Doluisio J T, Smith R B, Chun A H, Dittert L W
J Pharm Sci. 1978 Nov;67(11):1586-8. doi: 10.1002/jps.2600671122.
Serum pentobarbital levels following administration of the sodium salt as a 100-mg capsule orally and as two 120-mg suppository formulations (A and B) rectally were measured. From these data and previously determined kinetic constants after intravenous administration, the absorption rates and bioavailability of pentobarbital from each dosage form were determined. All three dosage forms were 100% absorbed. Peak serum pentobarbital levels occurred at 1, 4, and 10 hr for the capsule, Suppository A, and Suppository B, respectively. In vitro studies agreed with the serum data in that Suppository A released drug in an in vitro aqueous pH 1.4 system at a much greater rate that Suppository B. The capsule and Suppository A both appeared to be absorbed by simple first-order processes; however, Suppository B had a complex absorption pattern, which was modeled using sequential zero-order and first-order absorption.
测量了口服100毫克胶囊形式的戊巴比妥钠盐以及经直肠给予两种120毫克栓剂制剂(A和B)后的血清戊巴比妥水平。根据这些数据以及先前静脉给药后确定的动力学常数,确定了每种剂型中戊巴比妥的吸收速率和生物利用度。所有三种剂型的吸收率均为100%。胶囊、栓剂A和栓剂B的血清戊巴比妥峰值水平分别出现在1小时、4小时和10小时。体外研究与血清数据一致,即栓剂A在体外pH 1.4的水性系统中释放药物的速率比栓剂B快得多。胶囊和栓剂A似乎都通过简单的一级过程吸收;然而,栓剂B具有复杂的吸收模式,使用连续零级和一级吸收进行建模。