Kaewkroek Kanidta, Petchsomrit Arpa, Wira Septama Abdi, Wiwattanapatapee Ruedeekorn
Department of Pharmaceutical Technology, Faculty of Pharmaceutical Sciences, Prince of Songkla University, Hat Yai, Songkhla 90112, Thailand.
Faculty of Integrative Medicine, Rajamangala University of Technology Thanyaburi, Thanyaburi, Pathum Thani 12130, Thailand.
Saudi Pharm J. 2022 Feb;30(2):120-131. doi: 10.1016/j.jsps.2021.12.017. Epub 2022 Jan 5.
Gastroretentive expandable films were developed to provide controlled release of ginger extract (GE) for treatment of gastric diseases. The dosage form consisted of ginger extract solid dispersion (GE-SD) loaded in a starch/chitosan composite film, which was subsequently folded and inserted into a hard gelatin capsule. GE-SD was prepared by solvent evaporation using an optimum weight ratio of 1:1 for GE and PVP K30. Expandable films containing GE-SD were prepared by solvent casting combinations of chitosan and either rice-, glutinous rice - or pregelatinized maize starch with glycerin incorporated as a plasticizer. The optimized film formulation prepared from glutinous rice starch, exhibited tensile strength of 5.4 N/cm and high expansion in simulated gastric fluid (SGF), resulting in a 2.8-fold increase in area. The films resulted in sustained release of up to 90% of the content of 6-gingerol during 8 h exposure to SGF. Furthermore, the 6-gingerol released from the film displayed dose-dependent cytotoxic activity against AGS human gastric adenocarcinoma cells and anti-inflammatory activity by inhibiting the production of nitric oxide (NO) in LPS-stimulated RAW264.7 cells.
研制了胃滞留型可膨胀薄膜，用于控制姜提取物（GE）的释放，以治疗胃部疾病。该剂型由负载于淀粉/壳聚糖复合膜中的姜提取物固体分散体（GE-SD）组成，随后将其折叠并装入硬明胶胶囊中。GE-SD采用溶剂蒸发法制备，GE与PVP K30的最佳重量比为1:1。含GE-SD的可膨胀薄膜通过壳聚糖与大米淀粉、糯米淀粉或预胶化玉米淀粉的溶剂浇铸组合制备，并加入甘油作为增塑剂。由糯米淀粉制备的优化薄膜配方，其拉伸强度为5.4 N/cm，在模拟胃液（SGF）中具有高膨胀性，面积增加了2.8倍。在暴露于SGF 8小时期间，这些薄膜导致6-姜酚含量的持续释放高达90%。此外，从薄膜中释放的6-姜酚对AGS人胃腺癌细胞显示出剂量依赖性细胞毒性活性，并通过抑制LPS刺激的RAW264.7细胞中一氧化氮（NO）的产生而具有抗炎活性。
