OBJECTIVE:To study the pharmacokinetics of tramadol hydrochloride paracetamol tablets in healthy volunteers.METHODS:10 healthy volunteers were assigned to receive oral single dose of tramadol hydrochloride paracetamol tablets.Plasma concentrations of tramadol hydrochloride and paracetamol were measured by HPLC and the pharmacokinetic parameters were computed by 3p97 software.RESULTS:The concentration-time curves of tramadol hydrochloride and paracetamol all fitted one compartment open model.The pharmacokinetic parameters of tramadol hydrochloride and paracetamol were as follows:t1/2Ka were(0.23?0.16)h and(0.64?0.60)h,t1/2ke were(2.12?0.78)h and(5.48?2.90)h,tmax were(0.90?0.43)h and(1.88?1.12)h,Cmax were(9.37?2.56)?g?mL-1 and(115.27?98.88)ng?mL-1,CL/F(s) were(24.52?7.12)L?h-1 and(0.15?0.08)L?h-1,AUC0～t were(30.38?7.47)?g?h?mL-1 and(598.36?232.14)ng?h?mL-1,AUC0～∞ were(33.02?9.15)?g?h?mL-1 and(800.12?420.92)ng?h?mL-1,MRT0～t were(3.75?1.41)h and(5.46?1.64)h,MRT0～∞ were(5.24?2.92)h and(9.86?6.00)h,respectively.CONCLUSION:This study provided a basis for clinical application of tramadol hydrochloride paracetamol tablets.

OBJECTIVE:To study the relative bioavailability and pharmacokinetics of salbutamol sulfate orally disinte?grating tablets.METHODS:A single dose of8mg salbutamol sulfate orally disintegrating tablets or commercial salbutamol tablets was administered in a randomized crossover design in18volunteers and the plasma concentrations of salbutamol were determined by HPLC.The pharmacokinetic parameters were calculated with3p97pharmacokinetic program and the bioequiv?alency was evaluated.RESULTS:The concentration-time curve of two preparations fitted to two-compartment model.The peak plasma levels(C max )of salbutamol sulfate orally disintegrating tablet and commercial salbutamol sulfate tablet were(17.65?6.48)ng/ml and(16.60?6.21)ng/ml,respectively.The peak time(T max )were(1.92?1.18)h and(2.03?1.17)h and AUC 0～24 were(127.23?32.41)ng/(h?ml)and(131.42?37.73)ng/(h?ml),respectively.The relative bioavailability of salbu_ tamol sulfate orally disintegrating tablet was(99.32?15.58)%.CONCLUSION:The results of two one-side tests suggests that salbutamol sulfate orally disintegrating tablet is bioequivalent to the commercial salbutamol tablet.

OBJECTIVE: To study distribution and pharmacokinetics of gatifloxacin in ocular tissues of rabbit after ocular instillation.METHODS: The drug concentrations in ocular tissues were determined by HPLC after topical ocular instillation in rabbits;the pharmacokinetics parameters were figured out by 3p97 process. RESULTS: Results showed that the peak concentration of gatifloxacin in lacrimal fluid, cornea, aqueous humor, iris-ciliary body, lens and vitreous body 0.125h～1.0h after topical instillation were (1 115.75?151.04)?g/ml,(17.90?1.39)?g/g,(2.26?0.18)?g/ml,(9.12?0.33)?g/g,(1.07?0.13)?g/g and (0.77?0.04)?g/g respectively;t1/2? in various tissues were(2.14?0.33),(2.82?0.54),(3.33?0.43),(3.88?1.21),(3.89?1.43) and (3.14?0.43)h respectively;AUC(0→t) in various tissues were(541.77?69.73)(?g?h)/ml,51.31?3.04)(?g?h)/g,(6.55?0.45)(?g?h)/ml,(51.99?25.66)(?g?h)/g,(4.19?0.41)(?g?h)/g and (3.25?0.13)(?g?h)/g respectively.CONCLUSION:Gatifloxacin has a good permeability and high concentration in various intraocular tissues of rabbit after ocular instillation.

OBJECTIVE:To study pharmacokinetic parameters of melatonin tablet in beagle dogs.METHODS:A single oral dose of3mg melatonin tablet was given to6beagle dogs,drug concentrations in plasma were determined by HPLC method,the pharmacokinetic parameters were calculated by3P97pharmacokinetic program.RESULTS:The concentration-time curves of melatonin fitted two compartment model in the beagle dogs.The t 1/2Ka 、t 1/2Ke 、t max 、C max 、CL and AUC (0～T) were(0.16?0.10)h、(1.21?0.52)h、(0.50?0.18)h、(11.27?3.77)ng/ml、(0.13?0.04)L/h and(25.23?7.71)(ng?h)/ml re-spectively.CONCLUSION:It is rapid to absorb melatonin and initiate sleep in beagle dogs,but it's hold-time is short.

