Résumé
The pharmacodynamic active parts of protecting liver of Peristrope japonica (thunb.) Bremek were identified. Rat acute liver injury model was induced by D-galactosamine (D-GlaN). The active parts were identified on the whole extraction and 4 fractions. The results showed that the pharmacodynamic active parts of Peristrope japonica were the n-BuOH fraction.
Sujets)
Acanthaceae , Médicaments issus de plantes chinoises/pharmacologie , Médicaments issus de plantes chinoises/usage thérapeutique , Galactosamine , Lésions hépatiques dues aux substances/étiologie , Lésions hépatiques dues aux substances/prévention et contrôle , Tests de la fonction hépatique , Phytothérapie , Agents protecteurs/pharmacologie , Agents protecteurs/usage thérapeutique , Répartition aléatoireRésumé
The pharmacodynamic active parts of protecting liver of Peristrope japonica (thunb.) Bremek were identified. Rat acute liver injury model was induced by D-galactosamine (D-GlaN). The active parts were identified on the whole extraction and 4 fractions. The results showed that the pharmacodynamic active parts of Peristrope japonica were the n-BuOH fraction.
Sujets)
Animaux , Femelle , Mâle , Rats , Acanthaceae , Lésions hépatiques dues aux substances , Médicaments issus de plantes chinoises , Pharmacologie , Utilisations thérapeutiques , Galactosamine , Tests de la fonction hépatique , Phytothérapie , Agents protecteurs , Pharmacologie , Utilisations thérapeutiques , Répartition aléatoireRésumé
AIM To study the pharmacokinetic characters of dauricine(Dau) in rats after different administration ways. METHOD RP-HPLC method was used in the study. RESULT The results indicated that the plasma C-T curve conform to two-compartment open model after iv. The plasma concentration of Dau in rats after ig Dau 150 mg*kg-1 is low, less than 1 mg*L-1 of peak concentration. The absolute bioavailibility is about 16.6 %. The plasma concentration-time profile shows a double-peak phenomenon. The time taken to reach the peak is about 15 min after ig and the trough time is 3 h. The plasma concentration increased again in 4 h to form the second peak. The studies suppose a stomach-intestine recirculation of Dau is the major reason for double-peak phenomenon. Dau has a wide distribution in rat body. It lies in all tissues and organs in both adminastration ways. The tissue Dau concentration are hundreds times higher than that in plasma concurrently. Feces is the main route whereby Dau are excreted from the rats after ig 150 mg*kg-1. The excreted percentage through feces is 26.29 %, while through urine is 4.93%. The total amount is 31.22% after 48h of oral administration of Dau. The study of the mean percentage of the dose remaining in stomach, small intestine, large intestine and whole GI tract from each rat sacrificed at different times after oral administration of Dau suggest the stomach-intestine circle. CONCLUSION The bioavailibility of Dau is low. The plasma drug concentration versus time curve shows an innormal double-peak phenomenon. Dau can distribute abroadly to almost all kinds of the tissues in rats. The main excretion routes are through feces and urine. The pilot study suggests that stomach-intestine circle be the main reason for the innormal double-peak phenomenon.
Résumé
To establish the determination method of dauricine (Dau) concentration in rats' blood and other biological samples, a reverse-phase HPLC method was adopted. Under the given condition, dauricine could be well separated. The retention time (tR) of Dau and its internal standard,daurisoline were 9.2 and 6.1 respectively. The detection limit was 10-2 mg/ml. The absolute recoveries of all kinds of samples were above 70%, and the relative ones were over 85%. A good liner relationship has been obtained over the entire range of 0.030 to 3.000 mg/L in blood samples and 0.050 to 5.000 mg/L in other tissue samples. The intraday and interday coefficients of variation were below 10%. The results showed that the method can be used for detecting Dau in all kinds of biological samples.
Résumé
To establish the determination method of dauricine (Dau) concentration in rats' blood and other biological samples, a reverse-phase HPLC method was adopted. Under the given condition, dauricine could be well separated. The retention time (tR) of Dau and its internal standard,daurisoline were 9.2 and 6.1 respectively. The detection limit was 10-2 mg/ml. The absolute recoveries of all kinds of samples were above 70%, and the relative ones were over 85%. A good liner relationship has been obtained over the entire range of 0.030 to 3.000 mg/L in blood samples and 0.050 to 5.000 mg/L in other tissue samples. The intraday and interday coefficients of variation were below 10%. The results showed that the method can be used for detecting Dau in all kinds of biological samples.
Résumé
The in-vivo bioavailability of Qingxintong administrated by intramuscular injection, intravenous injection and gastric infusion was compared. Experimental results showed that Qingxintong was rapidly absorbed and excreted. The half-life time for absorption was 0.05 - 0.07 h and the half-life time for elimination was 0.14 - 0.29 h. The bioavailability of Qingxintong in the dose of 10 mg/kg by intramuscular injection or by intravenous injection was 94.71 %, and was 9.16% in the dose of 60 mg/kg by gastric infusion or in the dose of 10mg/kg by intramuscular injection.