OBJECTIVE： To study the pharmacokinetics and relative bioavalability of omeprazole capsules in humans.METHODS： 18 male healthy volunteers orally took domestic omeprazole capsules and losec capsulles(used as control)40mg respectively.Blood concentrations of drugs were determined by HPLC.RESULTS： Times to reach the peak levels of omeprazole and losec were （2.10± 0.64） h and （1.88± 0.70） h， the peak plasma concentrations were （895.64± 553.07） ng/ml and （974.67± 554.93） ng/ml and the areas under the drug concentration curves were （1 971.88± 1 220.98 ） ng/（h· ml） and （2 057.60± 1 306.32） ng/（h· ml） respectively.CONCLUSION： The two capsules have the same bioequivalence.

Aim To determine the effects of Qiliqian-gxin injected into lateral ventricle on Cardiac function, angiotensin Ⅱ( Ang Ⅱ) , angiotensin converting en-zyme(ACE), angiotensin type 1 receptor(AT1R) and the sympathetic nervous system in the hypothalamic pa-raventricular nucleus of rats with chronic heart failure. Methods Rat model of heart failure was prepared by acute myocardial infarction that was induced by ligation of the left anterior descending coronary artery. Four weeks after heart failure, Qiliqiangxin and Losartan were continuously administered via a syringe pump in-jector connected to lateral ventricle. After four weeks, echocardiogram was used to evaluate the cardiac func-tion and HE was used to observe myocardial tissue morphology, and enzyme linked immunosorbent assay was used to measure plasma norepinephrine( NE) , ser-um NT-proBNP and Ang Ⅱ in the paraventricular nu-cleus. The expression of ACE and AT1 R at mRNA and protein levels in the paraventricular nucleus was deter-mined by Real-time PCR and Western blot, and the RSNA was measured by PowerLab in anesthetized rats. Results Compared with the sham control, the cardiac function was significantly lower while the AngII, ACE, AT1 R expression in the paraventricular nucleus and RSNA were significantly increased in rats with heart failure. Compared with heart failure control, Qiliqian-gxin and Losartan decreased the RSNA and the AngII, ACE, AT1 R expression in the paraventricular nucleus. Conclusion Giving traditional Chinese medicine to the lateral ventricles can decrease the activation of the RAS system, reduce the renal sympathetic nerve activi-ty and improve cardiac function.

Objective:To prepare capsaicin liposomes and study the feasibility by in vitro percutaneous penetration test. Meth-ods:Capsaicin liposomes were prepared by a film-ultrasonic method. The best formula was screened by orthogonal test based on single factor studies with the entrapment efficiency as the index. The improved Franz diffusion cells were used to study the transdermal pene-tration of capsaicin suspensions, capsaicin liposomes and capsaicin ointments, and the cumulative penetration amount through the isola-ted rat skin was compared. Results:The optimal formula of capsaicin liposomes were as follows:the ratio of capsaicin to lipids was 1∶5;the amount of Tween-80 was 100 mg;the amount of vitamin E was 50 mg;10 ml dichloromethane was used as the solvent. The op-timal pH value of the external phase was 6. 5 with the volume of 10 ml. The ultrasonic time was 8 min. The order of 12-hour cumulative penetration amount was capsaicin liposomes>capsaicin-PBS suspensions>capsaicin ointments. Capsaicin liposomes had the highest 12-hour cumulative penetration amount and showed obvious sustained-release property. Conclusion:Capsaicin liposomes have high en-trapment efficiency, good percutaneous penetration and sustained-release property, and the preparation technology is simple.

Objective:To explore the clinical and electrophysiological characteristics of flail arm syndrome (FAS).Methods:Clinical and electrophysiological data were collected on 13 FAS patients and 31 persons with upper limb onset amyotropic lateral sclerosis (UL-ALS), including the amplitude of compound muscle action potential (CMAP) related to median nerve, ulnar nerve, and axillary nerve motor conduction. A split-hand index (SI) was calculated by dividing the CMAP amplitude of abductor pollicis brevis by that of the abductor digiti minimi. Clinical features, the CMAP amplitudes and SIs were compared between the FAS and UL-ALS patients.Results:Compared with UL-ALS patients, the age at onset among the FAS patients was older (averaging 60.9 years). The development to the second stage was longer (24±6 months). The upper limb reflexes of 15% of the FAS patients had disappeared and those of 77% were weakened, while the lower limb reflexes of 54% of the FAS patients were active and 38% were weakened, significantly different from the UL-ALS patients. However, there were no significant differences in the CMAP amplitudes of the median and ulnar nerves, nor in SI between the FAS and UL-ALS patients. The SIs of the FAS patients with upper motor neuron signs were significantly lower than those of FAS patients without such signs. Among the FAS patients, the average CMAP amplitude of the ulnar nerve was the highest, followed by those of the median and axillary nerves. Among the UL-ALS patients, however, the average CMAP amplitude of the ulnar nerve was not significantly different from that of the axillary nerve.Conclusions:FAS patients with upper motor neuron signs are more likely to have slip hand. The CMAP amplitude of their axillary nerve tends to be lower than that of their median and ulnar nerves. FAS seems to be a special type of ALS.

