Penjuri Subhash Chandra Bose, Damineni Saritha, Ravouru Nagaraju, Poreddy Srikanth Reddy
Mnr College Of Pharmacy, Department Of Pharmaceutics, Telangana, India.
Sultan-Ul-Uloom College Of Pharmacy, Department Of Pharmaceutics, Telangana, India.
Turk J Pharm Sci. 2017 Aug;14(2):108-119. doi: 10.4274/tjps.60352. Epub 2017 Aug 15.
The objective of the present study was to enhance the solubility, dissolution and hence anti-inflammatory activity of poorly soluble drug indomethacin (IMN) by formulating into self emulsifying systems.
Self emulsifying formulations were prepared using capmul MCM as oil, tween 80 as surfactant, transcutol P as cosurfactant. Fourier transform infrared spectroscopy and differential scanning calorimetry studies were conducted to know the interaction between drug and excipients. Pseudo ternary phase diagrams were constructed using surfactant and cosurfactant in 1:1 to 1:4 and 2:1 to 4:1 to know the efficient self emulsification region. The formulations were evaluated for their particle size, zeta potential, refractive index, viscosity and cloud point. dissolution studies were conducted in one part of pH 7.2 phosphate buffer and four parts of water. The pharmacokinetic parameters were analysed by Win Nonlin software.
The self emulsification was higher with the ratios 2:1, 3:1 and 1:2 of surfactant and co surfactant and the IMN formulations were prepared. The formulations were stable at different pH and dilutions. The globule size was in the range of 184.1 nm to 340.5 nm, as the ratio of oil, surfactant and cosurfactant mixture has varied effects on the size of globule. The negative charge on the globules of all formulations attributes their stability. The optimized formulation showed better release as compared to marketed product. The AUC of the optimised Self-Emulsifying Drug Delivery System was significantly higher than the marketed product.
Thus, from the present research, self emulsifying systems of IMN provide a useful alternative to enhance dissolution and hence anti inflammatory activity.
本研究的目的是通过将难溶性药物吲哚美辛（IMN）制成自乳化系统来提高其溶解度、溶出度，从而增强其抗炎活性。
以辛酸癸酸甘油三酯为油相、吐温80为表面活性剂、丙二醇为助表面活性剂制备自乳化制剂。进行傅里叶变换红外光谱和差示扫描量热法研究以了解药物与辅料之间的相互作用。使用表面活性剂和助表面活性剂以1:1至1:4以及2:1至4:1的比例构建伪三元相图，以确定有效的自乳化区域。对制剂的粒径、zeta电位、折射率、粘度和浊点进行评估。在一份pH 7.2磷酸盐缓冲液和四份水的混合液中进行溶出度研究。通过Win Nonlin软件分析药代动力学参数。
表面活性剂与助表面活性剂比例为2:1、3:1和1:2时自乳化效果更佳，并据此制备了IMN制剂。这些制剂在不同pH值和稀释度下均稳定。随着油相、表面活性剂和助表面活性剂混合物的比例对液滴大小产生不同影响，液滴大小在184.1 nm至340.5 nm范围内。所有制剂液滴上的负电荷赋予了它们稳定性。与市售产品相比，优化后的制剂显示出更好的释放效果。优化后的自乳化药物递送系统的AUC显著高于市售产品。
因此，从本研究来看，IMN的自乳化系统为提高溶出度从而增强抗炎活性提供了一种有用的替代方法。
