Attari Zenab, Bhandari Amita, Jagadish P C, Lewis Shaila
Department of Pharmaceutics, Manipal College of Pharmaceutical Sciences, Manipal University, Manipal, India.
Department of Quality Assurance, Manipal College of Pharmaceutical Sciences, Manipal University, Manipal, India.
Saudi Pharm J. 2016 Jan;24(1):57-63. doi: 10.1016/j.jsps.2015.03.008. Epub 2015 Mar 20.
The purpose of this study was to develop nanosuspension based on combinative technology to enhance the intestinal absorption of Olmesartan medoxomil (OLM), a potent antihypertensive agent with limited oral bioavailability. Two combinative approaches were employed and then characterized. In vitro intestinal absorption of OLM nanosuspension and plain OLM was studied using non-everted rat intestinal sac model. Optimal OLM nanosuspension was prepared by a combination of ball milling and probe sonication using stabilizer, Poloxamer 407. The formula exhibited particle size of 469.9 nm and zeta potential of -19.1 mV, which was subjected to ex vivo studies. The flux and apparent permeability coefficient in intestine from OLM nanosuspension was higher than the plain drug, thereby suggesting better drug delivery.
本研究的目的是基于组合技术开发纳米混悬液,以提高奥美沙坦酯(OLM)的肠道吸收,奥美沙坦酯是一种口服生物利用度有限的强效抗高血压药物。采用了两种组合方法并对其进行了表征。使用非外翻大鼠肠囊模型研究了OLM纳米混悬液和普通OLM的体外肠道吸收。使用稳定剂泊洛沙姆407,通过球磨和探头超声处理相结合的方法制备了最佳的OLM纳米混悬液。该配方的粒径为469.9 nm,ζ电位为-19.1 mV,并进行了体外研究。OLM纳米混悬液在肠道中的通量和表观渗透系数高于普通药物,从而表明其具有更好的药物递送效果。