Our experimental studies show that the IC50 on she action potential of isolated frpg sciatic nerve blocked by pH7.4 and 4.8 tetracaine solution are 0.34mg/ml and 0.67mg/ml (p

Objective To investigate the effect of recombinant human keratinocyte growth factor variant(K102) on mechanical corneal injury in rabbits.Methods Mechanical corneal injury was made in 108 rabbits surgically.K102 eye drop was given respectively at dose of 0.5,0.25,0.125 mg/ml,taking Beifushu eye drops and Dexamethasone sodium phosphate eye drops as the positive control,and K102 eye drop solvent as the blank control;4 times per day.Corneal haze was determined with slit lamp microscope and the histopathological changes were observed under light and electron microscope.Results Three months after operation,the corneal haze was less severe and the average number of corneal cells in shallow 50 ?m corneal basement was less than that in Beifushu group and blank group after 0.5 mg/ml K102 treatment.The results of light and electron microscopy showed the epithelial hypertrophy,disorders of cells and collagen arrangement after 0.5 mg/ml K102 treatment were much lighter than that in Beifushu group and blank group.Conclusion Local application of K102 eye drops reduces the number of stromal keratocyte,then effectively inhibits corneal haze at early stage after mechanical corneal injury in rabbits.

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 explore the anti-inflammatory effect of Musk eye drops on acute ceratitis.METHODS:The model of acute ceratitis resulting from surgical injury was established in rabbits and which were randomly assigned to Musk eye drops groups(0.3%,0.15%,and 0.05%),0.5% Cortisone acetete eye drops group and 0.9% Normal Saline group(control).The corneal epithelium growth at 24,48h,and 72h was observed by fluorescein(2%)staining,levels of protein,Ca2+,IL-1? in the aqueous humor were determined,corneas were weighted and corneas tissues were sampled for histopathologic examination.The anti-inflammatory effect of Musk eye drops on acute ceratitis resulting from surgical injury was discussed.RESULTS:Corneal bedewing was mitigated,transmigration of neutrophilic leukocytes were inhibited,levels of protein and IL-1? in the aqueous humor were decreased,level of Ca2+ in the aqueous humor was altered and the corneal epithelium growth was promoted in Musk eye drops groups(0.3%,0.15%,and 0.05%).CONCLUSION:Musk eye drops had remarkable anti-inflammatory effect on acute ceratistis.

OBJECTIVE: To investigate the effect of recombined human keratinocyte growth factor variant (K102) on corneal alkali burn in rabbit. METHODS: 60 New Zealand rabbits were randomized to 5 groups. Corneal alkali burn models were made and in the left eyes of the rabbits with 1 mol?L-1 NaOH solution. Then the trial groups (groups A, B and C) were treated with 0.5, 0.25, 0.125 mg?mL-1 K102 eye drops, respectively; group D (positive control group) with bFGF eye drops, and group E (negative control group) with solvent of K102 eye drops. The rate of corneal reepithelialization and the area of neovascularization (CNV) were observed under microscope. RESULTS: Within 24 h, the corneal epithelium growth rate in the trial groups (A, B and C) were 1.52, 1.57 and 1.46 mm2?h-1, respectively, which were significantly different as compared with negative control group (0.98 mm2?h-1) (P

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 plerosis effect of sodium magnesium fructose diphosphate (FDPM) on hypoxia/reoxygenation (H/R) injury of myocardial cells and the possible mechanism. METHODS: The myocardial cells which had been primary cultured for 4 days were used to establish H/R injury model before being assigned to five groups: H/R, H/R+FDPM (4.8, 2.4, 1.2 mg?mL-1). Then set up normal control with normal cells. The activities of lactate dehydrogenase(LDH), creatine phosphokinase (CPK) and the intracellular level of free calcium ([Ca2+]i) were detected after being treated with corresponding drugs, and the ultrastructures of myocardial cells were observed under transmission electron microscope. RESULTS: As compared with H/R group, FDPM groups significantly decreased the activities of LDH and CPK and the level of [Ca2+]i (P

OBJECTIVE:To explore the protective effect of the extracts from Radix et Rhizoma Rhei and Alisma orientalis against acute kidney injury induced by diethylene glycol (DEG) and its action mechanism. METHODS: The acute kidney injury model of mice was induced by intragastric administration of DEG. Then the model mice were administered intragastrically with the extracts of Radix et Rhizoma Rhei and Alisma orientalis. Serum levels of creatinine(Cr) and blood urea nitrogen (BUN), the activities of superoxide dismutase (SOD) and glutathione peroxidase(GSH-PX) and the content of malonaldehyde(MDA) were determined. RESULTS: After administration of DEG, the mice presents with obvious toxic reactions including the increase of the ratio of kidney to body weight, the increase of serum levels of BUN and Cr, the decrease of the activities of SOD and GSH-PX in kidney tissue, the increase of the content of MDA. However, after treatment with the extracts of Radix et Rhizoma Rhei and Alisma orientalis, the toxic symptoms in mice were attenuated markedly, the ratio of kidney to body weight decreased, serum levels of BUN and Cr decreased significantly, the activities of SOD and GSH-PX in renal tissues increased and the content of MDA decreased. CONCLUSION: The remarkable protective effect of the extracts from Radix et Rhizoma Rhei and Alisma orientalis against DEG-induced acute kidney injury in mice might be related to its actions of improving the activity of antioxidase of kidney while inhibiting lipid peroxidation.