Molina-Martinez I T, Herrero R, Gutiérrez J A, Iglesias J M, Fábregas J L, Martinez-Tobed A, Cadorniga R
Department of Pharmacy and Pharmaceutical Technology, Faculty of Pharmacy, Universidad Complutense, Madrid, Spain.
J Pharm Sci. 1993 Feb;82(2):211-3. doi: 10.1002/jps.2600820220.
We studied the influence of administration route on the biopharmaceutical behavior of etodolac. The levels obtained in plasma when the same dose of etodolac is administered orally (tablets, dosage form A) and rectally (suppositories, dosage form B) were compared. The study was done in a crossover design with healthy volunteers of both sexes, of average build, and younger than 35 years of age. From the concentration in plasma-time data, the maximum concentration in plasma (Cmax), time to Cmax, and area under the curve up to the last measurable concentration (AUC0t) or infinity (AUC 0 infinity) were calculated and compared by analysis of variance. With the exception of Cmax, no significant differences between treatments were found in the rest of the parameters. Finally, with formulation A (tablets) as a reference, the relative bioavailability was established, on the basis of the ratio (B:A) of AUC0t and AUC 9 infinity, within the range 100 +/- 20%. The results indicate that the two routes of administration are bioequivalent and that the rectal route is an alternative administration route for etodolac.
我们研究了给药途径对依托度酸生物药剂学行为的影响。比较了口服相同剂量依托度酸（片剂，剂型A）和直肠给药（栓剂，剂型B）后血浆中的药物水平。该研究采用交叉设计，受试者为年龄小于35岁、平均体型的健康男女志愿者。根据血浆浓度-时间数据，计算血浆中的最大浓度（Cmax）、达峰时间以及直至最后可测浓度的曲线下面积（AUC0t）或至无穷大的曲线下面积（AUC0∞），并通过方差分析进行比较。除Cmax外，其余参数在各治疗组间未发现显著差异。最后，以制剂A（片剂）为参比制剂，根据AUC0t和AUC0∞的比值（B:A）确定相对生物利用度，其范围为100±20%。结果表明，两种给药途径具有生物等效性，直肠给药途径是依托度酸的一种替代给药途径。
