Gowda Dv, Gowrav Mp, Gangadharappa Hv, Khan Ms
Department of Pharmaceutics, JSS College of Pharmacy, JSS University, Mysore, Karnataka, India.
J Young Pharm. 2011 Jul;3(3):189-96. doi: 10.4103/0975-1483.83757.
To minimize the unwanted toxic effects of anti-anginal ranolazine by kinetic control of drug release, it was entrapped into gastro-resistant, biodegradable eudragit (EU) and ethyl cellulose (EC) binary blend using phase separation method. Ten formulations were prepared using different polymer blend ratios and solvent. The prepared microparticles were characterized for micromeritic properties, polymer drug compatibility by Fourier Transform Infrared Spectroscopy (FT-IR) and Differential Scannibg Calorimetry (DSC), and surface morphology by Scanning Electron Micrography (SEM). The yield of microparticles was up to 90% and more than 98% of the isolated microparticles are having volume mean diameter of 285 μm. The obtained angle of repose, percentage Carr's index and tapped density values were within the limits indicating good flow properties. The surface morphology revealed that particles were free-flowing, spherical, with minute pores and invert dents on the surface. The prepared microparticles were evaluated for percentage yield, encapsulation efficiency and in vitro release studies. FT-IR and DSC studies showed no chemical interaction between the drug and used polymers The in vitro drug release studies were carried out using pH 1.2 acid buffer and pH 7.4 phosphate buffer. EU acts as an excellent pH-dependent binder and helps to release the drug in the intestine. The drug release kinetics followed different transport mechanisms. Increasing the weight fractions of EU and decreased EC helps to control the drug release from the particles. From the differential (f(1)) and similarity factor (f(2)), Formulation F5 was the formulation most similar to the commercially available oral formulation as reference standard. The drug release performance was greatly affected by the materials used in microparticle preparations, which allow absorption in the intestinal tract.
为了通过药物释放的动力学控制来最小化抗心绞痛药物雷诺嗪的不良毒性作用，采用相分离法将其包封于胃滞留型、可生物降解的丙烯酸树脂（EU）和乙基纤维素（EC）二元共混物中。使用不同的聚合物共混比例和溶剂制备了十种制剂。对制备的微粒进行了微观性质、通过傅里叶变换红外光谱（FT-IR）和差示扫描量热法（DSC）表征聚合物与药物的相容性，以及通过扫描电子显微镜（SEM）表征表面形态。微粒的产率高达90%，分离出的微粒中超过98%的体积平均直径为285μm。所获得的休止角、卡尔指数百分比和振实密度值均在表明良好流动性的范围内。表面形态显示颗粒自由流动、呈球形，表面有微小孔隙和倒凹。对制备的微粒进行了产率百分比、包封效率和体外释放研究。FT-IR和DSC研究表明药物与所用聚合物之间没有化学相互作用。体外药物释放研究使用pH 1.2酸性缓冲液和pH 7.4磷酸盐缓冲液进行。EU作为一种优异的pH依赖性粘合剂，有助于在肠道中释放药物。药物释放动力学遵循不同的转运机制。增加EU的重量分数并降低EC有助于控制药物从颗粒中的释放。根据差异因子（f(1)）和相似因子（f(2)），制剂F5是与市售口服制剂作为参比标准最相似的制剂。微粒制剂中使用的材料极大地影响了药物释放性能，这些材料允许药物在肠道中吸收。
