负载旋覆代赭汤的白及多糖胃漂浮剂的制备、表征及其胃肠道滞留性能评价OA
Preparation,characterization and gastrointestinal retention evaluation of a Bletilla striata polysaccharide gastric floating formulation loaded with Xuanfu Daizhe Tang
[目的]针对胃食管反流病,制备负载旋覆代赭汤提取物(XDT-P)的白及多糖胃漂浮剂(XDT@BSP-FS),并评价其漂浮与滞留性能.[方法]通过混合溶胀法制备白及多糖(BSP)-油酸甘油酯(GMO)水凝胶骨架(BSP-FS),负载XDT-P得到XDT@BSP-FS,对其漂浮性能、微观结构、理化表征、流变与力学特性、体外消化及在体滞留性能进行系统评价.[结果]XDT@BSP-FS可在0s内快速起漂,形成的浮层厚度为0.52 cm,漂浮可稳定维持>8 h.结构表征显示XDT@BSP-FS内部形成致密层状多孔网络,热分析(DSC)与红外(FT-IR)结果显示XDT-P在BSP-FS骨架中以物理结合形式存在.相同剂量XDT@BSP-FS表现出优于市售药物Gaviscon®的韧性.体内外荧光成像结果显示,XDT@BSP-FS灌胃后于活体成像中胃肠道荧光信号可持续>4 h,离体成像中至6h仍可检测到明显荧光信号,而吲哚菁绿(ICG)水溶液组荧光信号于4h时已明显减弱.[结论]XDT@BSP-FS具备快速起漂、长效漂浮与良好的体内滞留性能,可为胃食管反流相关疾病的胃滞留给药系统研究提供参考.
[Objective]To prepare a Bletilla striata polysaccharide gastric floating agent loaded with Xuanfu Daizhe Tang extract(XDT@BSP-FS)for gastroesophageal reflux induced nausea and vomiting,and to evaluate its floating and gastric retention properties.[Methods]A Bletilla striata polysaccharide(BSP)-glyceryl monooleate(GMO)hydrogel framework(BSP-FS)was prepared via a mixed swelling method,followed by loading with Xuanfu Daizhe Tang to yield XDT@BSP-FS.The floating performance,microstructure,physicochemical properties,rheological and mechanical properties,in vitro digestion behavior,and in vivo retention behavior were systematically evaluated.[Results]XDT@BSP-FS exhibited immediate floating(0 s),formed a floating layer with a thickness of 0.52 cm,and maintained stable buoyancy for over 8 h.Structural characterization revealed the formation of a dense,lamellar porous network within XDT@BSP-FS.Thermal analysis(DSC)and Fourier transform infrared spectroscopy(FT-IR)indicated that Xuanfu Daizhe Tang existed within the BSP-FS framework predominantly through physical interactions.At equivalent doses,XDT@BSP-FS demonstrated superior mechanical toughness compared with the commercially available product Gaviscon®.In vivo and ex vivo fluorescence imaging demonstrated that,following intragastric administration of XDT@BSP-FS,the gastrointestinal fluorescence signal persisted for more than 4 h in vivo,and obvious fluorescence was still detectable at 6 h ex vivo.By contrast,the fluorescence signal in the indocyanine green(ICG)aqueous solution group was already markedly attenuated at 4 h.[Conclusion]XDT@BSP-FS exhibited rapid flotation,prolonged floating duration,and favorable in vivo retention behavior,providing a reference for the development of gastroretentive drug delivery systems for gastroesophageal reflux related diseases.
李一帆;谭丽华;王萌
天津中医药大学组分中药国家重点实验室,天津 301617天津中医药大学组分中药国家重点实验室,天津 301617天津中医药大学组分中药国家重点实验室,天津 301617
医药卫生
旋覆代赭汤白及多糖胃食管反流病胃肠道滞留胃漂浮剂
Xuanfu Daizhe TangBletilla striata polysaccharidegastroesophageal reflux diseasegastrointestinal retentiongastric floating agent
《天津中医药》 2026 (8)
1000-1008,9
国家自然科学基金面上项目(82574547).
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