Получение микронизированной субстанции ибупрофена и оценка его биодоступности

Micronized ibuprofen, which differs from the original substance by reduced sizes of the crystals has been obtained using Mini Spray Dryer B-290 (BUCHI Switzerland) designed for drying of aqueous solutions and suspensions. The bioavailability of ibuprofen in the form of peroral capsules containing micronized substance (with an average crystal size of 30 microns) and capsules containing commercial ibuprofen substance (crystal size 150 microns) has been studied in Chinchilla rabbits. The concentration of unchanged ibuprofen in blood serum was determined by HPLC with spectrophotometric detection at 220 nm. The drug detection limit was 0.1 μg/ml. Ibuprofen was extracted from rabbit blood serum by using liquid – liquid extraction. The extraction of ibuprofen from serum was on average 78%. It has been found that the bioavailability of micronized ibuprofen increases more than 2 times as compared to the commercial substance (with an average crystal size of 150 microns). The rate of ibuprofen absorption and the rate of elimination from the systemic circulation remain the same.