依托考昔与泊洛沙姆188固体分散体系统的物理化学研究

Physicochemical investigation of the solid dispersion systems of etoricoxib with poloxamer 188.

作者信息

Karekar Poonam, Vyas Vikrant, Shah Manali, Sancheti Pankajkumar, Pore Yogesh

机构信息

Department of Pharmaceutical Chemistry, Government College of Pharmacy, Karad, Maharashtra, India.

出版信息

Pharm Dev Technol. 2009;14(4):373-9. doi: 10.1080/10837450802683974.

DOI:10.1080/10837450802683974

PMID:19552551

Abstract

Solid dispersion systems of a poorly water-soluble drug, etoricoxib were prepared with poloxamer 188 in 1:0.5, 1:1.5 and 1:2.5 ratios and evaluated by FTIR, powder XRD and dissolution studies. Physical studies demonstrated a strong hydrogen bonding with significant decrease in the crystallinity and formation of amorphous etoricoxib in its binary systems. All binary systems of etoricoxib showed faster dissolution than pure drug alone (P < 0.001). However, 1:2.5 proportion of etoricoxib: poloxamer 188 showed superior performance (DE45: 71.27% +/- 3.85) in enhancing solubility and dissolution rate of etoricoxib suggesting optimum ratio of the carrier.

摘要

采用泊洛沙姆188，以1:0.5、1:1.5和1:2.5的比例制备了难溶性药物依托考昔的固体分散体系统，并通过傅里叶变换红外光谱（FTIR）、粉末X射线衍射（XRD）和溶出度研究进行了评估。物理研究表明，在其二元体系中存在强烈的氢键作用，结晶度显著降低，且形成了无定形依托考昔。依托考昔的所有二元体系均表现出比单独的纯药物更快的溶出度（P<0.001）。然而，依托考昔与泊洛沙姆188比例为1:2.5时，在提高依托考昔的溶解度和溶出速率方面表现出优异的性能（45分钟溶出度：71.27%±3.85），表明该载体比例最佳。