ABSTRACT
OBJECTIVE To determine the pharmacokinetic parameters of perlolyrine in rats.METHODS The plasma concentration and pharmacokinetic parameters of perlolyrine were determined by means of GC-MS with selected ion (m/z 247 and m/z 248) and ［2-15N］perlolyrine(m/z 248) as the internal standard.RESULTS The concentration-time profile of perlolyrine after oral administration of perlolyrine fitted a two-compartment open model.The pharmacokinetic parameters were t1/2α=0.31 h, t1/2β=4.62 h, t1/2ka=0.10 h, tmax=0.34 h, cmax=18.74 ng.mL-1,K12=0.82 h-1, K21=0.38h-1,K10=0.29 h-1,Vb=108.16 L.kg-1,AUC=98.54 ng.h.mL-1,respectively.CONCLUSION The method is constant,sensitive and accurate.It provided a scientific basis for the clinical use of perlolyrine.
ABSTRACT
The influences of propylene glycol mannate sulfate (PGMS) on experimental thrombosis and thrombolysis in vivo were studies after iv 8. 125, 6. 25, 12. 5 , 25mg/Kg in rabbits, and the effect of antithrombosis of PGMS was compared with that of heparin. The results showed that PGMS possessed remarkable effect of antithrombosis. In order to explore the mechanism of antithrombosis of PGMS, we studied the influences on the fibrinolytic and coagulant function of rabbits. The results showed that PGMS can pronouncedly prolong the prothrombin time (PT), thrombin time (TT), kaolin partial thromboplastin time (KPTT), and enhance the activity of antithrombin-III (AT -III). PGMS can cause a remarkable increase in fibrin degradation product (FDP) , shorten euglobulin lysis time (ELT) , and a decrease in the contents of fibrinogen and plasminogen activity. These results suggested that PGMS probably exert the antithrombotic effect by inhibiting coagulation and activating fibrinolysis.
ABSTRACT
TMP. The results suggested that 12D-TMP and 6D-TMP possessed remarkable isotope effects, and that the pyrazine ring of TMP may be responsible for its pharmacodynamics, while the substituted groups might primarily govern its pharma-cokinetics and toxicity. The results also indicated that to study the structure activity relationship of TMP and to modify its chemical structure are very fruitful for the development of TMP analogues of high potency.
ABSTRACT
Experimental research showed that Gan Tang Zhi can influence blood clotting and plasma fibrinolytic system of rabbits, 15min after introvenous injecting 6.25mg/kg or 25mg/kg Gan Tang Zhi into rabbit it can pronouncedly prolong prothrombin time ( PT ) , thrombin time ( TT ) , and kaolin partial thromboplastin time ( KPTT ) ; and cause remarkable increase of fibrin degradation product ( FDP ) , Gan Tang Zhi can also shorten englobulin lysis time (ELT) and decrease fibri-nogen.