AIM To investigate the reativative and protective effect of Neferine (Nef) on the poisoning mice of cholinesterase (ChE) with dichlorves (DDVP) or dipterex (Dip) of LD 100 . METHODS The mice were randomly divided into poisoning group with DDVP or Dip and Nef, Atropine and Pyraloxime methylchloride (PAM Cl) treatment group. Activity of mice blood ChE was determined with Ellmaris method, and acute toxicity experiment was used to determine the protective effect. RESULTS ① Nef (15 mg?kg -1 , ip) exhibited a definite protective effect on poisoning mice, and the mortality of the animals treated with Nef was significantly lower than that of the control group with normal saline ( P 0 05). But Nef and atropine group was significantly lower than that of thePAM Cl group ( P

This study is to investigate the transportation of scutellarin in cell and live models and study on mechanism of absorption and transport of scutellarin in mouse liver. The concentration of scutellarin in plasma and liver from control and pretreated groups was determined by high performance liquid chromatography. The uptake of scutellarin was examined in control hepatocytes group, induced hepatocytes group and induced hepatocytes plus pravastatin group. Pravastatin can affect the pharmacokinetics of scutellarin in mouse: CL is decreased while AUC is increased. The scutellarin absorption of hepatocyte induced group was higher than that of control group, but was decreased in the group with pravastatin added. The research showed that there was potential drug interaction between pravastatin and scutellarin. The drugs may compete for oatp2 mediated transport pathway consisted in the uptake of scutellarin in liver.

AIM: To study the linear relationship between pharmacokinetic parameters and doses about potassium clavulanic acid (CAV) and amoxicillin (AMX). METHODS: 15 healthy male volunteers were randomly divided into 5 dose groups. The plasma concentration of CAV and AMX was determined by high performance liquid chromatography (HPLC) method. The pharmacokinetic parameters obtained with 3p97 soft were regressed to corresponding dose. RESULTS: The regression equations of AUC and c max to dose about CAV were Y= 2.0895 X+ 0.4438 (r= 0.9915 ) and Y= 0.9397 X+ 0.1796 (r= 0.9922 ), respectively. The regression equations of AUC and c max to dose about AMX were Y= 4.8795 X+ 2.4794 (r= 0.9988 ) and Y= 1.7276 X+ 1.4832 (r= 0.9935 ), respectively. CONCLUSION: There is good linear relationship between pharmacokinetic parameters and doses about CAV and AMX.

Aim The metabolic character of neferine(Nef) in rat liver microsomes was studied in vitro to identify which isoforms of cytochrome P450 were responsible for Nef metabolism in rats.Methods ① Wistar rats were untreated or treated with various inducers including dexamethasone(DEX,50 mg?kg~(-1),ig?4 d),phenobarbital(PB,75 mg?kg~(-1),ip?3 d) and ?-naphthoflavone(?-NF,80 mg?kg~(-1),ip?3 d).Liver microsomes were obtained from these rats and incubated with Nef in the presence of reduced form of nicotinamide adenine dinucleotide phosphate.A HPLC-UV method was developed to determine Nef and its metabolites.② The enzyme kinetics of the metabolism of Nef was investigated in rat liver microsomes.③ Troleandomycin,a CYP3A selective inhibitor,was used to study its inhibitory effect on the metabolism of Nef in vitro.Results ① The metabolism of Nef in rat liver microsomes showed the characteristic of enzymekinetics.② The correlation between peak area of a metabolite and original concentration of Nef in rat liver microsomes solution was significant(r=0.993).③ The disappearing rate of Nef in the incubation solutions of the rats liver microsomes,which treated with DEX or PB,were markedly quicker than that of control group(P0.05).The average disappearing rates of Nef in rat liver microsomes after incubation with different inducers were as follows: DEX,80.6%?9.5%;PB,61.5%?6.7%;?-NF,20.7%?1.5%;Control,19.9%?1.6%.④ Troleandomycin could significantly inhibit the metabolism of Nef in rat liver microsomes.Conclusion Our results suggest that both CYP3A and CYP2B are involved in Nef metabolism in rats liver microsomes,and CYP3A probably play a major role.

Aim To study the pharmacokinetics and bioequivalence of nimesulide dispersible tablet and its normal tablet. Methods 20 healthy volunteers were treated with a single oral dose of domestic nimesulide dispersible tablet or normal tablet (control) in a randomized crossover study and the plasma drug concentration was determined by HPLC. Results The plasma concentration time curve was fitted to the one compartment model. The pharmacokinetic parameters obtained were: c max ( 3.91 ? 0.74) ?g ?ml -1 , t (1/2)? ( 3.40 ? 0.78) h , t max ( 3.15 ? 0.67) h , AUC 0～24 ( 31.92 ? 6.36) ?g ?ml?h -1 , there was no significant difference between the active and control groups. The relative bioavailability obtained was ( 96.43 ? 8.41 ) %. Conclusion The pharmacokinetic profile for the 2 tablets was similar so it may be concluded that they are bioequivalent.

Cytochrome P450 enzymes are composed of many isozymes and involved in the biotransformation of both exogenous and endogenous substances. A growing number of studies have found that the P450 enzymes do not always follow the classical Michaelis-Menten kinetics, but show atypical kinetic behavior, which is also the current research hotspot. In this paper, the category and mechanisms of atypical kinetics of the P450 enzyme were reviewed, providing theoretical basis for the research of enzyme kinetics.

Aim An HPLC method was established for the study on pharmacokinetics and bioequivalence of oxaprozin enteric tablet in healthy volunteers.Methods The oxaprozin in plasma was determined using HPLC method following a single oral dose of 400 mg of oxaprozin given respectively to 18 healthy male volunteers in an open randomized crossover design.The pharmacokinetic parameters and relative bioavailability were calculated to evaluate the bioequivalence of 2 preparations.Results AUC_(0-240 h) of oxaprozin tested tablet and reference tablet were(2852.86?871.00)and (2992.84?854.02)?g?L~(-1)?h,C_(max) were(33.48?11.36)and (32.70?7.30)?g?L~(-1),T_(max) were(12.1?5.7)and(13.8?5.8)h,T_(1[]2ke) were(57.11?8.51)and(60.98?7.97)h,respectively.These main pharmacokinetic parameters obtained showed no statistically significant difference between the 2 products.Conclusion The method is simple and sensitive.Both preparations are bioequivalent.