Kumar L, Reddy M S, Shirodkar R K, Pai G K, Krishna V T, Verma R
Department of Pharmaceutics, Manipal College of Pharmaceutical Sciences, Manipal University, Manipal-576 104, India.
Department of Pharmaceutical Chemistry, Manipal College of Pharmaceutical Sciences, Manipal University, Manipal-576 104, India.
Indian J Pharm Sci. 2013 Sep;75(5):585-90.
Objective of the present study was to develop and evaluate vaginal films with essential in vitro studies. Films were developed using hydroxypropyl methylcellulose as a polymer and formulations were coded. The developed films were evaluated with Fourier transform infrared spectroscopy, drug content, viscosity, surface pH, thickness, mechanical characterisation and in vitro drug release study. Fourier transform infrared spectroscopy results confirmed that there is no chemical interaction between drug and stabilisers/excipients. The batch variation was not more than 5% for average thickness and weight of the films. The drug content for the prepared formulation was in the range of 72.32±0.18% to 94.48±0.54%. Viscosity of the formulations increased with the increase in concentration of polymer. Mechanical characterisation revealed that tensile strength and percentage elongation of the films improved as there is increase in degree of substitution of the polymer, but the values of modulus decreased which confirmed that all the prepared films are soft in nature. The in vitro study indicated that 1 and 2% concentrations of polymer are the least concentrations to control the release of drug whereas the 4% concentration of polymer is a good and more effective concentration to control the release. Only one prepared formulation released the drug by following anomalous transport whereas other film formulations released the fluconazole by following Fickian diffusion mechanism. Prepared vaginal films may be an important alternative for the treatment of vaginal candidiasis, because these prepared films suggest the benefits of controlled release of fluconazole at the site of absorption.
本研究的目的是通过必要的体外研究来开发和评估阴道薄膜。使用羟丙基甲基纤维素作为聚合物来制备薄膜，并对配方进行编码。对所开发的薄膜进行了傅里叶变换红外光谱、药物含量、粘度、表面pH值、厚度、机械性能表征以及体外药物释放研究。傅里叶变换红外光谱结果证实药物与稳定剂/辅料之间不存在化学相互作用。薄膜的平均厚度和重量的批次差异不超过5%。所制备配方的药物含量在72.32±0.18%至94.48±0.54%范围内。配方的粘度随着聚合物浓度的增加而增加。机械性能表征表明，随着聚合物取代度的增加，薄膜的拉伸强度和伸长率有所提高，但模量值下降，这证实了所有制备的薄膜本质上都是柔软的。体外研究表明，1%和2%浓度的聚合物是控制药物释放的最低浓度，而4%浓度的聚合物是控制释放的良好且更有效的浓度。只有一种制备的配方通过非正规转运释放药物，而其他薄膜配方通过菲克扩散机制释放氟康唑。制备的阴道薄膜可能是治疗阴道念珠菌病的重要替代方法，因为这些制备的薄膜显示了在吸收部位控制释放氟康唑的益处。
