ABSTRACT
Objective To examine the effect of berberine hydrochloride ( BER ) on the pharmacokinetic profiles of midazolam,a substrate of CYP3A,in rats. Methods The rats were intragastrically given different doses of BER (50,100, 200 mg?kg-1) or ketoconazole (75 mg?kg-1) for 10 days.Single-pass duodenum perfusion of 20 mg?kg-1 MDZ was performed and the inguinal artery was cannulated for blood sampling.Plasma concentrations of MDZ and 1'-OH-MDZ were analyzed by high performance liquid chromatography ( HPLC) with the CYP3A inhibitor ketoconazole serving as positive control. Results BER (50,100,200 mg?kg-1) and ketoconazole (75 mg?kg-1) could significantly increase the AUC(0-t),AUMC(0-t)and Cmax of MDZ in a dose-dependent manner ( P<0.05) ,and reduce the clearance rate ( CLz ) of MDA and its apparent volume of distribution in the body ( Vz ) ( P<0. 05). But they failed to dramatically affect the half-life ( t1/2z ) and the peak time ( tmax ) of MDZ. Additionally,BER ( 100,200 mg?kg-1 ) and ketoconazole ( 75 mg?kg-1 ) could significantly dose-dependently decrease the AUC(0-t),AUMC(0-t)and Cmaxof 1'-OH-MDZ,and profoundly increase the CLz,tmax and Vz of 1'-OH-MDZ (P<0.05),but they had no remarkable influences on the t1/2z.The ratio of AUC(1'-OH-MDZ)/AUC(MDZ) was decreased with the increase of BER concentration. Conclusion BER can inhibit the in vivo metabolism of MDZ in a dose-dependant manner, which is associated with the suppression of the activity of CYP3A.
ABSTRACT
Objective:To establish an HPLC method for the determination of gallic acid and berberine hydrochloride in Dihuang sprays. Methods:A ZORBAX SB-C18 column (250 mm × 4. 6 mm,5 μm) was used, the mobile phase was acetonitrile-0. 1% phos-phoric acid with gradient elution. The flow rate was 1. 0 ml·min-1 , the column temperature was 30℃, and the detection wavelength wassetat270nm.Results:Thelinearrangeofgallicacidandberberinehydrochloridewas20.36-305.40 μg·ml-1(r=0.9996) and 20.08-301.20 μg·ml-1(r=0.999 8), respectively. The average recovery was 98.9%(RSD =1.3%) and 98.5%(RSD =1. 5%) , respectively. Conclusion:The method is simple, reliable and accurate, which can be used in the determination of gallic acid and berberine hydrochloride of Dihuang sprays.
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Objective To establish a HPLC method for the determination of baicalin and berberine hydrochloride in Com-pound Qinbo Granules. Methods The gradient elution was performed on a Diamonsil C18 column using method-water (0. 05 % phosphate acid and 0. 1% trithylamine) as mobile phase, and the detection wavelength was 276 nm. Results The linear calibration curve of baicalin was obtained in the range of 10. 08～201.6 mg·L-1 with an average recovery of 98. 1% (RSD=1.11%). The linear calibration curve of berberine hydrochloride was in the range of 4. 08～81.6 mg·L-1 with an average re-covery of 97.9 % (RSD=1.24 %). Conclusion The method is simple and reproducible. It can be used for the quality con-trol of Compound Qinbo Granules.