ABSTRACT
OBJECTIVE: To develop a highly sensitive and specific LC-MS/MS method to explore the pharmacokinetic properties of araloside A. METHODS: Araloside A was administered in a dose of 50 mg•kg-1 via gastric in fusion and 5 mg•kg-1 by intravenous injection in rats. Araloside A was analyzed by a validated LC-MS /MS method in plasma after intravenous and intragastric administration. The pharmacokinetic parameters were evaluated by software DAS 3.0. RESULTS: The results of pharmacokinetic study showed that the linear range of araloside A was good in 1.0 - 10 000.0 μg•L-1 (r > 0.994 8). The specificity, precision and accuracy, matrix effect and extraction recovery rate and stability all meet the requirements. The main pharmacokinetic parameters for intragastric administration with araloside A 50 mg•kg-1 and intravenous injection of araloside A 5 mg•kg-1 were as follows: t1/2 was (8.65 ± 3.22 ) and (2.00 ± 0.21) h, AUC0-t was (277.14 ± 101.00) and (21 194.59 ± 4 385.13) ng•h•L-1, MRT0-t was (7.88 ± 0.64) and (1.21 ± 0.11) h, Vd/F was (2 229.99 ± 1 013.97) and (0.71 ± 0.20) L•kg-1, CL/F was (149.11 ± 62.28) and (0.24 ± 0.05) L•h-1•kg-1, respectively; ρmax was (32.68 ± 10.74) μg•L-1 for intragastric administration and tmax reached(1.21 ± 0.70) h, oral bioavailability of araloside A was about 0.14%. CONCLUSION: The LC-MS/MS method established is specific and sensitive, and can be successfully applied in basic pharmacokinetic study of araloside A in rat plasma.
ABSTRACT
Araloside A is one of the main active ingredients of Aralia taibaiensis. In this study, HPLC-MS/MS analysis method of araloside A in the main organs of SD rats was established. At the same time, the content of araloside A in the main organs (heart, liver, spleen, lung, kidney, brain) after oral administration with araloside A (50 mg•kg⁻¹) were determined to explore the tissue distribution characteristics of araloside A in vivo. The results showed that the methodological study of araloside A in the main organs of SD rats met the requirements, araloside A distributed in heart, liver, spleen, lung, kidney and brain tissues reached peak at 1 h or 2 h after oral administration with 50 mg•kg-1.The distributions of araloside A at different time points after administration were distinct as follows： the content of araloside A at 20 min：liver>heart>spleen>lung>kidney>brain; the content of araloside A at 1 h： liver>spleen>kidney>lung>heart>brain; the content of araloside A at 2 h： liver>kidney>heart>spleen>lung>brain; the content of araloside A at 4 h： kidney>liver>spleen>heart>lung>brain; the content of araloside A at 8 h： spleen>heart>liver>kidney>lung>brain. Therefore, araloside A was mainly distributed in liver tissue, which had a certain correlation with the common use of Aralia taibaiensis in the treatment of hepatic disease. In addition, araloside A shows a low content but an obvious distribution in brain tissues, which indicates that the drug can pass through blood-brain barrier, and provides the basis for the study of araloside A in brain tissue.
ABSTRACT
Objective: To explore the optimal separation of the araloside A from Aralia chinensis by selecting appropriate macroporous resins and to systematically study the factors which affect the separation. Methods: Static and dynamic adsoption-desorption methods were adopted and evaluated for separating efficiency by measuring the concentration of araloside A in A. chinensis with HPLC. Results: Macroporous resin AB-8 had the best separating efficiency when the content in A. chinensis liquid was 0.1 g/mL equivalent to raw material. The volume of drug is 6 BV (resin bed volume) with the adsorption-power 2.5 BV/h and the volume of 50% ethanol as eluant 4 BV with desorption-power 2 BV/h. After the treatment of AB-8 resin, the purity of araloside A could reach 30% and total araloside to 80%. Conclusion: This method is simple and feasible with good effect of separation, which can meet the industrial requirements.