Ozyazici Mine, Turgut Evren H, Taner Memduh S, Köseoglu Kamil, Ertan Gökhan
Faculty of Pharmacy, Department of Pharmaceutical Technology, University of Ege, Bornova, Izmir, Turkey.
J Drug Target. 2003 Apr;11(3):177-85. doi: 10.1080/10611860310001603814.
Vaginal suppository formulations of metronidazole were prepared using six different bases as Witepsol H15, Cremao, Ovucire WL2944, Ovucire WL3264, PEG 1500, PEG 6000. Three different dissolution methods were used to evaluate the in vitro drug release from the suppositories. The diffusion studies were performed through synthetic (cellophane) and natural membrane (rabbit vagina), but the drug did not show good permeation characteristics from natural membrane. Ovucire WL3264 suppositories of metronidazole labeled with 99mTc (Tecnetium-99m) were used for the vaginal absorption and biodistribution studies in the rabbits. Scintigraphic images were collected after vaginal administration of the labeled suppositories using SPECT gamma fitted with a low energy, high-resolution parallel hole collimator. The labeled drug showed high biodistribution in urine beside vaginal site. The results of this study suggested that the Ovucire WL3264 suppository of metronidazole prepared for vaginal infections could also be effective in the urinary infections.
采用六种不同基质（如Witepsol H15、Cremao、Ovucire WL2944、Ovucire WL3264、聚乙二醇1500、聚乙二醇6000）制备了甲硝唑阴道栓剂。使用三种不同的溶出方法来评估栓剂的体外药物释放。通过合成膜（玻璃纸）和天然膜（兔阴道）进行扩散研究，但药物在天然膜上未表现出良好的渗透特性。用99m锝（锝-99m）标记的甲硝唑Ovucire WL3264栓剂用于兔的阴道吸收和生物分布研究。使用配备低能、高分辨率平行孔准直器的单光子发射计算机断层扫描（SPECT）γ相机在阴道给药标记栓剂后采集闪烁图像。标记药物除在阴道部位外，在尿液中也显示出较高的生物分布。本研究结果表明，为治疗阴道感染而制备的甲硝唑Ovucire WL3264栓剂对泌尿系统感染也可能有效。
