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Estimation of Local Bioavailability for Transdermally Applied Drugs by the Monitoring of Unboud-form Drug Concentrations in the Skin

通过监测皮肤中未成型药物浓度估计透皮给药药物的局部生物利用度

基本信息

批准号：
15590132
负责人：
KUROSAKI Yuji
金额：
$ 2.3万
依托单位：
OKAYAMA UNIVERSITY
依托单位国家：
日本
项目类别：
Grant-in-Aid for Scientific Research (C)
财政年份：
2003
资助国家：
日本
起止时间：
2003 至 2004
项目状态：
已结题

项目摘要

Estimation of local bioavailability for transdermally applied drugs by the monitoring of unboud-form drug concentrations in the skin was studied.1.Estimation of pharmacokinetic local bioavailability(1)Application of Muliti-batch Zero-Net Flux microdialysisMuliti-batch Zero-Net Flux microdialysis method enables to shorten the sampling interval. The usefulness of this method in monitoring unboud-formdrug concentrations in the skin in vivo was clarified.(2)Application of Lipo-microdialysis (Lipo-MD)Photodegradation products of ketoprofen after the dermal application were detected by the use of Lipo-MD method in vivo.2.Estimation of pharmacodynamic local bioavailabilityIn the triphasic vascular response induced by bradykinin in rat perfused mesenteric vascular beds, serial responses interfere each other. Information derived from the kinetical analysis is valuable to discuss the mechanism of action obtained by pharmacodynamic analysis.3.Antibody-incorporated microdialysisAntibody-incorporated microdialysis enables to increase the relative recovery for teicoplanin 2 to 5 times compared with that in the conventional microdialysis.4.In vivo monitoring for implanted controlled-release DDS in the skinLocal pharamacokinetic profiles were determined in two positions by microdialysis. The profile determined at 10 mm away from the DDS was completely different from that determined just beside the DDS. The importance of the precise estimation of local pharmacokinetics of unboud-form drugs was clarified.

研究了通过监测皮肤中未溶出的药物浓度来估算透皮给药药物的局部生物利用度。1.药代动力学局部生物利用度的估算(1)多批零净通量微透析法的应用多批零净通量微透析方法可以缩短采样间隔。 (2)脂质体微透析(Lipo-MD)的应用采用Lipo-MD法检测体内酮洛芬经皮后的光降解产物。2.药效局部生物利用度的估计在由酮洛芬引起的三相血管反应中。缓激肽在大鼠肠系膜血管床灌注中，系列反应相互干扰。动力学分析得出的信息对于讨论药效学分析获得的作用机制具有重要价值。3.抗体掺入微透析与传统微透析相比，抗体掺入微透析能够将替考拉宁的相对回收率提高2至5倍。4.皮肤中植入控释DDS的体内监测局部通过微透析测定两个位置的药代动力学特征。在距 DDS 10 mm 处确定的轮廓与在 DDS 旁边确定的轮廓完全不同。阐明了精确估计未成型药物的局部药代动力学的重要性。