Ozer Ozgen, Ozyazici Mine, Tedajo Muriel, Taner Memduh S, Köseoglu Kamil
Ege University, Faculty of Pharmacy, Department of Pharmaceutical Technology, Bornova-Izmir, Turkiye.
Drug Deliv. 2007 Mar;14(3):139-45. doi: 10.1080/10717540601067463.
The aim of our study was to formulate a stable multiple emulsions containing two nitroimidazole derivates, metronidazole (MT) and ornidazole (OR), for vaginal therapy. MT and OR were located internal and external phases of multiple emulsion, respectively, and the in vitro release studies were realized in phosphate (pH 7) and lactate buffer (pH 4.5) solutions to investigate better the effect of pH and location of active substance on the release. The imaging studies were realized in rabbits following labeling MT and OR with Technethium-99m ((99m)Tc) to evaluate the in vivo absorption characteristics. The percentage of MT and OR released from the multiple emulsions in alkaline media were 3.2- and 2.8-fold greater than that observed in acidic media, respectively, when they were introduced in the internal phase of the multiple emulsions. The absorption rate of MT from vaginal epithelium was faster than OR. We observed that especially in alkaline medium a high release was found that was convenient for the vaginal infections seen in the alkaline pH. We concluded that W/O/W multiple emulsions were locally effective in vagina and they could be introduced as a new drug carrier system for vaginal delivery.
我们研究的目的是制备一种含有两种硝基咪唑衍生物甲硝唑（MT）和奥硝唑（OR）的稳定复乳，用于阴道治疗。MT和OR分别位于复乳的内相和外相，通过在磷酸盐（pH 7）和乳酸盐缓冲液（pH 4.5）溶液中进行体外释放研究，以更好地研究pH值和活性物质位置对释放的影响。在用99m锝（99mTc）标记MT和OR后，在兔子身上进行成像研究，以评估体内吸收特性。当MT和OR被引入复乳的内相时，它们在碱性介质中从复乳中释放的百分比分别比在酸性介质中观察到的高3.2倍和2.8倍。MT从阴道上皮的吸收速率比OR快。我们观察到，特别是在碱性介质中，释放量很高，这对于碱性pH值下出现的阴道感染是有利的。我们得出结论，W/O/W复乳在阴道局部有效，可作为一种新的阴道给药药物载体系统引入。
