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 explore the effect of Xiaoyu anshen capsule on the space learning-memory ability of chronic stress-induced depressed model rats.METHODS:The enrolled rats were divided into 6 groups:blank control group,model group,Fluoxetine group,Xiaoyu anshen capsule groups(high,medium and low dose).Chronic depression rat model was induced by chronic stress and isolated breeding.Water-maze video tracking analysis system was used to detect the capacity of rats' space learning-memory,and the indexes such as the body weight of rats before and after modeling and the consumption of sucrose,etc.were measured.RESUTLS:Compared with the blank control group,the model control group showed significantly decreased space learning-memory capacity,significantly lower in body weight increase and significantly less sucrose solution consumption.Compared with the model control group,the high,medium and low dose Xiaoyu anshen capsule-treated group showed significantly shortened escape latency,the high and medium dose groups showed increased number of times of crossing the hidden platform and body weight increase,and in high dose Xiaoyu anshen capsale group sucrose consumption increased.CONCLUSION:Xiaoyu anshen capsule is a nootropic Chinese herbal medicine for its inhibitory effect on the abnormality in body weight and sucrose solution consumption of chronic stress-induced depressed model rats and their action in enhancing the space learning-memory ability.

AIM: To investigate the therapeutic effect and its mechanisms of musk eye drops on allergic conjunctivitis (AC) in guinea pigs.METHODS: AC was developed by intraperitoneal injection of a mixture containing Ovalbumin (OVA) and Al(OH)3 in guinea pig.Sixty guinea pigs with AC were randomly divided into 6 groups,i.e.,AC model group,three treated groups treated with musk eye drops in high,middle and low dosage,group treated with dexamethasone sodium phosphate eye drops.Together with solvent group as sixth group.After one week of administration,the changes of guinea pigs in symptoms,histamine and OVA-specific IgE concentration of ocular tissues,and morphological features of conjunctiva were observed under light microscopy.RESULTS: Compared with the vehicle group,the conjunctiva symptoms scale,histamine and OVA-specific IgE concentration of ocular tissues and morphological changes scale of conjunctiva of guinea pigs in the model group were fairly good.Compared with the model group,the ocular symptoms of guinea pigs in each of the musk eye drops treated groups showed relieved (P

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 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 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.