Department of Pharmaceutics, SRM College of Pharmacy, SRMIST, Kattankulathur, India.
Int J Immunopathol Pharmacol. 2024 Jan-Dec;38:3946320241249429. doi: 10.1177/03946320241249429.
This study investigated the raft-forming suspension of famotidine as an anti-reflux formulation to improve the oral bioavailability of narrow absorption window drugs by enhancing gastric residence time (GRT) and preventing gastro-esophageal reflux disease (GERD).
Various combinations of raft-forming agents, such as Tragacanth gum (TG), guar gum (GG), and xanthan gum (XG), were evaluated alongside sodium alginate (SA) to develop an effective raft. Preformulation studies and preliminary screening were conducted to identify the most suitable raft-forming agent, and GG was chosen due to its mucilaginous properties. The formulation was optimized using a 32 full factorial design, with the quantities of GG and SA as independent factors and apparent viscosity and in-vitro drug release (%) as dependent factors. The in vivo floating behavior study was performed for optimized and stabilized formulation.
Among the tested batches, F6 was selected as the optimized formulation. It exhibited desirable characteristics such as adequate raft weight for extended floating in gastric fluid, improved apparent viscosity, and a significant percentage of drug release at 12 h. A mathematical model was applied to the in-vitro data to gain insights into the drug release mechanism of the formulation. The stability of the suspension was assessed under accelerated conditions, and it demonstrated satisfactory stability. The formulation remains floating in the Rabbit stomach for more than 12 h.
It concludes that the developed formulation has enhanced bioavailability in the combination of GG and SA. The floating layer of the raft prevents acid reflux, and the famotidine is retained for an extended period of time in the gastric region, preventing excess acid secretion. The developed formulations are effective for stomach ulcers and GERD, with the effect of reducing acid secretion by H2 receptor antagonists.
本研究通过延长胃滞留时间（GRT）和预防胃食管反流病（GERD）来提高窄吸收窗药物的口服生物利用度，考察了法莫替丁形成筏的混悬液作为一种抗反流制剂。
评估了诸如黄蓍胶（TG）、瓜尔胶（GG）和黄原胶（XG）等形成筏的各种组合与海藻酸钠（SA）一起形成有效的筏。进行了预配方研究和初步筛选，以确定最合适的形成筏的试剂，由于其胶粘性，选择 GG。使用 32 完全析因设计优化配方，以 GG 和 SA 的量作为独立因素，以表观粘度和体外药物释放（%）作为依赖因素。对优化和稳定的配方进行体内漂浮行为研究。
在所测试的批次中，选择 F6 作为优化配方。它表现出了令人满意的特性，例如在胃液中延长漂浮所需的足够筏重量、改进的表观粘度以及在 12 小时时显著的药物释放百分比。应用数学模型对制剂的体外数据进行分析，以深入了解制剂的药物释放机制。在加速条件下评估了悬浮液的稳定性，结果表明稳定性良好。该配方在兔胃中能保持漂浮 12 小时以上。
开发的配方与 GG 和 SA 结合使用可提高生物利用度。筏的漂浮层可防止酸反流，法莫替丁在胃区保留的时间延长，可防止胃酸过度分泌。开发的配方对胃溃疡和 GERD 有效，其通过 H2 受体拮抗剂减少胃酸分泌的效果。
