Vrána A, Andrýsek T
Department of Immunotherapeutic Products, IVAX-CR, a.s., Ostravská 29, 747 70 Opava 9, Czech Republic.
Biomed Pap Med Fac Univ Palacky Olomouc Czech Repub. 2001 Dec;145(2):9-15.
The effect of particle size on bioavailability of 9 different formulations with cyclosporine A was studied. A common feature of all the formulations was the ability to form submicron dispersions under dilution. The composition of individual formulations was chosen in such a way that they were based on same or similar excipients. For each formulation, pharmacokinetic study was carried out in beagle dogs. On groups of 10 dogs, the average AUC was evaluated. Particle size of formulations under dilution in water was measured by laser scattering method. According to the results of particle size measurement, the formulations were sorted out into groups of similar particle size distribution by use of two methods of multivariate statistical analysis. The average AUC within groups and between-groups was compared, and the effect of particle size on bioavailability was evaluated.
研究了粒径对9种不同环孢素A制剂生物利用度的影响。所有制剂的一个共同特点是在稀释条件下能够形成亚微米分散体。各个制剂的组成是这样选择的，即它们基于相同或相似的辅料。对每种制剂，在比格犬身上进行了药代动力学研究。在每组10只犬的群体中，评估了平均血药浓度-时间曲线下面积（AUC）。通过激光散射法测量制剂在水中稀释时的粒径。根据粒径测量结果，使用两种多元统计分析方法将制剂按粒径分布相似的组进行分类。比较了组内和组间的平均AUC，并评估了粒径对生物利用度的影响。
