ABSTRACT
Ketoprofen is widely used as non-steroidal anti-inflammatory drug. A potential sustained release ketoprofen tablet formulation was designed by orthogonal experiment on formulations composed of differential common excipients and homemade polymerides, and was screened by dissolution in vitro. The dissolution rate (%) of the ketoprofen tablet in simulated intestinal fluid was 16.6, 26.7, 42.2, 63.6, 83.1, 93.4, at 30min, 1, 2, 4, 6, 8 h, respectively. The plasma ketoprofen concentrations in six male volunteers were assayed after administration of a single oral dose (100 mg) of the sustained release tablet. It was found that the tablet formulation screened in vitro had sustained release effect in vivo too. This study suggests that there was a close correlation between the dissolution of sustained release ketoprofen tablet in vitro and the percent of dose absorbed in vivo, and the correlation coefficient was 0.9689. The influence of tablet hardness on the release rate of ketoprofen was also observed..
ABSTRACT
Uracil (I) (2,4-Diketo-pyrimidine) was isolated from the radix aconiti collected from Jiangyou region of Sichuan Province.The chemical structure of this principle was determined by elemental analysis,IR,UV,MS,'H and 13C-NMR spectral data. The experiments were made to study the effect of uracil (I) on the cardiac contractile force and beating rate of the isolated toad hearts in comparison with uracil (II) (artificial synthesis). The results indicated that the 5?mol/L of uracil (I) and uracil (II) both had the effect of increasing the amplitude of myocardial contraction (P0.05) at 3 and 5 min. When the concentration was increased to 10 and 20?mol/L, the amplitudes of myocardial contraction were more incremental and 3 min later,the estimated value of uracil (I) and uracil (II) to increase the amplitude of myocardial contraction by 50% approached to 4.17 and 4.68, respectively. As described above, uracil (I) is a new cardiotonic in Jiangyou Fuzi.