| Acori tatarinowii rhizoma (AC) belonging to the family Araceae is one of aromatic resuscitation drugs. Modern pharmacological studies have shown that the rhizomes of AS possessed a lot of pharmacological and biological activities such as sedative, anticonvulsant, antiepileptic, neuroprotective, activities, and to play this role of the active substance is AC volatile oil (ACO). In this paper, ACO is the research object to investigate its extraction method, analyze its chemical components by MS, determine β-asarone, a-asarone, methyl eugenol three phenylpropanoid components in it, develop β-asarone and a-asarone pharmacokinetic process in rats.Firstly, steam distillation method was adopted to extract ACO using the recovery rate of volatile oil as indicator and quantity of water, soaking time and extraction time as affecting factors. The optimal extraction process is as follows:cut crude drugs were soaked in9times water for2h, distilled for5h with vapour.The volatile constituents of AC from four growing areas:Sichuan, Zhejiang, Jiangxi, Jiangsu were investigated by gas chromatography-mass spectrometry(GC-MS). Total of61volatile constituents were tentatively identified. There were21common volatile constituents in ACO. The components and constituent contents were different due to different origins.β-Asarone and a-asarone in Sichuan had the highest concentration by peak area normalization method, while Jiangxi had the lowest.GC-MS method was applied to determine the concentration of β-asarone, a-asarone, methyl eugenol. The results showed that, β-asarone, a-asarone and methyl eugenol in the concentration range investigated good linear relationship (R>0.9996) and high sensitivity. Three compounds precision, stability and reproducibility of the RSD values were≤2.0%, recoveries were103.7%,102.7%,99.40%, indicating that the method was reliable, reproducible and accurate.GC-MS method was selected to determine β-asarone, a-asarone concentration in rats blood and brain tissue. Pharmacokinetic study of β-asarone, a-asarone after oral administration of the rhizomes of AC essential oil to rats was developed. a-Naphthol was chosed as internal standard and acetonitrile:methanol (9:1, V/V) was used to precipitate proteins. Pharmacokinetic parameters were calculated by the linear trapezoidal rule. The main pharmacokinetic parameters including time to reach the maximum concentrations (Tmax), maximum plasma concentration (Cmax), half-time(ti/2), area under concentration-time curve (AUCo't) were1.58±0.34h,2605.7±536.6μg·L-1,2.04±0.14h,12499.2±1314.4μg·h·L-1(β-asarone);1.58±0.61h,264.8±29.1μg·L-1,2.92±0.66h,1399.5±191.1μg·h·L-1(α-asarone), respectively. It was illustrated that the analytes had the similar oral absorption and distribution, which may contribute to their similar structures. The main pharmacokinetic parameters in brain tissue were0.7±0.27h,3160.8±577.1ng·g-1,1.39±0.11h,6702.2±860.1ng·h·g-1(β-asarone);0.7±0.27h,639.9±109.8ng·g-1,0.94±0.38h,979.3±165.6ng·h·g-1(a-asarone). β-Asarone and a-asarone could be rapidly detectived after of administration indicating that both can quickly enter the blood-brain barrier.The results of this thesis show that the extraction process is simple, feasible. The method of quality standard is high accuracy, good reproducibility. Pharmacokinetics laid an important material basis for the treatment of central nervous system diseases. |
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