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首页> 外文期刊>Journal of Young Pharmacists >Preparation and Evaluation of Mixture of Eudragit and Ethylcellulose Microparticles Loaded with Ranolazine for Controlled Release
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Preparation and Evaluation of Mixture of Eudragit and Ethylcellulose Microparticles Loaded with Ranolazine for Controlled Release

机译：负载雷诺嗪的Eudragit和乙基纤维素微粒混合物的制备及评价

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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.
机译：为了通过动力学控制药物释放来最大程度地降低抗心绞痛雷诺嗪的有害毒性作用，使用相分离法将其截留在耐胃液的，可生物降解的Eudragit（EU）和乙基纤维素（EC）二元混合物中。使用不同的聚合物共混比和溶剂制备了十种配方。通过傅立叶变换红外光谱（FT-IR）和差示扫描量热法（DSC）表征了制备的微粒的微团性质，聚合物药物相容性，以及通过扫描电子显微镜（SEM）表征了表面形态。微粒的产率高达90％，并且超过98％的分离的微粒的体积平均直径为285μm。所获得的休止角，卡尔指数百分数和堆积密度值均在指示良好流动性质的范围内。表面形态表明，颗粒为自由流动的球形，表面有细孔和倒凹。评价制备的微粒的百分产率，包封效率和体外释放研究。 FT-IR和DSC研究表明药物与使用的聚合物之间没有化学相互作用。体外药物释放研究是使用pH 1.2酸缓冲液和pH 7.4磷酸盐缓冲液进行的。 EU是一种出色的pH依赖性粘合剂，有助于在肠道内释放药物。药物释放动力学遵循不同的转运机制。增加EU的重量分数和降低EC有助于控制药物从颗粒中释放。从差异（f 1）和相似因子（f 2）来看，制剂F5是最类似于市售口服制剂作为参考标准的制剂。微粒制剂中使用的材料极大地影响了药物的释放性能，这些材料可以在肠道中吸收。

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