ABSTRACT
Objective To compare the effect of Compound Wurenchun Capsule (CWC) and Wuzhi Capsule (WZC), CWC single and long-term administration on the pharmacokinetics of tacrolimus (FK506). Methods Twenty-four rats were randomly divided into FK506, CWC + FK506, WZC + FK506 and CWC7d + FK506 groups, with six rats in each group. Rats in FK506, CWC + FK506, and WZC + FK506 groups were given a single gavage with FK506, CWC + FK506, and WZC + FK506 respectively. Rats in CWC7d + FK506 group was given a multiple gavage regimen of daily CWC gavage for 6 d, CWC and FK506 on day 7. Blood sample from orbit before and after gavage at different time points (CWC7d + FK506 group before and after the last administration) were tested for FK506 blood concentration and the pharmacokinetic parameters were calculated. Results Compared with FK506 group, peak blood concentration (Cmax) and area under the curve (AUC0-t) of FK506 increased significantly (P < 0.05, 0.01), body retention time (MRT0-t) of FK506 prolonged significantly (P < 0.05, 0.01), the apparent volume of distribution (V/F) and the drug elimination rate (CL/F) of FK506 decreased significantly (P < 0.01) in WZC + FK506 and CWC + FK506 groups. Compared with WZC + FK506 group, AUC0-t of FK506 increased significantly (P < 0.01), CL/F of FK506 decreased significantly (P < 0.01) in CWC + FK506 group. Compared with CWC + FK506 group, Cmax of FK506 increased significantly (P < 0.01), time to peak blood concentration (tmax) of FK506 shortened significantly (P < 0.05), AUC0-t of FK506 increased significantly (P < 0.05), CL/F of FK506 decreased significantly (P < 0.05) in CWC7d + FK506 group. Conclusion Both CWC and WZC can increase Cmax and AUC0-t, prolong MRT0-t, reduce V/F and CL/F of FK506. CWC is better than WZC in increasing AUC0-t and inhibiting CL/F of FK506. CWC long-term administration is better than single-dose in improving Cmax, AUC0-t and reducing tmax of FK506.
ABSTRACT
OBJECTIVE:To establish a method for content determination of schisandrin and schisandrin B in compound wurenchun capsule by RP-HPLC.METHODS:Column lichrosphere C18 was used,mobile phase of water and MeOH(gradient elution)was set up,the flow rate was 1.0mL?min-1,the column temperature was 30℃and the detection wavelength was 254nm.RESULTS:The linear ranges of schizandrin and schisandrin B were within 0.182 4～1.641 6?g(r=1.000 3)and 0.189 6～ 1.706 4?g(r=0 .999 9),respectively.The average recoveries were 98.32%(RSD=1.02%)and 97.22 %(RSD=0.94%),respectively.CONCLUSION:The established method is convenient,accurate and highly specific,and it can be used for the quality control of compound wurenchun capsule.