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含双氯芬酸钠的不同水/油微乳剂的比较:制备、表征、释放速率及皮肤刺激性研究

Comparison of different water/oil microemulsions containing diclofenac sodium: preparation, characterization, release rate, and skin irritation studies.

作者信息

Kantarci Gülten, Ozgüney Işik, Karasulu H Yeşim, Arzik Sevgi, Güneri Tamer

机构信息

Pharmaceutical Biotechnology Department, Faculty of Pharmacy, University of Ege, 35100 Bornova-Izmir, Turkey.

出版信息

AAPS PharmSciTech. 2007 Nov 2;8(4):E91. doi: 10.1208/pt0804091.

Abstract

The aim of the present study was to make a comparison of the in vitro release rate of diclofenac sodium (DS) from microemulsion (M) vehicles containing soybean oil, nonionic surfactants (Brij 58 and Span 80), and different alcohols (ethanol [E], isopropyl alcohol [I], and propanol [P]) as cosurfactant. The optimum surfactant:cosurfactant (S:CoS) weight ratios and microemulsion areas were detected by the aid of phase diagrams. Three microemulsion formulations were selected, and their physicochemical properties were examined for the pH, viscosity, and conductivity. According to the release rate of DS, M prepared with P showed the significantly highest flux value (0.059 +/- 0.018 mg/cm(2)/h) among all formulations (P < .05). The conductivity results showed that DS-loaded microemulsions have higher conductivity values (18.8-20.2 microsiemens/cm) than unloaded formulations (16.9-17.9 microsiemens/cm), and loading DS into the formulation had no negative effect on system stability. Moreover, viscosity measurements were examined as a function of shear rate, and Newtonian fluid characterization was observed for each microemulsion system. All formulations had appropriate observed pH values varying from 6.70 to 6.85 for topical application. A skin irritation study was performed with microemulsions on human volunteers, and no visible reaction was observed with any of the formulations. In conclusion, M prepared with P may be a more appropriate formulation than the other 2 formulations studied as drug carrier for topical application.

摘要

本研究的目的是比较双氯芬酸钠(DS)在含有大豆油、非离子表面活性剂(Brij 58和Span 80)以及不同醇类(乙醇[E]、异丙醇[I]和丙醇[P])作为助表面活性剂的微乳(M)载体中的体外释放速率。借助相图检测最佳表面活性剂:助表面活性剂(S:CoS)重量比和微乳区域。选择了三种微乳制剂,并对其pH值、粘度和电导率等理化性质进行了检测。根据DS的释放速率,在所有制剂中,用P制备的M显示出显著最高的通量值(0.059±0.018 mg/cm²/h)(P<.05)。电导率结果表明,载有DS的微乳的电导率值(18.8 - 20.2微西门子/厘米)高于未载药制剂(16.9 - 17.9微西门子/厘米),并且将DS载入制剂对系统稳定性没有负面影响。此外,对粘度测量值作为剪切速率的函数进行了检测,并且观察到每个微乳体系均具有牛顿流体特性。所有制剂的pH值在6.70至6.85之间,适合局部应用。对人体志愿者进行了微乳的皮肤刺激性研究,未观察到任何制剂有明显反应。总之,与所研究的其他两种制剂相比,用P制备的M作为局部应用的药物载体可能是更合适的制剂。

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