Lenhard G, Kieferndorf U, Berner G, Engels B, Vögtle-Junkert U
Institut für Klinische Forschung, Overath.
Arzneimittelforschung. 1990 Dec;40(12):1358-62.
In an open controlled randomized cross-over study in 16 healthy male and female volunteers the bioavailability of ibuprofen (CAS 15687-27-1) sugar-coated tablets (Dolo-Dolgit) was tested versus film-coated tablets containing ibuprofen 600 mg. As it results from the AUC evaluation, the bioavailability of both preparations is very good and almost identical. The ibuprofen concentrations achieved after administration of the test preparation, however, are significantly higher (Cmax = 52.03 micrograms/ml) than those achieved after the reference preparation showing a Cmax of 40.32 micrograms/ml. The tmax of 1.0 h is also significantly shorter than after the reference preparation (tmax = 1.5 h). The t1/2 beta after both the test and the reference preparation is within the known range, i.e. 1.8 h and 1.4 h, respectively. Even in long-term treatment with high dosages, administered 3-4 times daily, there is no accumulation of the active ingredient. Concerning the therapeutic relevance, special attention is to be given to the different time-dependent drug concentrations in the central compartment and in the target compartment. Both the higher Cmax and the shorter tmax achieved following administration of the test preparation are of therapeutic relevance.
在一项针对16名健康男性和女性志愿者的开放性对照随机交叉研究中,对布洛芬(CAS 15687-27-1)糖衣片(多洛-多尔吉特)与含600毫克布洛芬的薄膜包衣片的生物利用度进行了测试。根据AUC评估结果,两种制剂的生物利用度都非常好且几乎相同。然而,服用测试制剂后达到的布洛芬浓度(Cmax = 52.03微克/毫升)明显高于参比制剂,参比制剂的Cmax为40.32微克/毫升。测试制剂的达峰时间(tmax)为1.0小时,也明显短于参比制剂(tmax = 1.5小时)。测试制剂和参比制剂的消除半衰期(t1/2β)均在已知范围内,分别为1.8小时和1.4小时。即使每日3 - 4次高剂量长期治疗,活性成分也不会蓄积。关于治疗相关性,需要特别关注中央室和靶室中不同的时间依赖性药物浓度。服用测试制剂后达到的较高Cmax和较短tmax均具有治疗相关性。