[The pharmacokinetics and pharmacodynamics of intranasal preparation of Panax notoginseng Saponins].

AIM: To investigate the pharmacokinetic course of intranasal powders of Panax notoginseng Saponins (PNS) in a rat model and its protective effects against cardio-cerebrovascular diseases administrated in the form of its suspension. METHODS: After administration, Rgl concentration in the serum was analyzed by HPLC and the absolute bioavailability was calculated. The protective effects against cardia-cerebrovascular diseases were studied on actue myocardial infarction model in rats built by occlusion of left coronary artery and cerebral ischemia-reperfusion model in gerbils built by occlusion of bilateral common carotid artery (CCA). RESULTS: The in vivo course of Rgl in rats conformed to two-compartment model after intranasal administration of PNS suspension and the absolute bioavailability was 103.56%. The suspension significantly reduced myocardial infarct size induced by occlusion of the left coronary artery, alleviated cerebral edema and the stroke symptoms induced by occlusion of bilateral common carotid artery (CCA). And the effects were dose-dependent, the higher dose, the better effects. CONCLUSION: The results of pharmacokinetics and pharmacodynamics demonstrated that PNS intranasal preparation has a pretty prospect to develop.

[The in vitro kinetics of uptake, transport and efflux of 9-nitrocamptothecin in Caco-2 cell model].

AIM: To study the kinetics of uptake, transepithelial transport and efflux of 9-nitrocamptothecin (9-NC). METHODS: A human intestinal epithelial cell model Caco-2 cell in vitro cultured had been applied to study the kinetics of uptake, transport and efflux kinetics of 9-NC at small intestine. The effects of time, pH, temperature and P-glycoprotein inhibitors on the uptake of 9-NC were investigated. The determination of 9-NC was performed by HPLC. RESULTS: The uptake and absorption of 9-NC were passive diffusion as the dominating process. The uptake of 9-NC is positively correlated to uptake time, and negatively correlated to pH and temperature. The inhibitors, cyclosporine A and verapamil, significantly enhanced the uptake amount of 9-NC (P < 0.05). P(app) of Basolateral to Apical was much more than that of Apical to Basolateral (2.6-6.9 fold). The efflux of 9-NC was fitted to apparent two-order process. The m0 [(148.0 +/- 2.2) pmol x cm(-2)] and the efflux rate (41.1 pmol x cm2 min(-1)) on Apical side were higher than the m0 [(121 +/- 7) pmol x cm(-2)] (P < 0.05) and the efflux rate (29.2 pmol x cm2 x min(-1)) on Basolateral side (P < 0.01). CONCLUSION: The uptake and absorption of 9-NC were passive diffusion as the dominating process. P-glycoprotein had strong efflux effects on the uptake and transepithelial transport of 9-NC.