Qiguanyan 4 Dispersible Tablet's Preparation And Its Effect On Amoxicillin & Aminophylline Pharmacokinetics

Qiguanyan 4(compound recipe xiaoyepipa tablet), which is developed by The Second Hospital of Lanzhou University, is proved to possess the function of resolving sputum, relieving asthma, smoothing cough, and spasmolysis after many years' clinical application.The prescriptions of Qiguanyan 4 include rhododendron anthopogonoide, zedoary, epimedium and scutellaria baicalensis, which are prepared into normal tablets. In order to increase its dissolution, improve the bioavailability and decurtate the time to become effective, this paper tries to prepare it into dispersible tablet and study its effect on Pharmacokinetics of Amoxicillin and Aminophylline.A general study on Micromeritics properties of Qiguanyan 4 powdered extract and adjuvant, including flowability,filling ability and hygroscopicity of Qiguanyan 4 powdered extract and adjuvant, swelling volume ratio of disintegrants. So appropriate adjuvant and preparation techniqie can be selected.Single factor experiments were designed to select types of weting agent according to granulating effect, types of attenuant, disintegrants and swelling adjuvant with disintegration time as main parameter, types and dosage of lubricating agent with angle of repose as indicator. Orthogonal experiment was applied to select the dosage of Qiguanyan 4 powdered extract, polyvinylpolypyrrolidone and hydroxypropyl cellulose, using disintegration time as main parameter. Through range analysis and variance analysis of experimental results to select optimum prescription and preparation techniqie of Qiguanyan 4 Dispersible Tablet. Estalished quality evaluation system on Qiguanyan 4 Dispersible Tablet. Reproducible test results of tri-batch Qiguanyan 4 Dispersible Tablet showed that the mean disintegrating time is 80s and dispersal homogeneity is very good of Qiguanyan 4 Dispersible Tablet which prepared according to optimum prescription and preparation techniqie consistent with the requirements of Chinese Pharmacopoeia.Using dissolution percentage of quercetin, to inspect the dissolution rate of Qiguanyan 4 Dispersible Tablet, quercetin's dissolution percentage were over 95% of tri-batch Qiguanyan 4 Dispersible Tablet when dissolution 10 min.With self reference method, Qiguanyan 4 Dispersible Tablet's effects on Amoxicillin or Aminophylline Pharmacokinetics in rabbit have been studied. The data of concentration-time curve were processed by 3p97 software, pharmacokinetics model of Amoxicillin in rabbit body meet single compartment model of 1/c/c weighting coefficient when Amoxicillin is applied alone or combined with Qiguanyan 4 Dispersible Tablet. T test on Pharmacokinetics parameter of Amoxicillin is applied alone or combined with Qiguanyan 4 Dispersible Tablet indicates that there is no significant difference in all parameters (P>0.05). The experiment results show that the transport and metabolise of Amoxicillin and Qiguanyan 4 Dispersible Tablet are no distinct interaction in rabbit body. Pharmacokinetics model of Theophylline in rabbit body meet two compartment model of 1/c/c weighting coefficient when Aminophylline is applied alone or combined with Qiguanyan 4 Dispersible Tablet. T test on Pharmacokinetics parameter of Aminophylline is applied alone or combined with Qiguanyan 4 Dispersible Tablet, results indicate that hybrid parameter A increases 44%(P<0.05), Vc decreases 18%(P<0.05), Cmax increases 17%(P< 0.05), whereas there will be no significant difference in other parameters. Qiguanyan 4 Dispersible Tablet and Aminophylline application together will lead to concentration rise of Theophylline Cmax. Therefore, it is advisable to enhance clinical observation, and if necessary, monitor Theophylline concentration in plasm when Qiguanyan 4 Dispersible Tablet and Aminophylline are applied together or reduce it dosage.