Preparation And Pharmacokinetics Investigation Of Qingfeixiaoyan Granules

This study aimed to investigate optimum condition for preparation of Qingfeixiaoyan granules, including preparation of essential oils from Herba Schizonepetae, preparation process and pharmacokinetics.Objective:Qingfeixiaoyan recipe, composed of Radix Puerariae, Herba Schizonepetae, Gypsum Fibrosuum, etc, is an empirical prescription in our hospital. With the effects of anti-inflammatory and relieving cough and asthma, the recipe was widely applied in the treatment of respiratory disease such as cough, colds, fever and chronic bronchitis. The original prescription was decoction. It had been applied clinically for many years and got significant effects. In order to serve the patients better during applieation, to get a well-controlled quality and to promote the paitients' compliance, we changed the recipe into granule and did a systematic research on aspects of extraction process, preparation process, quality standard and preparation preliminary stability.Methods:①Hot water extraction. Orthogonal array design was employed to optimize the ratio of water to raw material (X1:10-30 mL/g), extraction time (X2:1-3 h) and extraction temperature(X3:80-100℃) to obtain a high puerarin yield from recipe.②Including preparation of essential oils from Herba Schizonepetae. Clathrate compounds were prepared for inclusion complex yield and experimental oil contents in inclusion complex by ultrasonic-assisted technique, electric blender technique and incorporation technique, respectively.③The extract which comes from the preparing procedures of water extraction and alcohol precipitation was mixed with accessories (soluble starch and dextrin).④According to the Chinese pharmacopoeia 2010 version of I appendix C, Qingfeixiaoyan granules were carried through a routine inspection under the provisions of the granules.⑤Pharmacokinetics of orally administered at a dose of 61.6g/kg granules were investigated in mice. The effective puerarin concentrations in serum and organs were measured using HPLC and concentration-time data analyzed with Pharmacokinetical Kinetics Software.Results:①The optimum condition was A3B1C3, i.e., a ratio of water to raw material of 30 mL/g and extraction time of 3 h at 80℃.②Evaluated by inclusion complex yield and experimental oil contents in inclusion complex, ultrasonic was the best technique.③Analyzed by improve powder hygroscopicity, particle formability and economic cost, soluble starch and dextrin at the ratio of 2:1 as this auxiliary material was considered in this experiment.④The Qingfeixiaoyan granules were correspond with China pharmacopoeia 2010 version of I appendix C granules under rules.⑤The pharmacokinetic parameters were determined after ig of granules to mice. The main pharmacokinetic parameters of puerarin in mice were Cmax=1.575μg·L-1, tmax=1.000 h, t1/2α=0.3281 h, and AUC=6.039μg·L-1·h-1.Conclusion:The method to extract puerarin from recipe is simple and feasible. It can provide the scientific basis for further development of preparation of Qingfeixiaoyan granules. The preparation process and including preparation were reasonable and feasible. The HPLC method is steady and accurate with a good repeatability which can be used for pharmacokinetic analysis of puerarin. This study established a solid pharmaceutical basis for future research.