Increasing permeation for pre-gastric absorption of active pharmaceutical ingredients
A pharmaceutical composition comprises a pharmaceutically effective amount of a biopharmaceutics classification system (BCS) Class II active pharmaceutical ingredient (API) or a pharmaceutically acceptable salt or solvate thereof, having a solubility of less than 0.1mg/ml and a log P value greater t...
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Zusammenfassung: | A pharmaceutical composition comprises a pharmaceutically effective amount of a biopharmaceutics classification system (BCS) Class II active pharmaceutical ingredient (API) or a pharmaceutically acceptable salt or solvate thereof, having a solubility of less than 0.1mg/ml and a log P value greater than 2.5; and a permeation enhancer comprising at least one selected from the group of counterions, a pH modifier, a surfactant with a hydrophilic lipophilic balance (HLB) greater than 10, a bile salt, a micelle, or a fatty acid; a matrix former, and a structure former. The active may be carvedilol. The permeation enhancer may be a poloxamer, a polyoxyethylene-(4)-sorbitan monolaurate, dodecyl-B-D-maltoside, sodium cholate, sodium lauryl sulphate, capric acid, citric acid, aspartic acid, alanine, arginine, lysine, benzoic acid, or glycine. The composition may be an orally dissolvable tablet (ODT). The matrix former may be gelatin, and the structure former may be mannitol. Alternative compositions comprising BCS Class II and III actives are also disclosed, including piroxicam, famotidine and atenolol. |
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