Aim To observe the effect of“Ying-nutrient and Wei-defense unblocking collaterals prescription”on the carotid sympathetic nerve in early atherosclero-sis. Methods The rabbits were randomly divided into 6 groups:Control group, high-fat group, Complex mod-el group, GSTL-H group, GSTL-L group and ATO group. The control group was fed with common food-stuffs, High-fat group with high-fat diet to build early atherosclerosis model, and all the other groups with high-fat diet combined with carotid artery cannula to build early atherosclerosis carotid artery injury rabbit model. All groups were given corresponding medicines intragastrically once a day for 4 weeks. The GSTL-H and GSTL-L group was given Guishaotongluo ultrafine powder 0. 6 g·kg-1·d-1, 0. 3 g·kg-1·d-1, and the ATO group was given suspension of atorvastain so-lution 2. 5 mg · kg-1 · d-1 . Biochemical method was used to detect blood lipid change. HE staining was ap-plied to observe the pathological morphology of intima-media, The content of NE in the carotid arterial was detected by ELISA. The immunohistochemical staining was used to detect the protein expression of NGF, TH around the carotid arterial. The expression of NGF, TH in the carotid artery adventitia was detected by Western blot. Results Compared with normal group, the levels of TC,TG and LDL-C in high-fat group and complex model group were significantly increased( P<0. 01). The degree of the intimal hyperplasia,the con-tent of NE and sympathetic density ( NGF, TH protein expression and distribution ) of the cartoid artery in complex model group were heavier compared with those in high-fat group; the lipid levels, degree of the inti-mal hyperplasia and sympathetic density ( NGF, TH protein expression and distribution ) in the GSTL-H, GSTL-L group were milder in varying degrees compa-ring with those in the complex model group(P<0. 05, P<0. 01 ) . Conclusion “Ying-nutrient and Wei-de-fense unblocking collaterals prescription” can reduce rabbit carotid atherosclerosis, and the mechanism may be related to regulating the sympathetic nerve of arterial wall.

Objective: To observe the effect of Tongxinluo (TXL) on homocysteine-induced rat’s cardiac micro vascular endothelial cell (RCMECs) injury and to study the oxidative stress mechanism. Methods: Primary RCMECs were cultured with tissue explants process, cell morphology was observed by inverted microscope and the cell was identiifed by CD31 immunolfuorescence method. RCMEC injury model was established by Homocysteine (Hcy) induction and the cells were divided into 5 groups: Control group, with normal cells, Hcy group, the cells were treated by Hcy at 10 mmol/L, Low-dose TXL group, Hcy treated cells were cultured with TXL at 100 mg/L, Middle-dose TXL (200 mg/L) group and high-dose TXL (400 mg/L) group. Cell survival rates were detected, supernatant levels of superoxide dismutase (SOD) activity and malondialdehyde (MDA) content were examined, intracellular protein expressions of reactive oxygen species (ROS) and endothelial nitric oxide synthase (eNOS) were detected and mRNA expression of endothelin-1 (ET-1) was measured in different groups respectively. Results: Compared with Control group, Hcy group showed decreased cell survival rate (74.61 ± 2.88)% vs (100.00 ± 2.07)%, increased supernatant level of MDA (4.10 ± 0.18) nmol/ml vs (1.92 ± 0.10) nmol/ml, reduced SOD activity (7.55 ± 0.71) U/ml vs (20.77 ± 0.68) U/ml, elevated ROS level(38.17 ± 10.28) % vs (19.83 ± 2.97) %, up-regulated mRNA expression of ET-1 and down-regulated protein expression of eNOS. Compared with Hcy group, the above indexes were improved in each TXL group at different levels. Conclusion: TXL could decrease Hcy induced RCMECs injury, such protection was conducted by reducing the oxidative stress mechanism in cells.

Objective To explore the impact of intermittent androgen deprivation therapy on prostate volume and lower urinary tract symptoms (LUTS) in patients with prostate cancer combined with prostatic hyperplasia (BPH),and to evaluate the clinical effect of intermittent androgen deprivation therapy as compared with conventional drug in patients with BPH.Methods Patients with prostate cancer (n=57) and BPH (n=83) were respectively treated with intermittent androgen deprivation therapy and finasteride combined with alpha-receptor antagonist.Prostate volume,international prostate symptom score (IPSS),quality of life index (QOL) and maximum urinary flow rate (Qmax) in patients were observed before and 1,3,6 and 12 months after treatment.Results The improvements in prostate volume,IPSS,QOL and Qmax were higher in prostate cancer patients treated with intermittent androgen deprivation therapy than in BPH patients treated with finasteride combined with alpha-receptor antagonist (P ＜ 0.05).Conclusions Intermittent androgen deprivation therapy can significantly reduce prostate volume and improve LUTS in patients with prostate cancer,and has a better clinical effect than finasteride combined with alpha-receptor antagonist treatment.

