Studies On Extractive Method, Quality Standard Of Alkeqing Capsules, And Pharmacokinetics Of Icariin, A Bioactive Marker Of Aikeqing Capsules, In Sd Rats

Aikeqing Capsules, consist of nine Chinese herbal medicines including Herba Epimedii, Rhizoma Polygoni cuspidate, Radix Scutellaria, Radix Glycyrrhizae and so on, are a compound preparation used for treatment of HIV/AIDS. This Chinese herbal medicine can enhance the condition of Kidney, activeation of blood circulation and detoxication. Acordding to the raw medicinal materials of the preparation, orthogonal test was employed to evaluate the optimum extracting rates for the marker compounds icariin, polydatin, baicalin, Ilexsaponin A and glycyrrhizic acid from the raw medicinal materials. The optimum condition for extracting Herba Epimedii was reflux for two hours with 50% ethanol two times, each time with 25-fold of the raw material. The optimum condition for extracting the mixed herbal materials including Rhizoma Polygoni cuspidate, Radix Scutellaria, and Radix Glycyrrhizae, was reflux for two hours with 80% ethanol three times, each time with 10-fold of the raw materials. The extraction arts and crafts were proved stable and feasible, with extracting rates for the marker compounds being 65% to 83%, by intermediate scale extracting experiments. Base on the requirements of the Chinese Pharmacopoea and drug registration, we established TLC methods to qualitatively identify Hebra Epmedii, Rhizoma Pplygoni Cuspidati, Fructus Ligustri Lucidi, Radix Scutellariae, Radix Ilex pubescens Hook.etArnand, Radix Glyccyrrhizae of the preparation through identification of marker compounds icariin, polydatin, oleanic acid, baicelin, Ilexsaponin A and glycyrrhizic acid, and HPLC methods to quantitatively determine the contents of icariin, polydatin, baicalin, ilexsaponin A and glycyrrhizic acid. The quality standard established for the preparation were proved reasonable, practicable, and stable.A simple and rapid method was developed to study the pharmacokinetics of icariin and polydatin, bioactive marker compounds of the preparation, in rats. The concentration of the icariin in plasma were determined by a reversed phase HPLC-MSn method. There was a good linear relationship between peak area and concentration of icariin,over the concentration range of 5-260 ng/mL for icariin.The extraction recovery from the plasma was found as 86.6%-92.4%. The inter-day and intra-day coefficients of variation (RSD) of the lower concentration were less than 20% and the mid and high concentration were less than 10%.The pharmacokinetics'parameters were calculated with the software DAS2.0. The concentration-time profiles of icariin after oral administration were found to fit two-compartment models.There are some parameters for icariin as follow:t1/2β=0.627h, V1/F=40.82 L/kg, AUC0â†'t=204.722μg/L*h, AUC0â†'∞=208.27μg/L*h, Ka=4.093 h-1, ti/2a=0.322 h.