OBJECTIVE: To study the formation technology of Ibuprofen dropping pills and determine the dissolution in vitro. METHODS: Based on single factor test and with the spherical degree, drug-loading rate and pill weight variation as the evaluated indexes, response surface methodology was employed to screen the ratios of drug to matrix, drug solution temperatures and cryogenic temperatures in the formation technology, and verification tests were conducted. The dissolution in vitro of the dropping pills prepared by the optimal technology was investigated and compared with that of the preparations sold in the market. RESULTS: The optimal formation technology of Ibuprofen dropping pills was as follows as the ratio of drug to matrix of 1 ∶ 6, drug solution temperature of 83 ℃ and cryogenic temperature of 7.3 ℃. In the verification tests, the self-made dropping pills demonstrated a spherical degree of 0.945 9, drug-loading rate of 99.82%, pill weight variation of 0.040 28 and drug-loading capacity of 30 mg/pill, with the actual comprehensive score of 0.972 5, deviating from the theoretical one (0.980 0) by 0.771 2% (RSD<1.5%, n=3). The dropping pills prepared had a dissolution rate of 25.36% at 5 min and an accumulated dissolution rate up to 90.12% at 30 min, similar with the Ibuprofen tablets sold in the market in drug release in vitro (f2=54.91), conforming to a first-order kinetic equation. CONCLUSIONS: The optimized formation technology is simple, stable, feasible and well reproducible, and the dropping pills which are prepared by such technology can release drug quickly.
关键词
布洛芬滴丸响应面法成型工艺体外溶出度
Keywords
IbuprofenDropping pillsResponse surface methodologyFormation technologyDissolution in vitro