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呋塞米自微乳释液体胶囊剂的处方前研究与体外评价。

Formulation and in vitro evaluation of self-nanoemulsifying liquisolid tablets of furosemide.

机构信息

Faculty of Pharmacy, Damascus University, Damascus, Syria.

Faculty of Pharmacy, Arab International University, P.O. Box 16180, Ghabaghib, Daraa, Syria.

出版信息

Sci Rep. 2021 Jan 14;11(1):1315. doi: 10.1038/s41598-020-79940-5.

Abstract

Self-nanoemulsifying drug delivery systems (SNEDDS) were used to enhance the dissolution rate of furosemide as a model for class IV drugs and the system was solidified into liquisolid tablets. SNEDDS of furosemide contained 10% Castor oil, 60% Cremophor EL, and 30% PEG 400. The mean droplets size was 17.9 ± 4.5 nm. The theoretical model was used to calculate the amounts of the carrier (Avicel PH101) and coating materials (Aerosil 200) to prepare liquisolid powder. Carrier/coating materials ratio of 5/1 was used and Ludipress was added to the solid system, thus tablets with hardness of 45 ± 2 N were obtained. Liquisolid tablets showed 2-folds increase in drug release as compared to the generic tablets after 60 min in HCl 0.1 N using USP apparatus-II. Furosemide loaded SNEDDS tablets have great prospects for further in vivo studies, and the theoretical model is useful for calculating the adequate amounts of adsorbents required to solidify these systems.

摘要

自微乳药物传递系统 (SNEDDS) 被用于提高呋塞米的溶解速率,将其作为 IV 类药物的模型,并且该系统被固化为液固片剂。呋塞米的 SNEDDS 包含 10%的蓖麻油、60%的 Cremophor EL 和 30%的 PEG 400。平均液滴大小为 17.9±4.5nm。使用理论模型来计算载体(Avicel PH101)和包衣材料(Aerosil 200)的量,以制备液固粉末。使用 5/1 的载体/包衣材料比,并向固体系统中添加 Ludipress,从而获得硬度为 45±2N 的片剂。与普通片剂相比,在使用 USP 仪器-II 的 0.1N HCl 中 60 分钟后,液固片剂的药物释放增加了 2 倍。载有呋塞米的 SNEDDS 片剂具有进一步进行体内研究的广阔前景,并且该理论模型可用于计算固化这些系统所需的吸附剂的适当用量。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5d58/7809212/f94691ddc152/41598_2020_79940_Fig1_HTML.jpg

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