OBJECTIVETo evaluate the effect of additives on absorption of Coptis chinensis total alkaloid and their pharmacokinetics in mice.

METHODThe mice were fed with the mixture of C. chinensis total alkaloids and additives (1:1). And then the feces and orbital blood were taken to detect the content of total alkaloids by HPLC and their pharmacokinetics.

RESULTGlutin could make the absorption of jatrorrhizine, coptisine, berberine and total alkaloids increased by 30%. Tween 80 and arabic gum did not affect the absorption of berberine, but inhibit that of other alkaloids. There had no influence of lecithin on the absorption of alkaloids. The peak time of total alkaloids in blood were 2 h (Cmax 1=5.9 mg x L(-1)) and 5.0 h (Cmax 2=3.4 mg x L(-1)), respectively, AUC was 17.6 mg x h x L(-1), the elimination of Half-life t1/2 was 5.2 h. After addition of glutin, the peak time of total alkaloids in blood were 1.5 h (Cmax 1=7.6 mg x L(-1)) and 4.8 h (Cmax 2=8.5 mg x L(-1)), AUC was up to 31.1 mg x h(-1) x L(-1), the elimination of Half-life t1/2 was 6.2 h.

CONCLUSIONGlutin could accelerate the mice on the absorption of C. chinensis total alkaloids, to extend the elimination half-life, increase the blood concentration and bioavailability.

Absorption ; drug effects ; physiology ; Alkaloids ; blood ; pharmacokinetics ; Animals ; Berberine ; analogs & derivatives ; blood ; Chromatography, High Pressure Liquid ; Coptis ; chemistry ; Diterpenes ; pharmacology ; Drug Interactions ; Female ; Food Additives ; pharmacology ; Half-Life ; Male ; Mice