吖伐他汀控释片的处方及体外评价

Nirmala Dasari, Retvik Chandra Padala, Sudhakar Muvva
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引用次数: 0

摘要

吖伐他汀生物半衰期短,仅1.9小时,生物利用度较低,需要每日多次给药,因此本研究旨在开发一种吖伐他汀控释制剂,以减少剂量相关的副作用,缩短给药方案。本课题旨在研制抗癌药物吖伐他汀控释口服制剂,用于缓解季节性变应性鼻炎的症状,如打喷嚏、鼻漏、瘙痒、流泪、鼻塞等。采用HPMC K4M、Carbopol 940、HPMC K 15M等高分子聚合物控制药物释放,并按预定比例混合。共制备了9个配方,并对其进行了压缩前和压缩后的参数评价,结果均在限定范围内。从药物与辅料相容性研究(FT-IR)中证实,所使用的药物与辅料没有相互作用。体外溶出度研究表明,含150mg HPMC k15m的F9制剂可控制药物释放长达12小时。因此,认为含F9的HPMC K 15M制剂适合作为150mg吖啶伐他汀控释片的制剂,药物释放动力学表明F9制剂具有超强的病例转运机制。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Formulation and In vitro Evaluation of Acrivastine Controlled Release Tablets
Acrivastine has a short biological half-life of 1.9 hour and having less bioavailability which necessitates multiple daily dosing hence the present study was aimed to develop a controlled release formulation of Acrivastine to reduce the dose related side effects and to reduce the dosage regimen. The present research project aimed to develop a Control release oral formulation of anticancer drug Acrivastine, Acrivastine used for the symptomatic relief of seasonal allergic rhinitis such as sneezing, rhinorrhea, pruritus, lacrimation, and nasal congestion. Polymers like HPMC K4M, Carbopol 940 and HPMC K 15M were used for controlling the drug release, and the polymers are mixed in a predetermined ratio. Totally 9 formulations were prepared and evaluated for pre compression and post compression parameters, and all the results were found to be within the limits. From the drug and excipients compatability studies (FT-IR) it was confirmed that the drug and excipients used weren’t have any interactions. The in vitro dissolution studies revealed that the F9 formulation containing 150mg of HPMC K 15M controls the drug release up to 12 hours. So HPMC K 15M containing F9 formulation was considered to be suitable for the formulation of Acrivastine controlled release tablets at 150mg, and the drug release kinetics revealed that the F9 formulation shows super case transport mechanism.
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