W/O/W multiple emulsions containing nitroimidazole derivates for vaginal delivery
W/O/W multiple emulsions containing nitroimidazole derivates for vaginal delivery
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DOI：
10.1080/10717540601067463
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发表时间：
2007-03-01
期刊：
影响因子：
6
通讯作者：
Koseoglu, Kamil
中科院分区：
文献类型：
--
作者：
Ozer, Ozgen;Ozyazici, Mine;Koseoglu, Kamil
我们研究的目的是配制一种稳定的多重乳剂，含有两种硝基咪唑衍生物甲硝唑 (MT) 和奥硝唑 (OR)，用于阴道治疗。 MT和OR分别位于多重乳液的内相和外相，并在磷酸盐（pH 7）和乳酸缓冲液（pH 4.5）溶液中进行体外释放研究，以更好地研究pH和活性物质位置对释放的影响。在用 Technethium-99m (Tc-99m) 标记 NIT 和 OR 后，在兔子中进行了成像研究，以评估体内吸收特性。当MT和OR被引入到多重乳液的内相中时，在碱性介质中从多重乳液中释放的MT和OR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。 NIT从阴道上皮的吸收速度比OR快。我们观察到，特别是在碱性介质中，发现高释放量，这有利于在碱性 pH 值中出现的阴道感染。我们得出的结论是，W/O/W多重乳剂在阴道局部有效，并且可以作为新的药物载体系统引入。用于阴道分娩。
The aim of our study was to formulate a stable multiple emulsions containing two nitromidazole 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 NIT and OR with Technethium-99m (Tc-99m) 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 NIT 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.