艾司西酞普兰快溶片的处方、研制及体外评价。

Q3 Psychology
Vishal Bhatia, Ashwani K Dhingra, Rameshwar Dass, Bhawna Chopra, Kumar Guarve
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引用次数: 1

摘要

背景:艾司西酞普兰是一种选择性5 -羟色胺再摄取抑制剂(SSRI),通过增加大脑中的5 -羟色胺水平起作用,被广泛用于抑郁症和焦虑症的治疗。然而,由于艾司西酞普兰的水溶性较低,其溶出率较差,这是制药行业在开发口服给药系统的药物剂型时面临的一个随之而来的问题。目的:为提高艾司西酞普兰的溶出度和生物利用度,制备新的处方。方法:快速溶解片(FDT)有望使药物快速释放,这将改善药物的溶解谱,允许在急性抑郁症发作时强制初始血浆浓度增加。在片剂中使用共加工辅料已被证明可增加片剂的压缩性和崩解性,从而改善体外药物释放和生物利用度。用香蕉粉(一种具有营养价值的天然超级崩解剂)和微晶纤维素(一种具有良好吸湿和吸收能力的高度可压缩物质)的混合物作为共加工辅料。结果:采用响应面法、随机中心复合设计和直接加压法制备。发现生产的片剂在10分钟内释放95%以上的药物,并且显示出比现有上市制剂更好的药物释放谱。结论:在确认体内潜力后,快速释放制剂在体外表现出令人印象深刻的结果,可能被证明是治疗急性抑郁症发作的一个好处。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Formulation, Development, and in-vitro Evaluation of Escitalopram Fast Dissolving Tablets.

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.

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来源期刊
Central nervous system agents in medicinal chemistry
Central nervous system agents in medicinal chemistry Psychology-Neuropsychology and Physiological Psychology
CiteScore
2.10
自引率
0.00%
发文量
21
期刊介绍: Central Nervous System Agents in Medicinal Chemistry aims to cover all the latest and outstanding developments in medicinal chemistry and rational drug design for the discovery of new central nervous system agents. Containing a series of timely in-depth reviews written by leaders in the field covering a range of current topics, Central Nervous System Agents in Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments in the field.
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