Study on Preparation Method and Endogastric Bioadhesion Properties of Berberine-carbomer Salt

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.