交泰丸中肉桂对黄连小檗碱在大鼠体内药动学的影响

目的 考察肉桂挥发油和水提液对黄连小檗碱在大鼠体内药动学的影响.方法 将20只大鼠随机分为4组,分别灌服黄连提取物、黄连提取物加肉桂总提物、黄连提取物加肉桂挥发油、黄连提取物加肉桂水提液,采用HPLC测定大鼠血浆中小檗碱的质量浓度.结果 黄连配伍肉桂总提物后小檗碱的Cmax和AUC均明显增大,达蜂时间提前；肉桂水提液对黄连小檗碱的药动学参数影响不显著,而肉桂挥发油使小檗碱的Cmax和AUC显著增大,但增加的幅度小于肉桂总提物.结论 交泰丸中黄连、肉桂配伍,肉桂能提高黄连小檗碱的的生物利用度,其中肉桂挥发油是小檗碱药动学参数变化的影响因素之一.

Effects of Cinnamomi Cortex on pharmacokinetics of berberine in Coptidis Rhizoma based on Jiaotai Pill

AIM To investigate the effect of cinnamon oil and cinnamon aqueous extract on the pharmacokinetics of berberine after oral administration of Jiaotai Pill(Coptidis Rhizoma and Cinnamomi Cortex).METHODS Twenty rats were assigned to four groups,including Coptidis extract,Coptidis extract plus cinnamon oil plus cinnamon aqueous extract,Coptidis extract plus cinnamon oil and Coptidis extract plus cinnamon aqueous extract.All rats were administered by gavage.Berberine concentration in rats’serum was measured by HPLC.RESULTS The results showed that the Cmax and AUC of berberine in Coptidis extract plus cinnamon oil plus cinnamon aqueous extract group markedly increased and the peak time was brought forward.Cinnamon aqueous extract had no effect on pharmacokinetics parameters of berberine.Cinnamon oil exerted the important influence on it,but not as good as cinnamon oil plus cinnamon aqueous extract.CONCLUSION With combination formulation of Jiaotai Pill,Cinnamomi Cortex can improve bioavailability of berberine in Coptidis Rhizoma.Volatile oil from Cinnamomi Cortex is a key factor to the change of berberine pharmacokinetics.