Kumar Krishan, Dhawan Neha, Sharma Harshita, Patwal Pramod S, Vaidya Shubha, Vaidya Bhuvaneshwar
a Department of Pharmaceutics , ISF college of Pharmacy , Moga, Punjab , India.
Artif Cells Nanomed Biotechnol. 2015;43(5):328-33. doi: 10.3109/21691401.2014.887017. Epub 2014 Mar 3.
Metoprolol succinate is a very potent drug for the treatment of hypertension but suffers from poor bioavailability due to its erratic absorption in lower GI tract. Therefore, in the present study, it was hypothesized that by formulating mucoadhesive particles, the residence time in the GIT and release of drug may be prolonged that will enhance the bioavailability of metoprolol succinate. Metoprolol succinate loaded chitosan microparticles were prepared by ionic gelation method. The optimized microparticles were coated with sodium alginate to form a layer over chitosan microparticles to increase the mucoadhesive strength and to release the drug in controlled manner. Coated and uncoated microparticles were evaluated for particle size, zeta potential, morphology, entrapment efficiency, drug loading and in vitro drug release. The coated microparticles showed comparatively less drug release in the 0.1 N HCl while sustained release in PBS (pH 6.8) as compared to uncoated microparticles. The in vivo study on albino rats demonstrated an increase in bioavailability of the coated microparticles as compared to marketed formulation. From the study it can be concluded that alginate coated chitosan microparticles could be a useful carrier for the oral delivery of metoprolol succinate.
琥珀酸美托洛尔是一种治疗高血压的强效药物，但由于其在胃肠道下部吸收不稳定，生物利用度较差。因此，在本研究中，我们假设通过制备粘膜粘附颗粒，可以延长药物在胃肠道的停留时间和释放时间，从而提高琥珀酸美托洛尔的生物利用度。采用离子凝胶法制备了负载琥珀酸美托洛尔的壳聚糖微粒。对优化后的微粒用海藻酸钠进行包衣，在壳聚糖微粒表面形成一层涂层，以提高粘膜粘附强度并实现药物的控释。对包衣和未包衣的微粒进行了粒径、zeta电位、形态、包封率、载药量和体外药物释放等方面的评价。与未包衣微粒相比，包衣微粒在0.1 N盐酸中药物释放相对较少，而在pH 6.8的磷酸盐缓冲液中呈现缓释。对白化大鼠的体内研究表明，与市售制剂相比，包衣微粒的生物利用度有所提高。从该研究可以得出结论，海藻酸钠包衣的壳聚糖微粒可能是口服递送琥珀酸美托洛尔的一种有用载体。
