Trontelj Jurij, Vovk Tomaz, Bogataj Marija, Mrhar Ales
Faculty of Pharmacy, University of Ljubljana, Askerceva 7, 1000 Ljubljana SI-1000, Slovenia.
Pharmacol Res. 2005 Oct;52(4):334-9. doi: 10.1016/j.phrs.2005.05.007.
Raloxifene hydrochloride is a selective estrogen receptor modulator and is currently being used for prevention of osteoporosis in postmenopausal women. In this article, a high performance liquid chromatography (HPLC) method for detection of raloxifene hydrochloride was developed and validated using an ultraviolet (UV) and coulometric detectors. Limit of quantification (LOQ) was 0.336 and 0.610 mg L(-1) for coulometric and ultraviolet detectors, respectively. Acceptable accuracy (93.1-100.3%) as well as intra- and inter-day precision (CV<or=2.38% and CV<or=7.93%, respectively) was demonstrated in the range of 0.5-10 mg L(-1) for both detectors. The presented method was applied without any interference of excipients to the determination of raloxifene hydrochloride content in tablets and to the in vitro dissolution studies. The proposed method could be used for routine quality control. Moreover, due to its low LOQ, excellent accuracy, precision and selectivity, the coulometric detection could be applied to in vitro metabolism experiments such as microsome or hepatocyte preparations and for studies of transport of raloxifene hydrochloride across biological membranes.
盐酸雷洛昔芬是一种选择性雌激素受体调节剂，目前正用于预防绝经后妇女的骨质疏松症。在本文中，开发了一种使用紫外（UV）和库仑检测器检测盐酸雷洛昔芬的高效液相色谱（HPLC）方法并进行了验证。库仑检测器和紫外检测器的定量限（LOQ）分别为0.336和0.610 mg L⁻¹。两种检测器在0.5 - 10 mg L⁻¹范围内均显示出可接受的准确度（93.1 - 100.3%）以及日内和日间精密度（CV分别≤2.38%和CV≤7.93%）。所提出的方法在测定片剂中盐酸雷洛昔芬含量和体外溶出度研究时不受辅料的任何干扰。该方法可用于常规质量控制。此外，由于其低定量限、出色的准确度、精密度和选择性，库仑检测可应用于体外代谢实验，如微粒体或肝细胞制剂实验，以及用于研究盐酸雷洛昔芬跨生物膜的转运。
