Distribution in vivo of colon-oriented berberine hydrochloride-carboxymethyl konjac glucomannan pellets in rats

AIM: To evaluate colon-oriented delivery characteristics of berberine hydrochloricde(BH) containing carboxymethyl konjac glucomannan(CMKGM) pellets. METHODS: BH-containing CMKGM pellets(pellets group) and BH-containing carboxymethyl cellulose suspension(control group) were intragastric administrated to rats at the dose of 50 mg/kg,respectively.Blood samples were obtained from the rat femoral artery,the gastric、entric、cecal、colonic tissues and their contents sampled at a given interval to measure the concentration of BH by HPLC.The bar charts of relative content of BH in different parts of the gastrointestinal tract and theirs contents were drawn.Drug delivery index(DDI) was calculated. RESULTS: Compared with the control group,the concentration and distribution of BH in gastric、enteric tissue and their contents decreased significantly,but in cecal、colonic tissue and their contents less at first,and more than the control group after 2～6 h.The DDI values of the pellets to gastric,enteric,cecal,colonic tissue and their contents were 0.392 4,0.478 6,3.916,4.193,(0.162 8,)0.619 4,3.843,4.087 against the control group,respectively. CONCLUSION: CMKGM pellets may be a useful colon-specific drug delivery system for BH.