Teaima Mahmoud, Abdel Hamid Magdi M, Shoman Nabil A, Jasti Bhaskara R, El-Nabarawi Mohamed A
Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo, Egypt.
Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Ahram Canadian University, Giza, Egypt.
Drug Des Devel Ther. 2020 Jul 14;14:2741-2757. doi: 10.2147/DDDT.S258571. eCollection 2020.
Bupropion is an antidepressant drug that facilitates weight loss. It is a highly water-soluble drug that needs multiple dosing, so it is considered a potential candidate for oral controlled-release dosage form. The aim of this research was to formulate and evaluate satiety-inducing swellable floating bupropion tablets by direct compression targeting depression associated with eating disorders. Various combinations of natural and semi-synthetic hydrogels were selected to achieve maximum swelling and remaining buoyant in the stomach. This synergistically enhances weight loss by increasing satiety.
An I-optimal mixture design was conducted to establish the optimal quantitative composition of tablets. Friability, floating lag time, swelling index after 4 and 8 hours, along with the percent of bupropion released at 1 and 8 hours were selected as dependent variables. The optimized formulation was characterized by physicochemical properties, thermal stability, and chemical interaction. In vivo radiographic evaluation of gastric residence besides, the oral bioavailability relative to marketed Wellbutrin sustained-release tablets were investigated using human volunteers.
The optimized formulation (73.3 mg xanthan, 120 mg glucomannan, 8.4 mg tamarind kernel powder, 78.3 mg HPMC K15M) was achieved with the overall desirability equals 0.782. In vivo radiographic study showed that formulation was retained for >8 hours in the stomach. Compared with the marketed BUP tablets, the C was almost the same with a significant increase (p =0.004) for T.
Using combinations of these hydrogels would be promising gastroretentive delivery systems in the control of bupropion rate release with enhanced floating and swelling features.
安非他酮是一种有助于减肥的抗抑郁药物。它是一种高度水溶性的药物，需要多次给药，因此被认为是口服控释剂型的潜在候选药物。本研究的目的是通过直接压片法制备并评估具有饱腹感诱导作用的可膨胀漂浮型安非他酮片，以针对与饮食失调相关的抑郁症。选择了天然和半合成水凝胶的各种组合，以实现最大程度的膨胀并在胃中保持漂浮状态。这通过增加饱腹感协同增强减肥效果。
进行I-最优混合设计以确定片剂的最佳定量组成。选择脆碎度、漂浮滞后时间、4小时和8小时后的溶胀指数以及1小时和8小时释放的安非他酮百分比作为因变量。通过物理化学性质、热稳定性和化学相互作用对优化后的制剂进行表征。此外，使用人体志愿者对胃滞留进行体内放射学评估，并研究相对于市售安非他酮缓释片的口服生物利用度。
获得了优化后的制剂（73.3毫克黄原胶、120毫克葡甘露聚糖、8.4毫克罗望子胶粉、78.3毫克羟丙基甲基纤维素K15M），总体可取性等于0.782。体内放射学研究表明，该制剂在胃中保留时间超过8小时。与市售的安非他酮片相比，曲线下面积（AUC）几乎相同，达峰时间（Tmax）显著增加（p = 0.004）。
使用这些水凝胶的组合将有望成为胃滞留给药系统，用于控制安非他酮的释放速率，具有增强的漂浮和溶胀特性。
