油酸预处理改善氯沙坦透皮渗透的体外观察和体内预测

Annas Binarjo, A. Nugroho
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引用次数: 1

摘要

*通讯作者电子邮件:annasbinarjo@yahoo.co.id观察油酸对氯沙坦透皮渗透的影响,探讨其作为化学促进剂的作用。使用15%丙二醇作为增溶剂,在pH 5.0的柠檬酸缓冲液中制备两种浓度水平的氯沙坦钾溶液,即2mg/mL和10mg/mL。使用雄性Wistar大鼠皮肤作为膜,在垂直扩散sel中测试在油酸预处理和不油酸预处理1小时的情况下从这样的溶液中的氯沙坦转运30小时。基于滞后时间扩散法对输运剖面进行了分析。结果表明,油酸预处理对氯沙坦的渗透速率和浓度为2mg/mL的氯沙坦钾的渗透效率没有影响。然而,对于10mg/mL的氯沙坦钾浓度,这种预处理使氯沙坦的渗透速率和效率分别提高了21和23倍。据预测,通过在正常应用区域的这种转运改善,氯沙坦在透皮给药中可以达到最低有效血浆浓度。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Improvement of Losartan Transdermal Permeation using Oleic Acid Pretreatment: in Vitro Observation and in Vivo Prediction
*Corresponding author Email: annasbinarjo@yahoo.co.id ABSTRACT The effect of oleic acid on losartan transdermal permeation has been observed to explore its ability as chemical enhancer. Potassium losartan solutions in citric buffer pH 5.0 were made in two levels of concentration i.e. 2 mg/mL and 10 mg/mL using propylene glycol 15% as solubilizing agent. Losartan transport from such solutions with and without oleic acid one hour pretreatment were tested using male Wistar rat skin as a membrane for 30 hours in vertical diffusion sel. The transport profiles were analyzed based on the lag time diffusion method. It is showed that oleic acid pretreatment did not effect on losartan permeation rate and efficiency of 2 mg/mL potassium losartan concentration. However, such pretreatment enhanced losartan permeation rate and efficiency 21 and 23-fold higher respectively for 10 mg/mL the potassium losartan concentration. It is predicted that losartan minimum effective plasma concentration can be achieved in transdermal administration through this transport improvement in normal application area.
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