ELABORATION OF IBUPROFEN MICROCOMPOSITES IN SUPERCRITICAL CO_2

摘要

A multitude of pharmaceutical compounds are often insoluble or slightly soluble in aqueous media, Hence, the bioavailability of the drugs are low and their toxicity thresholds are close to the therapeutic dosage. A promising method to improve the bioavailability of such drugs is the reduction of the particle size by supercritical fluids. Their unique properties are used to produce pharmaceutical compounds as micron-sized particles with a narrow particle size distribution. The rapid expansion of supercritical solutions (RESS) process, without any organic solvents, was used to elaborate a non-steroidal anti-inflammatory drug: ibuprofen. Prior to attempting ibuprofen micronization, it was necessary to understand and establish drug behaviour in SC CO_2 and optimum conditions for producing micronic particles of ibuprofen by the RESS process. At 35℃ and 120 bar, discrete particles of ibuprofen ranging from 1 to 2 μm were formed. However, the decrease of its particle size leads to low delivery and release kinetics because of its poor manipulability and their high surface tensions. This is why, the same process (RESS) was performed at similar conditions to produce ibuprofen microcomposites by impregnation with α-lactose and β-cyclodextrin as excipient.