Department of Pharmacy, Abasyn University, Peshawar, Pakistan.
Department of Pharmacy, Kohat University of Science and Technology, Kohat, Pakistan.
Drug Des Devel Ther. 2023 Jan 26;17:261-272. doi: 10.2147/DDDT.S377686. eCollection 2023.
Self-emulsifying drug-delivery systems (SEDDSs) are designed to improve the oral bioavailability of poorly water-soluble drugs. This study aimed at formulating and characterization of SEDDS-based tablets for simvastatin using castor and olive oils as solvents and Tween 60 as surfactant.
The liquids were adsorbed on microcrystalline cellulose, and all developed formulations were compressed using 10.5 mm shallow concave round punches.
The resulting tablets were evaluated for different quality-control parameters at pre- and postcompression levels. Simvastatin showed better solubility in a mixture of oils and Tween 60 (10:1). All the developed formulations showed lower self-emulsification time (˂200 seconds) and higher cloud point (˃60°C). They were free of physical defects and had drug content within the acceptable range (98.5%-101%). The crushing strength of all formulations was in the range of 58-96 N, and the results of the friability test were within the range of USP (≤1). Disintegration time was within the official limits (NMT 15 min), and complete drug release was achieved within 30 min.
Using commonly available excipients and machinery, SEDDS-based tablets with better dissolution profile and bioavailability can be prepared by direct compression. These S-SEDDSs could be a better alternative to conventional tablets of simvastatin.
自乳化药物传递系统（SEDDS）旨在提高水溶性差的药物的口服生物利用度。本研究旨在使用蓖麻油和橄榄油作为溶剂，吐温 60 作为表面活性剂，为辛伐他汀制备基于SEDDS 的片剂并对其进行表征。
将液体吸附在微晶纤维素上，使用 10.5 毫米浅凹圆形冲头压缩所有开发的制剂。
对预压和压后不同质量控制参数的辛伐他汀进行评估。辛伐他汀在油和吐温 60（10:1）的混合物中表现出更好的溶解度。所有开发的制剂均表现出较低的自乳化时间（<200 秒）和较高的浊点（>60°C）。它们没有物理缺陷，药物含量在可接受范围内（98.5%-101%）。所有制剂的抗压强度在 58-96 N 之间，脆碎度试验结果在 USP 范围内（≤1）。崩解时间在规定范围内（NMT 15 分钟），30 分钟内即可完全释放药物。
使用常用的赋形剂和机械，可以通过直接压缩制备具有更好溶解特性和生物利用度的 SEDDS 片剂。这些 S-SEDDS 可以替代辛伐他汀的常规片剂。
