Porous drug matrices and methods of manufacture thereof
First Claim
1. A method of delivering a drug to a patient in need thereof, comprisingadministering a therapeutically or prophylactically effective amount of the drug in a formulation comprising a porous matrix which comprises a wetting agent and microparticles of the drug, wherein the microparticles have a mean diameter between about 0.1 and 5 μ
- m and a total surface area greater than about 0.5 m2/mL, and wherein the porous matrix has a TAP density less than or equal to 1.0 g/mL or has a total surface area of greater than or equal to 0.2 m2/g and is in the form of a dry powder, and wherein the porous matrix is made by a process comprising, dissolving the drug in a volatile solvent to form a drug solution, combining at least one volatile salt with the drug solution to form an emulsion, suspension, or second solution, incorporating at least one wetting agent into the emulsion, suspension, or second solution, and removing the volatile solvent and volatile salt from the emulsion, suspension, or second solution to yield the porous matrix.
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Accused Products
Abstract
Drugs, especially low aqueous solubility drugs, are provided in a porous matrix form, preferably microparticles, which enhances dissolution of the drug in aqueous media. The drug matrices preferably are made using a process that includes (i) dissolving a drug, preferably a drug having low aqueous solubility, in a volatile solvent to form a drug solution, (ii) combining at least one pore forming agent with the drug solution to form an emulsion, suspension, or second solution, and (iii) removing the volatile solvent and pore forming agent from the emulsion, suspension, or second solution to yield the porous matrix of drug. The pore forming agent can be either a volatile liquid that is immiscible with the drug solvent or a volatile solid compound, preferably a volatile salt. In a preferred embodiment, spray drying is used to remove the solvents and the pore forming agent. The resulting porous matrix has a faster rate of dissolution following administration to a patient, as compared to non-porous matrix forms of the drug. In a preferred embodiment, microparticles of the porous drug matrix are reconstituted with an aqueous medium and administered parenterally, or processed using standard techniques into tablets or capsules for oral administration.
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Citations
17 Claims
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1. A method of delivering a drug to a patient in need thereof, comprising
administering a therapeutically or prophylactically effective amount of the drug in a formulation comprising a porous matrix which comprises a wetting agent and microparticles of the drug, wherein the microparticles have a mean diameter between about 0.1 and 5 μ - m and a total surface area greater than about 0.5 m2/mL, and wherein the porous matrix has a TAP density less than or equal to 1.0 g/mL or has a total surface area of greater than or equal to 0.2 m2/g and is in the form of a dry powder, and
wherein the porous matrix is made by a process comprising, dissolving the drug in a volatile solvent to form a drug solution, combining at least one volatile salt with the drug solution to form an emulsion, suspension, or second solution, incorporating at least one wetting agent into the emulsion, suspension, or second solution, and removing the volatile solvent and volatile salt from the emulsion, suspension, or second solution to yield the porous matrix. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17)
- m and a total surface area greater than about 0.5 m2/mL, and wherein the porous matrix has a TAP density less than or equal to 1.0 g/mL or has a total surface area of greater than or equal to 0.2 m2/g and is in the form of a dry powder, and
Specification