Preparation And Pharmacokinetics Study Of Xiaoke Tablets

ObjectiveXiaoke tablets, on basis of xiaoke pills. It can not only reduce the dosage and ameliorate the symptoms, but also extenuate the side effects. In order to improve the xiaoke pills, we change the traditional dosage pill to tablet, and carry out the study on the quanlity control and Pharmacokinetics.MethodOrthogonal experiment was used to modify the extraction method for the Radix Puerariae; TLC methods on silica gel G were developed for the identification of puerarin in Xiaoke tablets; HPLC-UV methods were developed for the determination of puerarin and glibenclamide in the preparation; A HPLC-ELSD method was established for the determination of astragaloside IV in Xiaoke tablets. A HPLC-UV method was developed for the determination of glibenclamide in plasma of rats after oral administration of Xiaoke tablets.ResultIt was found that the best extraction method was eight times of water and five extraction hours; Chloroform- hexamethylene- alcohol- glacial acetic acid (2.5:3:4:0.5, v/v) solution was used as the mobile phase for the TLC identification of puerarin. The assay of puerarin was carried out on an Hypersil BDS C₁₈ column. The acetonitrile-water (15:85) solution was adopted as the mobile phase, the detection wave was set at 306nm. It showed good linearity from 1.26-2.94 mg with a mean recovery 101.92%. The determination of glibenclamide was carried out on Hypersil BDS C₁₈ column. The methanol-ammonium dihydrogen phosphate solution (5:3) solution was adopted as the mobile phase. It showed good linearity from 0.3048-0.7112μg with a mean recovery 97.98%. The Hypersil BDS C₁₈ (4.6×200 mm, 5μm) analytical column was used for the determination of astragaloside IV, and the mobile phase was consisted of acetonitrile-water(32:68). Temperature of drift tube was set at 105℃; Gas flow was set at 2.7 L/min; Gain was set at 1; Impactor was set off. The calibration curve was in good linearity over the range of 0.264-2.64μg (r=0.9998). The average recovery was 98.36%, RSD=1.12%. The determination of glibenclamide in the plasma was carried on a SinoChrom ODS-BP C₁₈ (200 mm×4.6 mm, i.d., 5μm) column with the mobile phase of acetonitrile-0.1% glacial acetic acid (44:56,v/v). Glipizide was chosen as the internal standard. The detection was set at 230nm. Both accuracy and precision of the were satisfactory. The plasma concentration-time curves of glibenclamide were plotted and the the pharmacokinetic parameters were calculated.ConclusionTablets cannot only be more convenient to take along with for the patient but also elevate the stability of the medicine. The method of quanlity control is simple, accurate and reproductive. This method applied for the pharmacokinetic study of glibenclamide is specific, accurate and reproductive.