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Development and Evaluation of Taste Masked Granular Formulation of Satranidazole by Melt Granulation Technique

机译:熔融制粒技术制备苦味胺掩味颗粒制剂的开发与评价

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摘要

Drugs from nitroimidazole category are generally bitter in taste. Oral formulation with bitter taste is not palatable. Geriatrics and pediatrics patients usually suffer from swallowing difficulties. Many other patients in some disease conditions avoid swallowing tablets. Satranidazole is a new nitro-imidazole derivative with bitter taste and is available in market as film coated tablet. The purpose of this research was to mask the bitter taste of Satranidazole by coating complexation with low melting point wax and Eudragit EPO. Different types of wax (glyceryl monostearate, stearic acid and cetyl alcohol) were tried for taste masking. The drug to stearic acid ratio 1 : 2 was found to be optimum on the basis of taste evaluation and in vitro release. The formulated granules were found to possess good flow property. FTIR studies confirmed that there was no interaction between drug and excipients. Scanning Electron Microscopy of drug and the optimized batch of granules was performed. The in vitro release of drug from granules was compared with marketed tablet formulation. The taste masked granules of optimized batch showed 87.65% release of drug in 1 hr which is comparable to that of marketed tablet formulation.
机译:硝基咪唑类药物通常味苦。具有苦味的口服制剂是不可口的。老人和儿科患者通常会遭受吞咽困难。在某些疾病条件下的许多其他患者避免吞咽片剂。 Satranidazole是一种新的硝基咪唑衍生物,具有苦味,可作为薄膜包衣片剂在市场上购买。这项研究的目的是通过与低熔点蜡和Eudragit EPO形成​​复合物来掩盖Satranidazole的苦味。尝试使用不同类型的蜡(单硬脂酸甘油酯,硬脂酸和鲸蜡醇)掩盖味道。根据味道评估和体外释放,发现药物与硬脂酸的比率为1∶∶ 2是最佳的。发现配制的颗粒具有良好的流动性。 FTIR研究证实药物与赋形剂之间没有相互作用。进行药物的扫描电子显微镜检查和优化的颗粒批次。将药物从颗粒中的体外释放与市售片剂进行比较。优化批次的掩味颗粒在1?hr内显示出87.65%的药物释放,与市售片剂相当。

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