OBJECTIVE To investigate the attribution of berberine hydrochloride in the biological pharmaceutics classification system(BCS)and to determine its taxonomic properties.METHODS The solubility of berberine hydrochloride was investigated in pH 1.0-8.0 medium;its absorption parameters related to the rat duodenum,jejunum,ileum and colon were derived from in-situ intestinal perfusion model in vivo to determine its permeability.RESULTS The solubility in different pH dissolution media with the value of drug metering number(D0)and combined with the pharmacopoeia regulations found that berberine hydrochloride belonged to the low solubility drugs.From the results of permeability experiments,it was found that the permeability coefficient Peff(rat)of berberine hydrochloride in each intestinal segments was exceeded than 5.0 × 10-5 cm·s-1in rats,and the conversion into human absorption Fa(human)was exceeded than 85％,therefore,it was determined to be the high permeability drug.CONCLUSION The combination of solubility and permeability test results proves that berberine hydrochloride is a low solubility and high permeability drug,which belongs to BCS class Ⅱ.
关键词
盐酸小檗碱/溶解度/渗透性/生物药剂学分类系统/在体单向原位肠灌流
Key words
berberine hydrochloride/solubility/permeability/BCS classification/in-situ single pass intestinal perfusion
维普
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