Studies On Matrine Sustained-release Tablet

Matrine has been obtained from the Chinese drug Kuh Seng or the Japanese Shinlcyogan, the dried roots of Sophora an gust zfolia Sieb. In clinic, it is used in acute and chronic hepatitis and malignancy. Matrine was used as a water soluble drug model to prepare sustained- release oral matrix tablets that included its effective time and bioavailiability. The influence of composition factors and dissolution conditions on in vitro dissolution behavior was evaluated by orthogonal design. The formulation of sustained-release Matrine tablet using the combination of Carbopol and HPMC was screened. The dissolution profiles of Matrine sustained-release tablet conform to Higuchi formula whose dissolution index was : t30%=1OOmin, t50%=252min, t80%=6O8min. The release rate depends on the content of HPMC and Carbopol. The result showed dissolution rate was not affected by dissolution method~ pH and press strength of tablet. Acid-base titration method was used in determination of Matrine. UV method was used in determination of Matrine tablet and dissolution. Recovery of determination of Matrine (n5) was 99.56 ?0.59% Accuracy of determination of Matrine was 0.65% within day and 0.70% between day. Matrine concentrations in dog plasma were determined by RP-HPLC method. The mobile solution is methanol: H20: diethylamine=70:30:0.02. The calibration curve points of Matrine in dog plasma are between 0.3 12$-40.0 u g/ml ( Y =0.9996), minimum limit of detection is lSng/m10 Recovery of determination were 105.72% 101.83% and 100.115%. Accuracy of determination was 1.053% within day and 0.654% between day. Studies were carried out in eight dogs after single a oral administration of the self-prepared sustained-release tablet.. marketed capsule and marketed injection in a randomized crossover way. A two- compartment open model was adopted. Calculated areas under curve (AUC) were 2105 ug/ml-min 1344.31 ug/ml*min and 1456.7 ug/ml*min with respective of sustained-release tablet (300mg).. marketed capsule (300mg) and marketed injection(lSOmg). The mean residence time (MRT) in dogs was 301.3mm and 237.3mm. The results demonstrated that in vitro and in vivo correlation in dogs was very significant (p<0.0 1). Consequently, Matrine sustained-release tablet dosed twice a day is expected to show the same efficiency as marketed injection affirming with the designed requires.