High drug load buprenorphine microspheres and method of producing same
AssigneeOakwood Laboratories, LLC
InventorsTracy Richey, Bagavathikanun Chithambara Thanoo
Life of this patent
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Abstract
A sustained release microsphere formulation with a high drug load may be formed by a continuous oil-in-water emulsion process by combining an organic dispersed phase with an aqueous continuous phase. The dispersed phase may include an encapsulating polymer, a primary solvent, such as dichloromethane, a pharmaceutically effective amount of an active agent having a solubility relative to the dispersed phase, and a co-solvent, such as benzyl alcohol, which is capable of increasing the solubility of the active agent relative to the dispersed phase. The continuous phase may include an aqueous solution of polyvinyl alcohol and water.
Claims51
A method of making sustained release microsphere formulation having a high buprenorphine drug load, comprising:
- providing a dispersed phase by mixing an encapsulating polymer, a primary solvent, a pharmaceutically effective amount of buprenorphine having a solubility relative to the dispersed phase, and a co-solvent capable of increasing the solubility of the buprenorphine relative to the dispersed phase;
- providing a continuous phase comprising an aqueous solution;
- mixing the dispersed phase with the continuous phase;
- and
- preparing a pharmaceutically acceptable microsphere suspension suitable to be delivered to a patient.
A sustained release microsphere formulation having a high buprenorphine drug load, comprising:
- a dispersed phase comprising an encapsulating polymer, a primary solvent, a pharmaceutically effective amount of buprenorphine having a solubility relative to the dispersed phase, and a co-solvent capable of increasing the solubility of the buprenorphine relative to the dispersed phase;
- a continuous phase comprising an aqueous solution;
- wherein the dispersed phase may be mixed with the continuous phase to form the microsphere formulation.
A sustained release microsphere formulation for injection into a patient, comprising:
- a dispersed phase comprising an encapsulating polymer, at least one solvent, and a pharmaceutically effective amount of buprenorphine;
- a continuous phase comprising an aqueous solution;
- wherein the dispersed phase may be mixed with the continuous phase to form the microsphere formulation;
- and
- wherein the amount of buprenorphine is substantially released from the microsphere formulation in about one month, but less than two months, after it is injected into the patient.
A sustained release microsphere formulation for injection into a patient, comprising:
- a dispersed phase comprising an encapsulating polymer, at least one solvent, and a pharmaceutically effective amount of buprenorphine;
- a continuous phase comprising an aqueous solution;
- wherein the dispersed phase may be mixed with the continuous phase to form the microsphere formulation;
- and
- wherein the amount of buprenorphine is substantially released from the microsphere formulation in about two months, but less than three months, after it is injected into the patient.
A sustained release microsphere formulation for injection into a patient, comprising:
- a dispersed phase comprising an encapsulating polymer, at least one solvent, and a pharmaceutically effective amount of buprenorphine;
- a continuous phase comprising an aqueous solution;
- wherein the dispersed phase may be mixed with the continuous phase to form the microsphere formulation;
- and
- wherein the amount of buprenorphine is substantially released from the microsphere formulation in more than three months, but less than nine months, after it is injected into the patient.
Dependencies are inferred from the claim text.