Daar Junaid, Khan Ahmad, Khan Jallat, Khan Amjad, Khan Gul Majid
Department of Pharmacy, Quid I Azam University, Islamabad, Pakistan.
Basic Science Department, Khuwaja Fareed University of Engineering and Information Technology, Rahim Yar Khan, Pakistan.
Pak J Pharm Sci. 2017 Mar;30(2(Suppl.)):601-606.
The aim of the study was to successfully design, formulate and evaluate self-nanoemulsifying drug delivery system (SNEDDS) of poorly aqueous soluble drug viz. flurbiprofen using long (LCT), medium (MCT) and short chain triglycerides (SCT). The SNEDDS are thermodynamically stable lipid based drug delivery systems which consist of mixture of oil, surfactant and co-surfactant. Upon aqueous dilution, this mixture produces nano-emulsion spontaneously on slight agitation. The excipients intended to be used were screened for their potential to dissolve the drug and to form clear dispersion upon aqueous dilution. Labrafil M 1944 CS, capryol-90 and triacetin were selected as long, medium and short chain triglycerides, respectively, as lipids while tween-80 and polyethylene glycol-400 (PEG-400)/ethanol (3:1 ratio) were selected as surfactant and co-surfactant, respectively. The excipients were studied at every possible combination ratios using pseudo-ternary diagram. The LCT, MCT and SCT-SNEDDS were optimized using thermodynamic studies, percentage transmittance value, viscosity, refractive index (RI), electrical conductivity, globule size analysis and in-vitro drug release studies. The drug release profiles of optimized SNEDDS were then compared with market product at different pH mediums. The LCT-SNEDDS was considered to be superior for enhancement of the drug bioavailability when compared with other SNEDDS formulations and market product.
本研究的目的是成功设计、制备并评价难溶性药物氟比洛芬的自纳米乳化药物递送系统(SNEDDS),使用长链甘油三酯(LCT)、中链甘油三酯(MCT)和短链甘油三酯(SCT)。SNEDDS是基于脂质的热力学稳定的药物递送系统,由油、表面活性剂和助表面活性剂的混合物组成。在用水稀释时,该混合物在轻微搅拌下会自发形成纳米乳剂。对拟使用的辅料进行筛选,考察其溶解药物的能力以及在用水稀释后形成澄清分散体的能力。分别选用Labrafil M 1944 CS、辛酸癸酸甘油三酯和三醋精作为长链、中链和短链甘油三酯作为脂质,同时分别选用吐温80和聚乙二醇-400(PEG-400)/乙醇(3:1比例)作为表面活性剂和助表面活性剂。使用伪三元相图研究了辅料在各种可能的组合比例下的情况。通过热力学研究、百分透光率值、粘度、折射率(RI)、电导率、球粒大小分析和体外药物释放研究对LCT、MCT和SCT-SNEDDS进行优化。然后将优化后的SNEDDS的药物释放曲线与市售产品在不同pH介质中的情况进行比较。与其他SNEDDS制剂和市售产品相比,LCT-SNEDDS被认为在提高药物生物利用度方面更具优势。