Methods of improving pharmaceutical substance solubilization and products thereof
AssigneeCosci Med-Tech Co. Ltd.
InventorsZheng Tang, Jingang Wang, Chen Yang
Life of this patent
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Abstract
Methods for improving solubility of active pharmaceutical ingredients (APIs) through co-attriting the APIs with select excipients, especially solubility enhancing excipients, and the products prepared by the methods, are disclosed. Pharmaceutical compositions containing co-attrited mixture of an API with a solubility enhancing excipient and use of the pharmaceutical compositions for treatment of diseases or disorders are also disclosed.
Claims30
A method of increasing solubility of an active pharmaceutical ingredient (API), comprising co-attriting a dry or substantially dry mixture of the API and a solubility-enhancing excipient with a kneading or extrusion device at a temperature below the melting point of the API to form a co-attrition mixture, and applying an attrition force sufficient to increase the API solubility by at least 20%, preferably by at least 50%, and more preferably by at least 150%, wherein the API content in the co-attrition mixture ranges from 10% to 90% by weight.
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A pharmaceutical composition comprising an extruded or kneaded mixture of an active pharmaceutical ingredient (API) with a solubility enhancing excipient, wherein the API is poorly soluble drug substance or heat-sensitive drug substance, possesses enhanced solubility and/or bioavailability and maintains bioactivity in the extruded or kneaded mixture;
- and wherein the API solubility is increased by at least 20% through an extruding or kneading process with the solubility enhancing excipient.
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Dependencies are inferred from the claim text.