FORMULATION AND EVALUATION OF NASAL INSITU-GEL OF ELETRIPTAN FOR THE TREATMENT OF MIGRAINE

EPRA International Journal of Multidisciplinary Research (IJMR) Pub Date : 2024-05-17 DOI:10.36713/epra16853

Bhoomi S. Patel, Dr. Sachin.B. Narkhede, Abhay H. Rana, Mrunali S. Patel, Jinal G. Barodia, Sofiya S. Bhojani, Janhvi D. Nemade

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Abstract

Nasal in situ gel based formulations are those which upon administration get converted into gel by various mechanism like pH , Temperature & other factor. Eletriptan is BCS class 1 drug with lesser aqueous solubility which is used for Migrane. Existing market formulation include tablet for the same with less than 50 percentage bioavailability because of cytochrome induction and first pass metabolism. Mainly cause for failure of the formulation to achieve desired bioavailability and therapeutic action is because of first pass metabolism and cytochrome induction which can be avoided by nasal delivery. Polaxomer 407 and Carbopol 934 used to formulate the nasal in situ gel of Eletriptan by cold method of preparation. While polyethylene glycol400 increase the solubility of drug in polaxomer along with increasing the permeation through nasal membrane. Hence by formulating nasal in situ gel of Eletriptan we can avoid FTM and get brain targeted drug delivery for the migrane. KEYWORDS: Nasal in-situ gel, Eletriptan, Migraine, cytochrome induction, first pass metabolism, brain targeted drug delivery.

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用于治疗偏头痛的依立普坦鼻腔注射凝胶的配方和评估

鼻腔原位凝胶制剂是指用药后通过 pH 值、温度和其他因素等各种机制转化为凝胶的制剂。依立普坦是 BCS 1 类药物，水溶性较差，用于治疗偏头痛。现有的市场配方包括片剂，但由于细胞色素诱导和首过代谢，生物利用度低于 50%。制剂无法达到理想的生物利用率和治疗作用的主要原因是首过代谢和细胞色素诱导，而鼻腔给药可以避免这一点。Polaxomer 407 和 Carbopol 934 采用冷制备法配制埃利普坦鼻腔原位凝胶。聚乙二醇 400 增加了药物在 Polaxomer 中的溶解度，同时增加了通过鼻膜的渗透性。因此，通过配制埃雷普坦鼻腔原位凝胶，我们可以避免FTM，并获得针对偏头痛的脑靶向给药。

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EPRA International Journal of Multidisciplinary Research (IJMR)

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