Ahmed I S, Fatahalla F A
Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Egypt.
Drug Dev Ind Pharm. 2007 May;33(5):505-11. doi: 10.1080/03639040601150237.
The pharmacokinetics of ketoprofen from a fast-dissolving lyophilized tablet (LT), which need not be swallowed, as compared to an immediate release (IR) tablet as reference after single oral dose (25 mg) administration was determined in six healthy subjects aged between 25-40 years using a randomized crossover design. In this study, the rate and extent of absorption of ketoprofen were found to be very different after administration of the LT and the IR tablet. The rate of absorption of ketoprofen from LT was significantly faster than that of IR tablet and had significantly higher Cmax (by about 50%) and earlier tmax (by 15 min), whereas the extent of absorption expressed by AUC was about 68% higher as compared to the IR tablet. The relative bioavailability (frel) of the LT compared with the IR tablet was 168%. The difference between the two formulations for half-life and MRT were statistically significant (p<0.05). The tolerance of the two tested formulations was excellent. Ketoprofen LT remained physically and chemically stable for 12 months at 25 degrees C and 60% relative humidity.
在6名年龄在25至40岁之间的健康受试者中，采用随机交叉设计，测定了与速释（IR）片作为参比制剂相比，无需吞咽的速溶冻干片（LT）单次口服给药（25 mg）后酮洛芬的药代动力学。在本研究中，发现服用LT和IR片后酮洛芬的吸收速率和程度有很大差异。LT中酮洛芬的吸收速率明显快于IR片，Cmax显著更高（约高50%），tmax更早（早15分钟），而AUC表示的吸收程度比IR片高约68%。LT与IR片相比的相对生物利用度（frel）为168%。两种制剂在半衰期和平均滞留时间方面的差异具有统计学意义（p<0.05）。两种受试制剂的耐受性良好。酮洛芬LT在25℃和60%相对湿度下12个月内保持物理和化学稳定性。
