Djebbar Mohamed, Chaffai Nacéra, Bouchal Fatiha
Galenic Pharmacy Laboratory, Pharmacy Department Medicine Faculty, Badji Mokhtar University, P.O. Box 204 Route Zaafrania, Annaba, Algeria.
Pharmaceutical Laboratory, Department of Engineering Process, Faculty of Technology, Abderrahmane-Mira University, Bejaia, Algeria.
Adv Pharm Bull. 2020 Jul;10(3):399-407. doi: 10.34172/apb.2020.048. Epub 2020 May 11.
The aim of this study was to evaluate the combined effect, acacia gum(AG)/ hydroxypropylmethylcellulose (HPMC), on biopharmaceutical performances of floating tablets of metformin hydrochloride (MTH) prepared by thermoplastic granulation using stearic acid. We have prepared the matrixes using AG/HPMC as a polymer combination. This combination of polymers which represents 15% of the total mass of tablet was used at various ratios 3:1, 1:1, 1:3, with two viscosity grade of HPMC (k15M and k100M). The developed matrixes have been evaluated for their pharmacotechnical and biopharmaceutical properties. In addition to the satisfactory physical characteristics of matrixes, it was revealed that the Fc3 and Fc6 formulations with AG/HPMC k15M and AG/HPMC k100M respectively, at ratio, 1:3 were considered the most performance. These formulations have shown swelling, fast flotation, 360 and 480 seconds respectively, and remained floating on the surface of the medium for more than 24 hours, with the matrix integrity, while F1, containing only AG, did not show swelling and did not float. In addition, extended release (>8 hours) with decreased dissolved MTH rates was demonstrated for Fc3 and Fc6 matrixes, 95% and 91% respectively, compared to F1 where MTH dissolution was complete after 2 hours. The drug release from the highest-performance matrixes (Fc3 and Fc6) was found to follow Korsmeyer-Peppas's model. The mechanism drug release was controlled by diffusion and erosion. The AG/HPMC combination was suitable as a polymer matrix to improve the biopharmaceutical properties of MTH compared to AG.
本研究的目的是评估刺槐豆胶（AG）/羟丙基甲基纤维素（HPMC）对采用硬脂酸通过热塑性制粒法制备的盐酸二甲双胍（MTH）漂浮片生物药剂学性能的联合作用。我们使用AG/HPMC作为聚合物组合制备了基质。这种占片剂总质量15%的聚合物组合以3:1、1:1、1:3的不同比例使用，HPMC有两种粘度等级（k15M和k100M）。对所制备的基质进行了药物工艺学和生物药剂学性质评估。除了基质具有令人满意的物理特性外，结果显示，分别含有AG/HPMC k15M和AG/HPMC k100M、比例为1:3的Fc3和Fc6制剂被认为性能最佳。这些制剂分别在360秒和480秒时表现出溶胀、快速漂浮，并在介质表面漂浮超过24小时，且基质保持完整，而仅含AG的F1制剂未表现出溶胀和漂浮。此外，与2小时内MTH溶解完全的F1相比，Fc3和Fc6基质表现出延长释放（>8小时），MTH溶解速率降低，分别为95%和91%。发现性能最佳的基质（Fc3和Fc6）的药物释放符合Korsmeyer-Peppas模型。药物释放机制受扩散和侵蚀控制。与AG相比，AG/HPMC组合作为聚合物基质适合改善MTH的生物药剂学性质。
