Gammans R E, Mayol R F, Mackenthun A V, Sokya L F
Biopharm Drug Dispos. 1985 Apr-Jun;6(2):139-45. doi: 10.1002/bdd.2510060205.
Dose dependency of the pharmacokinetics of buspirone, a new anxiolytic agent, was tested in 24 healthy volunteers. Each subject received 10, 20, and 40 mg doses according to a randomized, three-way crossover design with a 7-day interval between treatments. Buspirone AUC values at 10, 20, and 40 mg doses were in the ratio of 1:1.7:3.5 while Cmax values had a ratio of 1:1.9:3.7. The dose normalized (10 mg basis) AUC and Cmax values, Tmax values, and half-lives were not significantly different (p greater than 0.05) among the doses. Buspirone half-life did not change as a function of dose (mg kg-1). It was concluded that buspirone exhibits linear pharmacokinetics following doses in the therapeutic range.
在24名健康志愿者身上测试了新型抗焦虑药丁螺环酮的药代动力学剂量依赖性。每位受试者按照随机、三交叉设计接受10毫克、20毫克和40毫克剂量的药物，治疗间隔为7天。丁螺环酮10毫克、20毫克和40毫克剂量时的AUC值之比为1:1.7:3.5，而Cmax值之比为1:1.9:3.7。各剂量之间剂量标准化（以10毫克为基础）的AUC和Cmax值、Tmax值及半衰期无显著差异（p大于0.05）。丁螺环酮的半衰期不随剂量（毫克/千克）而变化。得出的结论是，丁螺环酮在治疗范围内的剂量下呈现线性药代动力学。
