Department of Pharmaceutical Sciences and Pharmaceutics, Faculty of Pharmacy, Applied Science Private University. Amman, Jordan.
Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmaceutical Sciences, The Hashemite University, 13115 Zarqa, Jordan; Department of Pharmaceutical Sciences, Faculty of Pharmacy, Jerash University, 26150 Jerash, Jordan.
Int J Pharm. 2023 Feb 5;632:122568. doi: 10.1016/j.ijpharm.2022.122568. Epub 2022 Dec 29.
In this work, the swelling and disintegration of drug-free sodium alginate (SA) compacts and the release of metformin HCl from SA matrix tablets were investigated in acidic media of different ethanol concentrations (0, 10, 20, and 40 % v/v), pH (1.2 and 4.5) and HPMC K4M concentrations (0-1 % w/v). The investigated dissolution media represented the consumption of different alcoholic beverages, the pH of fasted and fed states, and a range of viscosity resembling diluted homogenized FDA meal. The dissolution efficiency and the time to 50 % release (t) were selected as release parameters. It was found that both ethanol concentration and medium pH affected drug release from SA matrix tablets and the swelling of SA compacts. Dose dumping occurred at high ethanol concentration (40 %) at both media pH with almost complete drug release within 15-30 min associated with rapid matrix disintegration. HPMC at 0.5-1 % concentrations increased the medium's viscosity, preventing dose dumping at high ethanol concentrations. Erosion and disintegration of SA compacts were decelerated by increasing HPMC concentration in hydroethanolic media in consonance with decreased release rate from matrix tablets. ANOVA tests showed significant effects of pH and concentrations of ethanol and HPMC in the dissolution medium on the release parameters.
在这项工作中，研究了在不同乙醇浓度（0、10、20 和 40%v/v）、pH 值（1.2 和 4.5）和 HPMC K4M 浓度（0-1%w/v）的酸性介质中，无药物的海藻酸钠（SA）片剂的溶胀和崩解以及盐酸二甲双胍从 SA 基质片剂中的释放。研究的溶解介质代表了不同酒精饮料的消耗、空腹和进食状态的 pH 值以及类似于稀释的均匀化 FDA 膳食的粘度范围。溶解效率和达到 50%释放的时间（t）被选为释放参数。结果发现，乙醇浓度和介质 pH 值都影响 SA 基质片剂中药物的释放和 SA 片剂的溶胀。在两种介质 pH 值下，高乙醇浓度（40%）都会发生药物突释，几乎在 15-30 分钟内完全释放药物，同时伴有基质快速崩解。在 0.5-1%浓度下的 HPMC 增加了介质的粘度，防止了在高乙醇浓度下的药物突释。在水醇介质中增加 HPMC 浓度会减缓 SA 片剂的侵蚀和崩解，与从基质片剂中降低的释放速率一致。方差分析测试表明，溶解介质中 pH 值和乙醇及 HPMC 浓度对释放参数有显著影响。