[ ABSTRACT] AIM:To investigate the transient outward potassium channel protein expression in paraventricular nucleus (PVN) and its contribution to renal sympathetic nerve activity (RSNA) in rats with chronic heart failure (CHF). METHODS:A rat model of CHF was prepared by acute myocardial infarction that was induced by ligation of the left ante -rior descending coronary artery .Four weeks after heart failure , echocardiogram was applied to identify the CHF model and plasma norepinephrine (NE), serum NH2-terminal pro-brain natriuretic peptide (NT-proBNP) were detected by ELISA. The expression of ransient outward potassium channel proteins Kv 4.2 and Kv4.3 at mRNA and protein levels was deter-mined by real-time PCR and Western blot .The mean arterial pressure ( MAP) , heart rate ( HR) and RSNA were measured in anesthetized rats with PVN microinjection of potassium channel blockers 4-AP.RESULTS:In CHF group , the rat car-diac function and Kv4.2 and Kv4.3 expression in PVN were obviously lower while plasma NE and serum NT-proBNP were obviously higher than those in sham group .Microinjection of 4-AP into PVN induced an increase in MAP , HR and RSNA in both sham and CHF rats , while the CHF rats exhibited smaller responses to 4-AP than sham-operated rats .CONCLU-SION:Downregulation of Kv4.2 and Kv4.3 expression in the PVN may be a potential mechanism for sympathoexciation in the rats with chronic heart failure .

Objective:To investigate the effects of ursolic acid (UA) on the proliferation and differentiation of osteoclasts (OC), and to explore its role in orthodontic force-induced root resorption and its relationship with OC.Methods:The mononuclear / macrophage cells RAW264.7 were induced to the OC.Tacrolimus acid phosphatase (TRAP) staining and bone resorption lacunae observation were used to identify the induction.CCK-8 method was used to select the appropriate concentration of UA for RAW264.7 cell-free biotoxicity and to observe its effect on the proliferation and differentiation of RAW264.7.In experimental groups, UA with gradient concentrations (1.0,2.5,5.0,10.0,20.0and 40.0 μmol·L-1)were added.UA was not added in control group.Results:The TRAP staining and bone resorption lacunae observation showed that after the RAW264.7 cells were induced for 5 d, the TRAP staining positive cells were found;the resorption lacunae were rounded,and oval, etc,the bottom wall was coarser,and the boundary was clear,which indicated that the RAW264.7 cells were successfully differentiated into the osteoclasts.The CCK-8 detection results showed that high concentration of UA (> 10.0 μmol·L-1) significantly inhibited the proliferation of OC;the appropriate concentration of UA (5.0 μmol·L-1) was in the biological safety concentration range and could inhibit the OC proliferation;low concentration of UA (<2.5 μmol·L-1) had no effect.Conclusion:RANKL can induce the differentiation and maturation of RAW264.7 cells.UA is correlated with the proliferation and differentiation of OC;UA has inhibitory effect on OC at the appropriate concentration (5.0 μmol·L-1) in a time-dependent manner.

Aim To explore the effect of pharmacolog-ical activation of serotonin 5-HT2C receptor (5-HT2C R) on naloxone-precipitated withdrawal in morphine-de-pendent mice. Method EthoVision Noldus video tracking system was used to record the effect of 5-HT2C R agonist WAY on locomotor activities and behavioral performances in mice.Results Selective 5-HT2C R ag-onist WAY (0.5,0.75 or 1 .0 mg·kg -1 ,i.p.)a-lone did not alter the locomotor activities as determined by distance traveled and velocity (all P values >0.05).Chronic morphine treatment induced depend-ence in mice as demonstrated by increases in distance traveled,velocity and jumping behavior.WAY (0.5, 0.75 or 1 .0 mg·kg -1 ,i.p.)and clonidine (0.2 mg ·kg -1 ,i.p.)significantly ameliorated naloxone-pre-cipitated withdrawal symptoms,including burrowing, jumping,body grooming,rearing,“wet dog”shakes, head shakes,face grooming,penile grooming,scratch (all P values <0.05).Conclusion Pharmacological activation of 5-HT2C R ameliorates naloxone-precipitated withdrawal symptoms in morphine-dependent mice.5-HT2C R may be a novel target to develop therapeutic ap-proach against morphine physical dependence,craving and relapsing.