Sustained drug release and improved product stability using non-covalent particle coating methods
First Claim
1. A method of stabilizing an active agent or drug comprising:
- providing an active agent or drug hydrate having a bound water, wherein the active agent or drug degrades in the presence of water;
removing the bound water from the active agent or drug hydrate;
wherein removing the bound water from the active agent or drug hydrate further comprises;
dissolving the active agent or drug hydrate in a solvent, wherein the solvent consists of one or more independent solvents comprising 0.05% water by volume or less, wherein the solvent is capable of forming an azeotrope with a dissolved previously bound water of the active agent or drug hydrate;
wherein dissolving the active agent or drug hydrate in the solvent forms a solution comprising the dissolved active agent or drug and an azeotrope of the solvent and the dissolved previously bound water;
adding a substrate to the solution to form a suspension with the solution, wherein the substrate is a pharmaceutically suitable excipient; and
sequestering the dissolved previously bound water from the active agent or drug;
wherein sequestering the dissolved previously bound water further comprises depositing an anhydrous active agent or drug of the active agent or drug hydrate onto the substrate; and
evaporating the azeotrope until a substrate powder is formed, wherein at least one molecule of the anhydrous active agent or drug of the substrate powder is non-covalently bound to the substrate.
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Accused Products
Abstract
The present invention relates to improved methods of making compositions and compositions made by these methods having improved stability and/or extended release of an active agent or drug upon administration. These compositions may generally comprise an active agent or drug non-covalently immobilized or bound to an excipient substrate. The active agent or drug may include a wide variety of drugs. Binding of the active agent or drug to the substrate may be achieved by evaporating a solvent containing the active agent dissolved therein or by triggering co-precipitation by addition of a precipitating solvent. Additional steps of vacuum removal of surrounding atmosphere and replacement with inert gas may provide additional stability. Present methods and compositions also facilitate manufacturing of drug products and may make these processes safer in some cases. The present invention further provides improved methods of treatment or administration, which may take advantage of improvements with present compositions.
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Citations
41 Claims
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1. A method of stabilizing an active agent or drug comprising:
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providing an active agent or drug hydrate having a bound water, wherein the active agent or drug degrades in the presence of water; removing the bound water from the active agent or drug hydrate; wherein removing the bound water from the active agent or drug hydrate further comprises; dissolving the active agent or drug hydrate in a solvent, wherein the solvent consists of one or more independent solvents comprising 0.05% water by volume or less, wherein the solvent is capable of forming an azeotrope with a dissolved previously bound water of the active agent or drug hydrate; wherein dissolving the active agent or drug hydrate in the solvent forms a solution comprising the dissolved active agent or drug and an azeotrope of the solvent and the dissolved previously bound water; adding a substrate to the solution to form a suspension with the solution, wherein the substrate is a pharmaceutically suitable excipient; and sequestering the dissolved previously bound water from the active agent or drug; wherein sequestering the dissolved previously bound water further comprises depositing an anhydrous active agent or drug of the active agent or drug hydrate onto the substrate; and evaporating the azeotrope until a substrate powder is formed, wherein at least one molecule of the anhydrous active agent or drug of the substrate powder is non-covalently bound to the substrate. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 37, 38, 39, 40, 41)
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29. A method of stabilizing a thyroid hormone congener comprising:
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forming an azeotropic solution comprising dissolving a thyroid hormone congener hydrate in a solvent, wherein the azeotropic solution comprises the thyroid hormone congener dissolved in an azeotrope, the azeotrope comprising the solvent and a previously bound water from the thyroid hormone congener hydrate; wherein the solvent comprises 0.05% water by volume or less before forming the azeotrope, and forming an azeotropic suspension by adding a substrate to the azeotropic solution, wherein the substrate comprises a pharmaceutically suitable excipient; and depositing an anhydrous thyroid hormone congener onto the substrate to form a substrate powder by evaporating the azeotrope from the azeotropic suspension until the substrate powder is formed, wherein the substrate powder comprises at least one molecule of anhydrous thyroid hormone congener that was dehydrated from of the thyroid hormone congener hydrate during evaporating the azeotrope, and wherein the anhydrous thyroid hormone congener is non-covalently bound to the substrate. - View Dependent Claims (30, 31, 32, 33, 34, 35, 36)
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Specification