Experimental study of pharmaceutic stress myocardial perfusion imaging with higenamine / 中华心血管病杂志

<p><b>OBJECTIVE</b>To evaluate the applicative value of higenamine used as a new agent for pharmaceutical stress test in detection of coronary artery disease by radionuclide myocardial perfusion imaging.</p><p><b>METHODS</b>Thirteen pigs with chronic coronary artery stenosis by placement of the Ameroid constrictor in the middle section of left anterior descending artery were included in this study. Rest, higenamine and dobutamine stress radionuclide myocardial perfusion imaging was performed with Tc-99m-sestamibi.</p><p><b>RESULTS</b>The sensitivity for detection of coronary artery disease by radionuclide myocardial perfusion imaging was 85% in both higenamine and dobutamine stress imaging. Imaging scores (9.9 +/- 8.5 vs. 9.4 +/- 8.6, P = NS) and defect severity (68% +/- 12% vs. 68% +/- 15%, P = NS) showed no significant difference between higenamine and dobutamine stress test. Agreement of imaging scores between higenamine and dobutamine stress imaging was good (kappa = 0.849, P < 0.0001).</p><p><b>CONCLUSION</b>Our study demonstrates that detection of coronary artery stenosis and ischemic myocardium by myocardial perfusion imaging with higenamine is highly sensitive.</p>

Pharmacokinetics and relative bioavailability of probucol inclusion complex capsule in healthy dogs / 药学学报

<p><b>AIM</b>To study the pharmacokinetics and relative bioavailability of probucol inclusion complex capsule.</p><p><b>METHODS</b>Following oral administration of a single dose of 250 mg of conventional tablet (formulation A, purchased from the market) and probucol inclusion complex capsule (formulation B, a new formulation for preclinical trial) to each of 6 healthy dogs in a randomized crossover design, the plasma levels of the active drug at different time points were determined by HPLC and the plasma concentration-time profiles of formulation A and B were obtained. The pharmacokinetic parameters as well as relative bioavailability were analyzed.</p><p><b>RESULTS</b>The concentration-time curves of formulation A and formulation B were found to fit a two-compartment open model. The Tmax values of formulation A and formulation B were (9.3 +/- 2.1) h and (9.3 +/- 2.1) h, the Cmax values were (1.5 +/- 1.0) microgram.mL-1 and (2.3 +/- 0.9) microgram.mL-1 and the AUC0-240 values were (85 +/- 56) microgram.h.mL-1 and (134 +/- 55) microgram.h.mL-1, respectively. The relative bioavailability of formulation B was found to be (198 +/- 90)% compared with formulation A. The results of variance analysis and two one-side t-test showed that there was significant difference between the two formulations in the AUC0-240.</p><p><b>CONCLUSION</b>The high bioavailability by the inclusion of formulation B is attributed to the improvement of its water-solubility by the inclusion process and this is supposed to be a key factor for improving drug bioavailability.</p>