selected from the group consisting of benzyl alcohol, methyl paraben, propyl paraben, and combinations thereof.
- The formulation according to claim 9, wherein said buprenorphine is a free base buprenorphine formed by dispersing said buprenorphine free base into the suspending agent solution and mixing the formulation with a high shear homogenizer.
- A buprenorphine oil formulation comprising a buprenorphine salt suspended in a pharmaceutically acceptable oil.
- The formulation according to claim 15, wherein said buprenorphine salt is buprenorphine HCl.
- The formulation according to claim 15, wherein said pharmaceutically acceptable oil is selected from the group consisting of cottonseed oil, corn oil, peanut oil, and soybean oil.
- The formulation according to claim 15 further comprising a suspending agent as a sorbitan fatty acid hexitan ester.
- A method of providing sustained release of buprenorphine over a period of time by administering the formulation according to claims 1, 9, and 16.
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Abbott Lab
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Luangdilok Carmela
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Flanagan Douglas R
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Li Luk-chiu
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Widman Matthew
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A61K31/485
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- Publication: Sep 4, 2008
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Application:
Feb 28, 2008
US 2008/0055211 W
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Priority:
Feb 28, 2007
US 89207707 P