Nulman Irena, Koren Gideon
The Motherisk Program, Division of Clinical Pharmacology & Toxicology, The Hospital for Sick Children, Toronto, Canada.
Can J Clin Pharmacol. 2009 Fall;16(3):e400-6. Epub 2009 Oct 29.
The delayed-release combination of doxylamine succinate and pyridoxine hydrochloride was the most commonly used antiemetic (Bendectin) approved by FDA for nausea and vomiting of pregnancy (NVP) until its removal of the market in 1983. The drug is widely used today in Canada (Diclectin). The pharmacokinetics of Diclectin has never been described in humans.
To compare the pharmacokinetics of Diclectin to oral solutions of its two components.
A randomized, cross over, open label design, comparing the pharmacokinetics of Diclectin to those of the oral solutions of the two components in 18 healthy adult, non pregnant women of childbearing age.
Diclectin exhibited similar oral bioavailability to those of the oral solutions. In contrast, the time-to-peak, (Tmax), reflecting the rate of absorption, was 3-6 times longer for the two components of the delayed-release drug confirming its delayed-release characteristics.
The pharmacokinetic profile of Diclectin well explains its documented delayed efficacy.
琥珀酸多西拉敏和盐酸吡哆醇的缓释组合曾是美国食品药品监督管理局（FDA）批准用于治疗妊娠恶心和呕吐（NVP）的最常用止吐药（敏克静），直到1983年该药退市。如今，这种药物在加拿大仍被广泛使用（迪克莱汀）。迪克莱汀的药代动力学在人体中从未被描述过。
比较迪克莱汀与其两种成分的口服溶液的药代动力学。
采用随机、交叉、开放标签设计，比较18名健康成年非孕育龄妇女中迪克莱汀与其两种成分口服溶液的药代动力学。
迪克莱汀的口服生物利用度与两种成分的口服溶液相似。相比之下，反映吸收速率的达峰时间（Tmax），对于缓释药物的两种成分来说要长3至6倍，证实了其缓释特性。
迪克莱汀的药代动力学特征很好地解释了其已记录的延迟疗效。
