Department of Chemistry and Center of Advanced Studies in Chemistry, Panjab University, Chandigarh 160014, India.
AAPS PharmSciTech. 2010 Mar;11(1):143-53. doi: 10.1208/s12249-009-9356-5. Epub 2010 Jan 20.
The microemulsion composed of oleic acid, phosphate buffer, ethanol, and Tween (20, 40, 60, and 80) has been investigated in the presence of antitubercular drugs of extremely different solubilities, viz. isoniazid (INH), pyrazinamide (PZA), and rifampicin (RIF). The phase behavior showing the realm of existence of microemulsion has been delineated at constant surfactant/co-surfactant ratio (K (m) = 0.55) with maximum isotropic region resulting in the case of Tween 80. The changes in the microstructure of Tween 80-based microemulsion in the presence of anti-TB drugs have been established using conductivty (sigma) and viscosity (eta) behavior. The optical microscopic images of the system help in understanding the effect of dilution and presence of drug on the structure of microemulsion. Partition coefficient, particle size analysis, and spectroscopic studies (UV-visible, Fourier transform infrared, and 1H NMR) have been performed to evaluate the location of a drug in the colloidal formulation. To compare the release of RIF, PZA, and INH from Tween 80 formulation, the dissolution studies have been carried out. It shows that the release of drugs follow the order INH>PZA>RIF. The kinetics of the release of drug has been analyzed using the Korsmeyer and Peppas equation. The results have given a fair success to predict that the release of PZA and INH from Tween 80 microemulsion is non-Fickian, whereas RIF is found to follow a Fickian mechanism.
已经研究了由油酸、磷酸盐缓冲液、乙醇和吐温(20、40、60 和 80)组成的微乳液,其中含有溶解度非常不同的抗结核药物,即异烟肼(INH)、吡嗪酰胺(PZA)和利福平(RIF)。在恒定的表面活性剂/助表面活性剂比(K(m)= 0.55)下,已经描绘了显示微乳液存在范围的相行为,在这种情况下,吐温 80 产生最大各向同性区域。在抗结核药物存在的情况下,使用电导率(sigma)和粘度(eta)行为来确定基于吐温 80 的微乳液的微结构变化。该系统的光学显微镜图像有助于理解稀释和药物存在对微乳液结构的影响。进行了分配系数、粒度分析和光谱研究(紫外-可见、傅里叶变换红外和 1H NMR),以评估药物在胶体制剂中的位置。为了比较 RIF、PZA 和 INH 从吐温 80 制剂中的释放,进行了溶解研究。结果表明,药物的释放顺序为 INH>PZA>RIF。使用 Korsmeyer 和 Peppas 方程分析了药物释放的动力学。结果成功地预测了 PZA 和 INH 从吐温 80 微乳液中的释放是非菲克型的,而 RIF 则遵循菲克型机制。