Preclinical Pharmacokinetics Of Ligustilide / Cyclodextrin Series Inclusion Complex

Ligustilide, which is the main active compounds of Chuanxiong, with a strong pharmacological effect, is currently one of the important bases for evaluating the quality of medicines and preparations such as angelica, chuanxiong and so on. There are many reports on pharmacology, but most of the experiments is complished with Angelica oil and Chuanxiong oil mixture containing ligustilide, and thus the pharmacological studies are not enough depth and detail. This is due to the instability of ligustilide which lead to pure products preparation and preservation of the more difficult. Therefore, it is the research focus on developing a better stability and water-soluble drug delivery system.In recent years cyclodextrin (cyclodextrin, CD) and its derivatives in drug development in more and more widely. Cyclodextrin (Cyclodextrin, CD) is a cyclodextrin glucosyltransferase starch under the action of the enzyme obtained from 6 to 12 D-pyran-type glucose molecules through the a-1,4 glycosidic bond to form the ring Oligosaccharides natural products. Is a hollow "molecular capsule" can be the size of the inclusion of hydrophobic guest molecules to form a special kind of inclusion, so that the drug stability, solubility, dissolution rate, volatility, degree of physical and chemical nature of the release of significant Changes in molecular recognition, simulation Chiral separation of enzymes and has high research and application.This paper examines the ligustilide bioavailability and tissue, ligustilide/β-cyclodextrin inclusion complex, Ligustilide/methyl-β-cyclodextrin and the materials. PO 400 mg/kg of raw materials Ligustilide,300 mg/kg Lig-β-CD,100 mg/kg Lig-methy-β-CD after the plasma drug concentration-time curves fitted well by non-compartment model to estimate the absolute bioavailability was 100%,7.47%,20.12% and 35.86%. Shows that the two ligustilide cyclodextrin were raised ligustilide bioavailability.In the methodological part of this study the pretreatment of biological samples using liquid-liquid extraction of n-hexane extraction method to improve the methodology for the recovery and sensitivity.