小檗碱-卡波姆盐类复合物的制备及其胃生物粘附性与抗Hp活性评价
Study on Preparation Method and Endogastric Bioadhesion Properties of Berberine-carbomer Salt
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摘要: 目的 研究小檗碱-卡波姆盐类复合物的制备方法、体外释药特性、胃生物粘附性能和抗Hp活性。方法 以小檗碱-卡波姆盐收率和载药量为指标，采用单因素法优选卡波姆品种、卡波姆浓度、小檗碱浓度、用量比和反应体系pH值。采用体外释放度测定法研究小檗碱-卡波姆盐的缓释性能。采用体外大鼠胃黏膜组织粘附留存量测定法、体外大鼠胃黏膜粘附分离力测定法以及大鼠胃内留存量测定法评价小檗碱-卡波姆盐的胃生物粘附性能。采用打孔琼脂扩散法初步评价小檗碱-卡波姆盐的体外抗幽门螺杆菌活性。结果 优选卡波姆品种为974P，卡波姆浓度为0.25%，小檗碱浓度为0.3%，卡波姆溶液与小檗碱溶液用量比为2∶1。小檗碱-卡波姆盐对体外大鼠胃黏膜组织的粘附留存量和体外大鼠胃黏膜粘附分离力小于卡波姆，但显著大于游离小檗碱；小檗碱-卡波姆盐在大鼠胃内的留存量显著高于小檗碱。小檗碱-卡波姆盐在人工胃液中分解释放出小檗碱并显示出缓释特性，在体外对Hp具有显著抑制活性。结论 小檗碱-卡波姆盐既具有良好的胃生物粘附性能又具有缓释特性，可提高小檗碱在胃内的滞留时间，进而提高小檗碱杀灭Hp的疗效。Abstract: OBJECTIVE To study preparation method and drug releasing in vitro and endogastric bioadhesion properties and killing Hp activity in vitro of berberine-carbomer salt. METHODS Influencing factor such as variety of carbomer， the concentration of carbomer and berberine are studied by single factor experiment using the yield and the drug loading as evaluating indicator. The release rate of berberine from berberine-carbomer salt in vitro are measured by using Chinese Pharmacopeia (CP) 2010 oar method. The endogastric bioadhesion of berberine-carbomer salt are evaluated by determining the adhesive force of berberine-carbomer salt with the rat gastric mucosa in vitro， and the remaining percentage on the rat’s gastric mucosa in vitro or in rat’s stomach in vivo. The killing Hp activity in vitro of berberine-carbomer salt are evaluated by cylinder plate method. RESULTS The optimizing variety is carbomer 974P， and the concentration of carbomer 974P is 0.25%， berberine is 0.3%， with the ratio between carbomer solution and berberine solution being 2∶1. The releasing of berberine-carbomer salt indicates the delayed releasing properties in the dissolution mediator with pH 1.2. The adhesive force of berberine-carbomer salt with the rat gastric mucosa and the remaining percentage on the rat’s gastric mucosa in vitro are larger than berberine. The endogastric stagnation time in rat of berberine-carbomer salt is longer than berberine. CONCLUSION Berberine-carbomer salt possess superordinary properties of delayed releasing and endogastric bioadhesion.
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Key words:
- Carbomer /
- Berberine /
- bioadhesion /
- Helicobacter pylori
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