Abdallah Marwa H, Abdelnabi Dina M, Elghamry Hanaa A
Department of Pharmaceutics, College of Pharmacy, University of Ha'il, Hail 81442, Saudi Arabia.
Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Zagazig University, Zagazig 44519, Egypt.
Gels. 2022 Jun 22;8(7):395. doi: 10.3390/gels8070395.
The purpose of the current investigation was to formulate, assess, and optimize oral in situ gels of buspirone hydrochloride (BH) with the specific end goal of expanding the time the medication spends in the stomach, thereby ensuring an extended medication discharge. This would allow the use of a once-a-day dose of liquid BH formulations, which is ideal for the treatment of pediatric anxiety. In situ gels loaded with BH were prepared using various concentrations of sodium alginate (Na alg.), calcium chloride (CaCl), and hydroxypropyl methylcellulose (HPMC K15M). The in situ gels exhibited the desired consistency, drug distribution, pH, ability to form gel, and prolonged drug release in vitro. The (3) full factorial design was utilized for the revealing of the ideal figures for the selected independent variables, Na alg. (X), HPMC (X), and CaCl (X) based on measurements of the viscosity (Y) and percentage drug release after 6 h (Y). A pharmacokinetic study of the optimum formulation on rabbits was also performed. The formulation containing 2% of Na alg., 0.9% of HPMC-K15M, and 0.1125% of CaCl was selected as the ideal formulation, which gave the theoretical values of 269.2 cP and 44.9% for viscosity and percentage of drug released after 6 h, respectively. The pharmacokinetic study showed that the selected oral Na alg. in situ gel formulation displayed a prolonged release effect compared to BH solution and the marketed tablet (Buspar), which was confirmed by the low C and high T values. The optimum oral Na alg. in situ gel showed a 1.5-fold increment in bioavailability compared with the drug solution.
当前研究的目的是制备、评估并优化盐酸丁螺环酮（BH）口服原位凝胶，其特定最终目标是延长药物在胃中的停留时间，从而确保药物的持续释放。这将使得每日一次剂量的液体BH制剂成为可能，这对于治疗儿童焦虑症而言是理想的。使用不同浓度的海藻酸钠（Na alg.）、氯化钙（CaCl）和羟丙基甲基纤维素（HPMC K15M）制备了载有BH的原位凝胶。原位凝胶在体外表现出所需的稠度、药物分布、pH值、形成凝胶的能力以及延长的药物释放。基于粘度（Y）和6小时后药物释放百分比（Y）的测量，采用（3）全因子设计来揭示所选自变量Na alg.（X1）、HPMC（X2）和CaCl（X3）的理想数值。还对家兔进行了最佳制剂的药代动力学研究。含有2% Na alg.、0.9% HPMC-K15M和0.1125% CaCl的制剂被选为理想制剂，其粘度和6小时后药物释放百分比的理论值分别为269.2 cP和44.9%。药代动力学研究表明，与BH溶液和市售片剂（Buspar）相比，所选的口服Na alg.原位凝胶制剂显示出缓释效果，这通过低Cmax和高Tmax值得到证实。最佳口服Na alg.原位凝胶与药物溶液相比，生物利用度提高了1.5倍。
