Department of Pharmaceutics, I.T.S. Paramedical (Pharmacy) College , Muradnagar, Ghaziabad, U.P. , India.
Artif Cells Nanomed Biotechnol. 2014 Jun;42(3):167-77. doi: 10.3109/21691401.2013.800081. Epub 2013 Jun 13.
Gabapentin follows saturation kinetics for absorption because of carrier-mediated transport and narrow absorption window in stomach. There is need to develop a gastroretentive formulation to maximize the absorption without crossing the saturation threshold for absorption.
The aim was to develop a gastroretentive formulation of gabapentin to increase the fraction of drug absorbed in stomach.
Sodium alginate and sodium carboxymethylcellulose were used to formulate the microsphere by ionotropic gelation with calcium chloride. The formulation was optimized using a three-factor, three-level Box-Behnken design.
The particle size varied from 559.50 to 801.10 μm, entrapment efficiency from 61.29 to 81.00% and in vitro release from 69.40 to 83.70%. The optimized formulation was found using point-prediction, and formulation OF-3 showed optimum results at 608.21 μm size, 79.65% entrapment efficiency and 82.72% drug release and 81% mucoadhesion up to 10 h. The drug release was controlled for more than 12 h.
The particle size was most influenced by sodium alginate while entrapment efficiency and drug release depended upon both polymers. The release followed Higuchi model.
Gastroretentive formulation was successfully optimized by a three-factor, three-level Box-Behnken design and found to be useful.
由于载体介导的转运和胃内狭窄的吸收窗口，加巴喷丁的吸收遵循饱和动力学。因此需要开发一种胃滞留制剂，以最大限度地提高吸收，而不超过吸收的饱和阈值。
旨在开发一种胃滞留型加巴喷丁制剂，以增加胃内吸收的药物分数。
采用离子凝胶法，用氯化钙将海藻酸钠和羧甲基纤维素钠制成微球。采用三因素三水平 Box-Behnken 设计优化配方。
粒径为 559.50-801.10 μm，包封率为 61.29%-81.00%，体外释放为 69.40%-83.70%。通过点预测发现最佳配方为 OF-3，其粒径为 608.21 μm，包封率为 79.65%，药物释放 82.72%，10 h 时粘膜黏附率为 81%。药物释放可控制超过 12 h。
粒径受海藻酸钠影响最大，而包封率和药物释放则取决于两种聚合物。释放遵循 Higuchi 模型。
采用三因素三水平 Box-Behnken 设计成功优化了胃滞留制剂，具有一定的应用价值。
