| ObjectiveExtraction and purification of β-asarone, to determine the best molding process of ShenQing dripping pills, and quality standards inspection preparation, Preliminary investigation of stability and pharmacokinetic studies to provide scientific, production and application in the future ShenQing dripping pills basis.Methods(1) To extract the volatile oil from the gramineus herbs, and then use of freezing crystallization purification of β-asarone.(2) Preparation conditions using a single factor test to determine inspection dripping pills, roundness, hardness, trailing, adhesive and other indicators, respectively, the ratio of the coolant, matrix, drug and matrix, the dripping temperature, coolant temperature, The dropper caliber, drops from the study to determine the process conditions.(3) Dripping Pills beta-asarone and eugenol content was determined by HPLC, and ShenQing dripping:pills pills weight variation, dissolution time and to inspect the appearance of quality indicators.(4) By speeding up the experiment, the appearance of ShenQing dripping pills, content, pills, weight variation and dissolution time indicators to inspect.(5) Dripping Pills plasma concentration of beta-asarone and eugenol in rats by intragastric administration, inspection, and half-life ti/2, time to peak Tmax is the peak concentration, Cmax, and other kinetic parameters, and β-asarone monomer Dripping Pills group pharmacokinetic parameters in rats.Results(1) ShenQing dripping pills preparation process:optimal conditions for beta-asarone and eugenol, the better compatibility ratio of4:1as a raw material drugs, drop pills of PEG4000:PEG6000=1:6matrix, matrix anddrug ratio of7:1,80for drops away from5cm drip for30d/min conditions under trickle-down gradient condensation of liquid paraffin.(2) Quality standards:ShenQing dripping pills of β-asarone and eugenol were9.43%and2.18%. Dripping pills weight about30mg, dropping pills dissolution time required.(3) Preliminary stability study:In the accelerated test conditions, the appearance of ShenQing dripping pills, pills, weight, dissolution time and content to remain stable.(4) Pharmacokinetic Study:Rats were β-asarone Dripping Pills suspension absorbed at Tmax=10min to reach peak Cmax=1.3948mg/L, absorption half-life t1/2a=1.975min, elimination half-life t1/2β=93.286min, the area under the plasma concentration-time curve AUC=48.41mg/L*min, After the suspension of the the intragastric ShenQing dripping pills, the absorption peak at Tmax is=30min to reach Cmax=0.8965mg/L, and absorption half-life t1/2a=13.005min, elimination half-life t1/2P=17.489min, the plasma concentration-time The area under the curve AUC=57.747mg/L*min.Conclusion(1) The stability of the preparation process of the optimization of ShenQing dripping pills, forming rate.(2) A method for the determination of ShenQing dripping pills has established; and the development of dripping pills the rest of the quality program.(3) ShenQing dripping pills in the basic stability of the accelerated test conditions to achieve the preparation design requirements.(4) Dripping Pills group (ie, β-asarone and eugenol compatibility group) time to peak of about30min, time to peak of β-asarone monomer group of about10min, visible and eugenol compatibility, can significantly extend thetime to peak of β-asarone.From the distribution half-life, pills group of approximately13.005min, monomer is1.975min, visible compatibility with eugenol, can significantly increase the distribution half-life of β-asarone. From the elimination half-life, pills group of approximately17.489min, the monomer of93.286min, found compatibility with eugenol, can significantly shorten the elimination half-life of β-asarone. The reason to be explored.From the peak concentration, the compatibility group prorated.8965X1.25=1.1206(mg/L),1.395similar to the monomer group, suggesting that compatibility with eugenol, the plasma concentration of beta-asaronenot obvious. |
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