Objective Study the effect of chlorogenie acids(CHA)on insulin resistance in obese rats induced by high‐fat diet . Methods We induced the obese rat model by feeding high‐fat diet ,obese rat model were divided into 4 groups:model group ,piogli‐tazone group(4 .5 mg/kg) ,CHA large dose group and group ,and finally determinated the levels of glucose tolerance ,serum insulin , serum lipid profiles and others .Results CHA showed a higher anti‐obesity activity with lower rate of increase of obese rats′body weights ,reversingglucose intolerance induced by high‐fat diet ,ameliorating the hyperinsulinemia ,decreaseing the levels of TG and TC ,and increase liver glycogen and muscle glycogen level compared with other group which treated with high‐fat diet .And in‐creased HOMA‐ISI ,decreased HOMA‐IR .Conclusion CHA can ameliorate the symptoms of insulin resistance in obese rats ,which mechanism may be related with CHA can stimulate glucose uptake and utilization by peripheral tissues ,and decrease the the serum levels of FFA ,decrease oxygen stress ,prevent and cure the injury induced by lipid peroxidation .

Objective To observe the effect of oxymatrine on the Absorption of carbohydrate and fat and the activity of peroxisome proliferator activated receptor ? and ?.Methods 64 masculine SD rats were randomly divided into three groups,20 sugar tolerance test,20 triacylglycero Absorption test and 24 oxymatrine effecting on triacylglycero and cholesterin test,and observed the effect of oxymatrine on glycosidase activity,blood sugar and activity of peroxisome proliferator activated receptor ? and ?.Results ① The depressant effect of oxymatrine on the activity of glycosidase was strengthened by the increased dosage.② Oxymatrine could suppress the upgraded level of blood sugar after took amylon and cane-sugar,and inhibit the upgraded level of triacylglycerol after feed by olive oil and hypso-cholesterol,but did not suppress the upgraded level of blood sugar after took glucose and hardly influence the level of high density lipoprotein cholesterol and low density lipoprotein cholesterol.③ Oxymatrine could obviously activate the activity of peroxisome proliferator activated receptor ? and ?,the activity of peroxisome proliferator activated receptor ? and ? increased gradually by the augment of the oxymatrine,and expressed evident dose-response relation.Conclusions Oxymatrine could not only directly inhibit the Absorption of triacylglycerol and depress the elevated level of postprandial triacylglycerol,but also activate peroxisome proliferator activated receptor ?,moreover possess dose-response relation.

0.05) in the results of Vd of mannitol and glycerol for both rabbits and human studies

This paper dicusses the significance of drug clinical trials,and summarises the experiences in policy making,personnel trainning,supervising and management in drug clinical trials at the First People's Hospital of Changzhou,which may provide reference for drug clinical trials in China.

AIM: To investigate correlation between the expression of survivin and caspase-3 proteins in juvenile laryngeal papilloma. METHODS: The expression of survivin and caspase-3 proteins were detected with immunohistochemial method in 43 cases of juvenile laryngeal papilloma, 25 vocal nodules and 25 normal laryngeal mucosa. RESULTS: The positive rates of survivin protein in juvenile laryngeal papilloma were 57.14% and higher than that in voeal nodules (P<0.01)and the normal laryngeal moeusa (P<0.01). And the Caspase-3 protein positive rate was 26.19% in juvenile laryngeal papilloma and lower than that in voeal nodules and the normal laryngeal mucosa (P<0.01).There was a significant negative correlation between the expression of survivin and caspase-3 in juvenile laryngeal papilloma. CONCLUSION: The abnormal expression of survivin and caspase-3 may play important role in the pathogenesis of juvenile laryngeal papilloma.

Objective: To explore the protective effect of Shenmai lyophilized preparation (SMP, 参麦冻干剂) on acute myocardial infarction (AMI) in cats. Methods: AMI cat model was induced by ligation of the left coronary artery for 4 hours. Cats were randomly divided into five groups: AMI group (4 ml/kg of normal saline ), large dose SMP group (1.76 g/kg), small dose SMP group (0.88 g/kg), Shenmai injection (参麦注射液) group (0.88 g/kg) and nitroglycerine group (0.44 mg/kg). Drugs were given 5 minutes after the left coronary artery ligation. Mean arterial pressure (MAP) and ventricle cardiac arrhythmia were monitored by multichannel biological signal analytical system. MultiCD*2lead ?ST on chest was recorded by cardiofax after myocardial ischemia for 4 hours, the area of AMI was measured by dyes with triphenyl tetrazolium chloride (TTC). Changes of creatine kinase (CK) and lactate dehydrogenase (LDH) in serum were assayed by colorimetric assay. Results: SMP at the dosage of 0.88 and 1.76 g/kg increased MAP, decreased ?ST and incidence of ventricle cardiac arrhythmia in cats with AMI, shrank the area of AMI and decreased the LDH content and CK activity in serum, respectively compared to the AMI group, the differences being significant in the aboveCD*2mentioned parameters (P