张梅 赵维娟 王金平 (北京军区临床药物研究所 北京100700)
摘 要 目的：研究丁螺环酮透皮贴剂给药的药物动力学及生物利用度。方法：以丁螺环酮片剂为对照，采用HPLC法测定家兔随机交叉使用丁螺环酮贴剂和片剂在相同单剂量给药后的血药浓度，采用3p97软件处理数据，进行药物动力学及生物利用度的研究。结果：与片剂比较，贴剂达峰时间较长，但可维持较长时间平稳的血药浓度，在1.5～8 h内血药浓度保持在34.190±3.382 ng·ml-1左右；贴剂和片剂的AUC0→∞分别为（403.741±108.828）和（102.031±39.570）h·ng·ml-1,二者有极显著性差异(P<0.01)，贴剂相对生物利用度是片剂生物利用度的3.96倍。结论：外用贴剂相对口服片剂而言，有较高的生物利用度。
关键词 丁螺环酮贴剂；丁螺环酮片剂；透皮吸收；药物动力学；生物利用度
中图分类号：R969.1
文献标识码：A
文章编号：1008-049X(2007)04-0308-03
Study on the Pharmacokinetics of Buspirone Transdermal Patch
Zhang Mei，Zhao Weijuan，Wang Jinping (Pharmaceutical Institute of Beijing Military Command, Beijing 100700,China)
ABSTRACT Objective: To study the pharmacokinetics of buspirone transdermal patch.Method: The rabbits were randomized to receive a single crossover dose of test patch or oral tablet. The plasma Buspirone concentration data were determined by HPLC. Pharmacokinetics and bioavailability of buspirone were calculated by 3p97 program.Result: The tmax of the patch was longer than the tablet, but the drug level was stable, which was almost (34.19±3.382)ng·ml-1 after giving drug from 1.5 h to 8 h. There was significantly differences（P＜0.01） between the AUC0→∞of the patch(403.741±108.828) and the table(102.031±39.570) h·ng·ml-1. The relative bioavailability of the patch was 3.96 times as that of the tablet.Conclusion: The bioavailability of buspirone in the patch is better than the tablet.
KEY WORDS Buspirone patch； Buspirone tablet; Transdermal delivery； Pharmacokinetics; Bioavailability
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