Kees F, Dehner R, Dittrich W, Raasch W, Grobecker H
Lehrstuhl für Pharmakologie Universität Regensburg.
Arzneimittelforschung. 1990 Sep;40(9):1039-43.
The bioavailability of doxycycline (Doxy-Diolan 100 tablets, test, active substances: 100 mg doxycyclin per tablet) was compared with that of another commercially available tablet-formulation containing the same active substance (reference). In a cross-over study, 16 young healthy male volunteers were administered in fasting state orally by one tablet containing 100 mg active substance. The concentrations of doxycycline were determined in plasma and saliva by a high-performance liquid chromatographic assay. Mean maximum plasma concentration (cmax +/- standard deviation) of doxycycline were 1.57 +/- 0.40 micrograms/ml (test) and 1.59 +/- 0.38 micrograms/ml (reference), respectively, and were reached 1.47 +/- 0.55 h and 1.66 +/- 0.57 h after administration. Plasma half-lives were 16.6 +/- 2.9 h and 16.8 +/- 3.0 h, the areas under the plasma concentration-time curves (AUC0-00) 29.3 +/- 4.5 mg/l.h and 29.7 +/- 4.4 mg/l.h. The concentration of doxycycline in saliva were low, median maximum concentrations of 50 ng/ml were measured 1-2 h after administration. The statistical evaluation revealed bioequivalence between both drugs.
将多西环素(强力霉素片100,试验品,活性物质:每片含100mg多西环素)的生物利用度与另一种含有相同活性物质的市售片剂剂型(参比制剂)进行比较。在一项交叉研究中,16名年轻健康男性志愿者在禁食状态下口服一片含有100mg活性物质的片剂。通过高效液相色谱分析法测定血浆和唾液中的多西环素浓度。多西环素的平均最大血浆浓度(Cmax±标准差)分别为1.57±0.40μg/ml(试验品)和1.59±0.38μg/ml(参比制剂),给药后分别在1.47±0.55小时和1.66±0.57小时达到。血浆半衰期分别为16.6±2.9小时和16.8±3.0小时,血浆浓度-时间曲线下面积(AUC0-∞)分别为29.3±4.5mg/l·h和29.7±4.4mg/l·h。唾液中的多西环素浓度较低,给药后1-2小时测得的最大浓度中位数为50ng/ml。统计评估显示两种药物具有生物等效性。