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Formulation, Development, and in-vitro Evaluation of Escitalopram Fast Dissolving Tablets

机译:艾司西酞普兰速溶片的配方、开发和体外评价

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Background: Escitalopram, a selective serotonin reuptake inhibitor (SSRI), acts by increasing the serotonin level in the brain and is used widely for the management of depression and anxiety disorders. However, the poor dissolution rate of escitalopram due to less water solubility is a consequential problem confronting the pharmaceutical industry in developing pharmaceutical dosage forms for oral delivery systems. Objective: The present work aims to deliver a novel formulation for improving the dissolution profile and, thus, the bioavailability of escitalopram. Methods: Fast Dissolving Tablets (FDT) are expected to enable quick drug release, which will improve the drug's dissolving profile, allowing for the initial increase in plasma concentration mandatory in an acute depression attack. The use of co-processed excipients in tablets has been shown to increase the compressibility and disintegration properties of the tablets, resulting in improved in-vitro drug release and bioavailability. As co-processed excipients, a mixture of banana powder (a natural super disintegrant with nutritional value) and microcrystalline cellulose (a highly compressible substance with good wicking and absorption capacity) was used. Results: The tablets were made using a response surface, randomised central composite design, and a direct compression technique. The manufactured tablets were found to be released more than 95 of the drug within 10 minutes and showed an improved drug release profile than the available marketed formulation. Conclusion: After confirming in-vivo potential, the fast release formulation exhibited impressive in-vitro findings and may prove to be a boon in treating acute depression attacks.
机译:背景:艾司西酞普兰是一种选择性血清素再摄取抑制剂 (SSRI),通过增加大脑中的血清素水平起作用,广泛用于治疗抑郁症和焦虑症。然而,由于水溶性较低,艾司西酞普兰的溶出率低是制药行业在开发用于口服给药系统的药物剂型时面临的一个重要问题。目的:本工作旨在提供一种新的配方,用于改善艾司西酞普兰的溶出度,从而改善生物利用度。方法:快速溶解片 (FDT) 有望实现药物快速释放,这将改善药物的溶解特性,允许在急性抑郁症发作时必须增加血浆浓度的初始增加。在片剂中使用共加工辅料已被证明可以增加片剂的可压缩性和崩解性能,从而改善体外药物释放和生物利用度。作为共加工辅料,使用了香蕉粉(一种具有营养价值的天然超级崩解剂)和微晶纤维素(一种具有良好芯吸和吸收能力的高可压缩物质)的混合物。结果:片剂采用响应面、随机中心复合设计和直接压缩技术制成。发现制造的片剂在 10 分钟内释放了超过 95% 的药物,并且显示出比现有上市制剂更好的药物释放曲线。结论:在确认体内潜力后,快速释放制剂显示出令人印象深刻的体外发现,可能被证明是治疗急性抑郁症发作的福音。

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