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: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 investigate the protective effects of NIF,NHH,TNHH on focal cerebral ischemic injury induced by middle cerebral artery occlusion in rats.METHODS:24 SD rats were randomly divided into 4 groups:control group(n=6)received normal saline 0.1ml/kg,group NIF(n=6),group NHH(n=6)and group TNHH(n=6)received NIF,NHH,TNHH 2mg/kg i.v.(NIF,NHH,TNHH were dissolved in normal saline 2mg/kg)respectively just before middle cerebral artery occlusion(MCAO)with 3～0 nylon monofilament suture for 3 days.The neurological behavior was evaluated at 4hr,8hr,24h,48h,72h after operation.The infarct volume was then assessed after TTC staining following the last neurological behavior evaluation.Two specimens were randomly taken in 4 groups and were sent to HE staining.RESULTS:The neurologic defect score(NDS)of group NIF,NHH,TNHH after operation decreased significantly(P

With transdermal absorption speed constant as index, the percutaneous osmosis experiments were carried out by orthodox design method to study the preparation process of EVA membrane.The results indicate that the best preparation process of EVA membrane is:10% EVA 36,dissolved by chloroform without the addition of plasticizer, expanding the membrane at the thickness of 0 5 ?m, dried at 80℃ for 6 hours. The membrane is with good releasing-control activity under the above condition.

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

OBJECTIVE: To determine the content of the related substances in azithromycin tablet by HPLC-electrochemical detector.METHODS: The column was Gamma ARP-1/P.The mobile phase consisted of 0.014 mol?L-1 dipotassium hydrogen phosphate/0.020 mol?L-1 sodium hydroxide(pH was adjusted to 11 by phosphoric acid and sodium hydroxide)-acetonitrile(71∶29) at a flow rate of 0.7 mL?min-1.The column temperature was 40 ℃.The injection volume was 50 ?L.Glass carbon working electrode was set at +900 mV.RESULTS: The linear ranges of erythromycin peroxide,deoxyazithromycin,azithromycin impurity A,and N-demethlation azithromycin were 0.15～1.80 ?g(r=0.999),0.09～1.08 ?g(r=0.999),0.23～2.76 ?g(r=0.998) and 0.30～3.60 ?g(r=0.998),respectively.The average recoveries were 98.9%(RSD=1.1%),94.6%(RSD=5.4%),103.4%(RSD=3.4%) and 96.2%(RSD=4.3%),respectively.The contents of the related substances were all below 0.7%.CONCLUSION: The established method is reproducible,sensitive and reliable,and applicable for the detection of the related substances in azithromycin tablets.

OBJECTIVE:To compare the pharmacokinetics and bioavailability between domestic(test)and imported(reference)citalopram hydrobromide tablets and to evaluate the bioequivalence of the two preparations.METHODS:A single dose of 40 mg test tablet or reference tablet of citalopram hydrobromide was administered by randomized crossover way in 20 healthy male volunteers and the plasma concentrations of the citalopram hydrobromide were determined by HPLC.The pharmacokinetic parameters were calculated with 3p97 pharmacokinetic program and the bioavailability was evaluated.RESULTS:The concentration-time curves of two preparations fitted two compartment mode1.The pharmacokinetic parameters of the test preparation versus the reference preparation were as follows,Cmax:(147.00?86.04)ng?mL-1 vs.(154.13?87.57)ng?mL-1;tmax:(4.55?1.35)h vs(4.75?1.65)h;AUC0～196:(6 590.69 ? 1 866.00)ng?h?mL-1 vs.(7 156.26?2 181.18)ng?h?mL-1;AUC0～∞:(7 767.56?2 193.92)ng?h?mL-1 vs.(8 433.45?2 631.88)ng?h?mL-1.The relative bioavailability of the test citalopram hydrobromide tablet was(92.10?18.68)%.CONCLUSION:The domestic and the reference citalopram hydrobromide tablet are bioequivalent.

OBJECTIVE: To compare the bioequivalence between two kinds of Simvastain Tablets.METHODS: A single dose of 40mg of domestic Simvastain Tablets(test preparation) and imported Simvastain Tablets(reference preparation) was administered by randomized crossover way in 20 healthy volunteers with plasma concentrations of simvastain determined by liquid chromatography mass spectrometry. The pharmacokinetic parameters were calculated with 3p97 pharmacokinetic program and the bioavailability was evaluated.RESULTS: The concentration-time curve of two preparations fitted one compartment model.The pharmacokinetic parameters of the test preparation vs.the reference preparation were as follows: Cmax:(13.23?4.41) ng?mL-1 vs.(12.68?4.43) ng?mL-1;tmax:(1.64?1.20) h vs.(1.54?1.28) h;AUC0～12:(47.48?22.96)vs.(44.49?18.47) ng?h?mL-1;AUC0～∞:(50.87?24.06) ng?h?mL-1 vs.(47.11?19.54) ng?h?mL-1.The relative bioavailability of the test simvastain tablets was(106.72?15.20)%.CONCLUSION: The results suggest that two preparations are bioequivalent.