Faculty of Pharmacy, Nursing and Health Professions, Birzeit University, Al-Sahel Street 627, Ramallah, Palestine.
Samih Darwazah Institute for Pharmaceutical Industries, Faculty of Pharmacy, Nursing and Health Professions, Birzeit University, Al-Sahel Street 627, Ramallah, Palestine.
Sci Rep. 2019 Aug 12;9(1):11675. doi: 10.1038/s41598-019-48260-8.
Expandable drug delivery systems are one of many gastroretentive delivery systems which have emerged during the last few years. Expandable systems are usually folded in a capsule and expand to dimensions greater than the pyloric sphincter upon contact with gastric fluid. This prevents them from being evacuated by gastric emptying. The main objective of developing such systems is to increase the residence time of a specific drug in stomach; controlling its release, increasing its bioavailability and decreasing its side effects and dosing frequency. An expandable gastroretentive drug delivery system containing Gabapentin was developed using experimental design (D-optimal reduced quadratic design). This system was able to unfold at stomach pH in less than 15 minutes and obtain a controlled release of 78.1 ± 4.7% in 6 hours following zero-order release kinetic model. It is rigid in stomach and its rigidity decreases at intestinal pH. FTIR analysis indicated the occurrence of hydrogen bonding in Gabapentin when present in the developed system, which might be responsible for the drug's controlled release. XRD analysis indicated that Gabapentin physical properties changed from crystalline in the typical state to amorphous in the developed system.
可膨胀药物输送系统是近年来出现的众多胃滞留输送系统之一。可膨胀系统通常在胶囊中折叠，在与胃液接触时会膨胀到超过幽门括约肌的尺寸，从而防止它们被胃排空。开发此类系统的主要目的是延长特定药物在胃中的停留时间；控制其释放，增加其生物利用度，降低其副作用和用药频率。使用实验设计（D-最优减少二次设计）开发了一种含有加巴喷丁的可膨胀胃滞留药物输送系统。该系统能够在不到 15 分钟的时间内在胃 pH 值下展开，并在遵循零级释放动力学模型的情况下在 6 小时内获得 78.1±4.7%的控制释放。它在胃中是刚性的，在肠道 pH 值下其刚性会降低。傅里叶变换红外光谱（FTIR）分析表明，当加巴喷丁存在于所开发的系统中时，会发生氢键相互作用，这可能是药物控制释放的原因。X 射线衍射（XRD）分析表明，加巴喷丁的物理性质从典型状态的结晶态变为所开发系统中的无定形态。
