| To study the material basis and analgesic mechanism of Lamiophlomis rotata(Benth.)kudo , a medicinal plant in xi-zang(tibet). Component were separated by extraction with solvent and gradient elution with macroporous adsorptive resin. Screening effective part of analgesic by acetic acid writhing and hot plate test in mice,and analysis the analgesic mechanism. Samples of separated by two methods have obviously analgesic pharmacological action to writhing reaction by acetic acid in mice,and could prolonged the latencies of paw licking behind 3h,but inefficacy in 2h to gradient elution with macroporous adsorptive resin, n-butanol extract petroleum ether extract and water extract were mainly effective parts of analgesic in extraction with solvent;30% ethanol 90% ethanol elution parts and precipitate were mainly parts of gradient elution with macroporous adsorptive resin. Lamiophlomis rotata(Benth.)kudo has significant analgesic pharmacological action ,and the site of analgesic mechanism is located in the periphery.Study the technological parameters of the purification process of total flavones from Lamiophlomis rotata with macroreticular resin.The static capacity adsorption static elution ratio dynamic saturation ratio dynamic absorption ratio dynamic eluation ratio of eight types macroreticular resins were studied and compared and find the best macroreticular resin. Then, technical process for purification of total flavones with the best macroreticular resin were screening by total flavones product purity and yield. LSA-10 type macroreticular resin have best adsorption and eluation parameters. The dynamic absorption ratio were 100.6 mg g-1 and washed with 3BV of distilled water ,then eluted with 3BV of 50% ethanol , yield of total flavones was 85% and product purity was 94.5%. The LSA-10 type macroreticular resin showed better comprehensive adsorption property.It can be used to purify the extract of Lamiophlomis rotata.Use central composite design to optimize the preparation of dispersible tablets . Dispersible tablets was prepared by direct compression method .The effects of dissolution time(t80 of luteoloside ), disintegration time, suspended coefficient and overall desirability value on the PVPP, pregelatinized starch and colloidal silicium dioxide were investigated .The optimal formulation was established by the central composite design and response surface method. A second-order polynomial equation was fitted to the data and resulting model was used to predict the response in the optimal region . All the investigated response variables were found to be highly dependent on the formulation variables. Lamiophlomis rotata dispersible tablets were prepared by selecting 12% PVPP as disintegration, 14% Pregelatinized Starch as sweller ,3% Colloidal silicium dioxide as Lubricants and Clidants agents and 45% MCC as filler. Under the optimized condition , the values of dissolutiontime(t80 of luteoloside disintegration time suspended coefficient were 1.68min 20.6s 0.0689. In conclusion , fast dispersible tablets with acceptable hardness and desirable taste could be prepared within the central composite design .To develop a sensitive and rapid HPLC method for the determination of luteoloside in rat plasma and to study its pharmacokinetics in rat. Luteoloside in plasma of rat at different samples time was determined after single dose 30mg kg ig by RP-HPLC.The mean plasma concentration-time curve was protracted and pharmacokinetic parameters were calculated. The linear calibration curves were obtained in the concentration range of 0.412 ~ 32.96 mg L-1, the main pharmacokinetics parameters as follows: the value of T1/2 was (2.44?.54)h , AUC0- was (82.31+3.22)mg h L-1 The method is shown to be accurate and convenient,and will be suitable in determination of luteoloside in plasma and pharmacokinetics. |
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