Institute of Pharmacy, University of Greifswald, Felix-Hausdorff-Strasse 3, 17487, Greifswald, Germany,
AAPS PharmSciTech. 2014 Feb;15(1):230-6. doi: 10.1208/s12249-013-0050-2. Epub 2013 Dec 3.
The aim of the present work was the investigation of robustness and reliability of drug release from 50 to 400 mg quetiapine extended release HPMC matrix tablets towards mechanical stresses of biorelevant intensity. The tests were performed under standard conditions (USP apparatus II) as well as under simulated gastrointestinal stress conditions. Mechanical stresses including pressure and agitation were applied by using the biorelevant dissolution stress test apparatus as it has been introduced recently. Test algorithms already established in previous studies were applied to simulate fasting gastrointestinal conditions. The dissolution experiments demonstrated striking differences in the product performance among standard and stress test conditions as well as dose strengths. In USP apparatus II, dissolution profiles were affected mainly by media pH. The dissolution experiments performed in biorelevant dissolution stress test device demonstrated that stress events of biorelevant intensity provoked accelerated drug release from the tablets.
本工作旨在研究 50 至 400 毫克喹硫平 HPMC 延释基质片在模拟胃肠道相关强度的机械应力下释放药物的稳健性和可靠性。测试在标准条件（USP 仪器 II）和模拟胃肠道应激条件下进行。使用最近引入的生物相关溶解应激测试仪器施加机械应力，包括压力和搅拌。测试算法已在前研究中应用于模拟空腹胃肠道条件。溶解实验表明，在标准和应激测试条件以及剂量强度之间，产品性能存在显著差异。在 USP 仪器 II 中，溶解曲线主要受介质 pH 值的影响。在生物相关溶解应激测试设备中进行的溶解实验表明，生物相关强度的应激事件会加速片剂中药物的释放。
