Study On The Pharmacokinetics Of β-Asarone From Acorus.Tatarinowii Schott.

It was reported that the volatile oil from Acorus.Tatarinowii Schott. has so many actions such as sedation, antispasm, conquer breath heavily and antiarrhythmia. β -Asarone is an activity component extracted from the Acorus. Tatarinowii Schott volatile oil. But reports about the pharmacokinetics of β -Asarone has not been seen at the present time. In this article, we developed a GC method for β -Asarone determination in blood and studied its pharmacokinetics.1. The oral administration pharmacokinetics of P -Asarone in the volatile oil from Acorus.Tatarinowii Schott. in rabbitsA capillary GC method was applied to determine the concentration of β-Asarone in blood. The P-Asarone was affirmed by a GC-MS method. The GC system was consisted of: HP-35 capillary column, Helium as carrier gas, oven temperature started at 30 ℃, then raised to 220 ℃ by a step of 6 ℃/min, stayed for 10 minutes, injector temperature at 250 ℃, detector temperature at 320 ℃ Injection volume was 2.01 with splitless inject mode. Methanol was used as solvent and a -naphthol as interior standard substance. The calibration curve in blood was linear in the range of 0.04 g/ml to 40 g/ml. The recovery for β-Asarone in blood was between 90.3% and 99.3%. The quantification limit was 0.04 g/ml. The intraday and the inter day relative standard deviation of precision were less than 11.0%. After oral administration of volatile oil from Acorus. Tatarinowii Schott., the inner body process of P-Asarone in rabbit accorded with 2-compartment model with 1st order absorption. The drug concentration reached the peak value in 20 minutes. 18min and 114min were obtained as T1/2a and T1/2β respectively. It was concluded that p-Asarone was absorpted and distributed rapidly and linearity kinetics was showed at the dosage range 0.1g.kg-1 to 0.4 g . kg-1.Absolute bioavailibility was as low as 9.0%.2. The oral administration pharmacokinetics of β -Asarone standard in rabbitsAfter oral administration of β -Asarone standard, the inner body process ofβ-Asarone in rabbit accorded with 2-compartment model with 1st order absorption too. But the Ka was increased and the T(peak), T1/2β, T1/2 , AUC were reduced obviously. We can see that the absorption, distribution and elimination of 3 -Asarone standard were more rapid. The possible reason was the influence of other components on the pharmacokinetics of P-Asarone.3. The absorption and distribution of β -Asarone in the volatile oil from Acorus.Tatarinowii Schott. in mice by oralAfter oral administration of the volatile oil, the inner body process of P-Asarone in mice accorded with 2-compartment model with 1st order absorption. 10min, 6.5min and 93.6min were obtained as T(peak), T1/2a and T1/2β respectively.The absorption and elimination of p-Asarone were speedy after ig in mice. P-Asarone could be detected in issues following 5min. Within 10min, the drug concentration in most of the issues achieved a high level. The concentration in small intestine was the highest. The kidney, the heart, the blood, the liver, the lung, the brain, the spleen and the muscle were inturn. The drug concentration in all these issues decreased more than 90% within 7h.Conclusions: The capillary GC method used to determine the concentration of β-Asarone in blood was exact , sensitive and simple. It was applied to study the pharmacokinetics of β-Asarone satisfactorily. After oral administration of volatile oil from Acorus. Tatarinowii Schott., the inner body process of β-Asarone in rabbit accorded with 2-compartment model with 1st order absorption.β-Asarone was absorpted and distributed rapidly and linearity kinetics was showed. The other components in volatile oil will influence the pharmacokinetics of β-Asarone. The absorption process of β-Asarone exsited difference between rabbit and mouse. The absorption and elimination of β-Asarone were speedy after ig in mice. The drug concentration in brain can reach a high level.