School of Pharmacy, Sungkyunkwan University, Suwon, Republic of Korea.
Eur J Pharm Biopharm. 2013 Apr;83(3):460-7. doi: 10.1016/j.ejpb.2012.11.009. Epub 2012 Dec 12.
The present investigation is aimed to formulate floating gastroretentive tablets containing metformin using a sublimation material. In this study, the release of the drug from a matrix tablet was highly dependent on the polymer concentrations. In all formulations, initial rapid drug release was observed, possibly due to the properties of the drug and polymer. The effect of the amount of PEO on swelling and eroding of the tablets was determined. The water-uptake and erosion behavior of the gastroretentive (GR) tablets were highly dependent on the amount of PEO. The water-uptake increased with increasing PEO concentration in the tablet matrix. The weight loss from tablets decreased with increasing amounts of PEO. Camphor was used as the sublimation material to prepare GR tablets that are low-density and easily floatable. Camphor was changed to pores in the tablet during the sublimation process. SEM revealed that the GR tablets have a highly porous morphology. Floating properties of tablets and tablet density were affected by the sublimation of camphor. Prepared floating gastroretentive tablets floated for over 24 h and had no floating lag time. However, as the amount of camphor in the tablet matrix increased, the crushing strength of the tablet decreased after sublimation. Release profiles of the drug from the GR tablets were not affected by tablet density or porosity. In pharmacokinetic studies, the mean plasma concentration of the GR tablets after oral administration was greater than the concentration of glucophase XR. Also, the mean AUC(0-∞) values for the GR tablets were significantly greater than the plasma concentrations of glucophase XR.
本研究旨在使用升华材料制备含有二甲双胍的漂浮胃滞留片。在这项研究中，药物从基质片中的释放高度依赖于聚合物浓度。在所有配方中，观察到药物初始快速释放，这可能是由于药物和聚合物的性质。还确定了 PEO 量对片剂溶胀和侵蚀的影响。胃滞留（GR）片剂的吸水和侵蚀行为高度依赖于 PEO 的量。片剂基质中 PEO 浓度的增加会导致吸水率增加。随着 PEO 用量的增加，片剂的失重减少。樟脑用作制备低密度且易于漂浮的 GR 片剂的升华材料。樟脑在升华过程中变成片剂中的孔。SEM 显示 GR 片剂具有高度多孔的形态。片剂的漂浮性能和片剂密度受樟脑升华的影响。制备的漂浮胃滞留片可漂浮超过 24 小时，且无漂浮滞后时间。然而，随着片剂基质中樟脑的量增加，片剂在升华后抗压强度降低。药物从 GR 片剂中的释放曲线不受片剂密度或孔隙率的影响。在药代动力学研究中，口服 GR 片剂后的平均血浆浓度大于葡萄糖相 XR 的浓度。此外，GR 片剂的 AUC(0-∞) 值均显著大于葡萄糖相 XR 的血浆浓度。
