Adult ; Dimethylformamide ; adverse effects ; Glutathione ; blood ; Humans ; Male ; Methanol ; adverse effects ; Nitric Oxide ; blood ; Occupational Exposure ; Oxygen ; metabolism ; Superoxide Dismutase ; blood ; Surveys and Questionnaires ; Toluene ; adverse effects

AIM: To compare the pharmacokinetics and bioequivalence of between capsule and solution of benzoylmetronidazole. METHODS: Ten chinese healthy male volunteers in a randomized 2-way crossover study were given a single oral dose 960 mg capsule(test) and solution (control) respectively. The serum concentrations of metronidazole, one of the metabolites of benzoylmetronidazole, was measured by high performance liquid chromatography. RESULTS: The serum concentration- time curves appeared one-compartment open model. The results of the capsule and the solution of benzoylmetronidazole showed that Tmax(5.10 ± 1.60) h and (3.12 ± 0.90) h; Cmax(5.32 ± 0.87) mg·L-1 and (6.51 ± 1.25) mg·L-1; T1/2(10.56 ± 1.75) h and (10.16 ± 1.65) h; AUC (106.96 ± 19.62) mg·h-1·L-1 and (113.59 ± 19.84) mg·h·L-1. CONCLUTION: No significant difference appears in the pharmacokinetic parameters between the two formulations except of Tmaxand Cmax(P<0.05). The relative bioavailability of benzoylmetronidazole capsule is (95.07 ± 14.70) %. The AUC between the two formulations is bioequivalent, but the Tmax and Cmax are non-bioequivalent.

ObjectTo study the effect of polydatin (PD) and asymmetric dimethylarginine (ADMA) on the endothelial function in aorta vascular strips of healthy rabbits and the interaction between PD and ADMA. MethodsDose-response curves of phenylephrine (PE) on the aortic strips with or without ADMA and/or PD. E max and Kd from PE were obtained and compared. ResultsNormal aortic strips could not respond to ADMA. Pretreatment with either PD or ADMA had no effect on the contractive response of aortic strips to PE. But PD could significantly weaken the contractive response of aortic strips pretreated with ADMA caused by PE in a dose-dependent manner, increase Kd and decrease E max of PE. ConclusionEither ADMA or PD alone does not influence the normal aortic strip contractive functions, the PE affinity to ?-receptor, and E max. But PD could noncompetitively antagonize the contractive reaction of aortic strips to PE in the presence of ADMA.

Objective To study P300 of the first episode depression and mismatch negativity(MMN) changes after antidepressant treatment. Methods Sixty-four patients with first episode depression were evaluated by HAMD 17, and P300 and MMN tests were performed at the baseline and week 12. The cognitive potentials were compared with those of control group(N=36). Results Compared with the control group, depressive patients had longer latency of P300 and MMN,lower amplitude of P300 and MMN before treatment (P

Objective To summarize the ultrasonic characteristics of urinary calculus in infants who had history of feeding melamine contaminated milk powder.Methods A total of 163 children[aged(19.4?10.9)months] with urolithiasis,who had feeding melamine contaminated milk powder,were retrospectively analyzed using ultrasonography.Twenty children [aged(16.7?9.9)months] with urolit-hiasis,who had no feeding history of melamine contaminated milk powder,were chosen as controls.Ultrasonic characteristics were compared between the 2 groups.Results For melamine calculus cases,sporadic spot or hyperechic mass with different size and shape in the collecting system,partly without acoustic shadow,was found in 65 cases;dense echo and luminous belt with obscured acoustic shadow under a band without echo was found in 48 ureteral calculus cases;irregular strong echo mass or small spot with thick acoustic shadows without side lobe artifact in the dark liquid areas was found in 8 cases with bladder calculus.There was significant difference in morphology of the calculus(P0.05).Conclusions The unique ultrasonic characteristics in infants with melamine calculus had become a very useful tool to diagnose the pediatric urinary melamine calculus.J Appl Clin Pediatr,2009,24(1):67-69

OBJECTIVETo investigate the female sexual dysfunction (FSD) in type 2 diabetes patients, by comparing the sexual function between type 2 diabetic women and non-diabetic women with Female Sexual Function Index (FSFI).

METHODS115 type 2 diabetic women and 107 age-matched non-diabetes women were enrolled with similar backgrounds. Their sexual functions were evaluated with FSFI. Metabolic parameters such as body mass index, blood lipid profile, hemoglobin A1C, plasma glucose were also collected.

RESULTSTotal score of FSFI of the type 2 diabetic women were significantly lower than that of the non-diabetic controls (18.27±8.96 vs. 23.02±5.78, P=0.000). Scores of the FSFI domains (desire, arousal, lubrication, orgasm, satisfaction, pain) of the type 2 diabetic group were also lower than those of the control group. According to the FSD criterion (FSFI<25) available in China, the percentage of FSD in the type 2 diabetic group was significantly higher than that of the control group (79.2%vs. 55.0%, P<0.001). These trends seemed more prominent in pre-menopause subgroups. The logistic regression analysis indicated that age and diabetes were independent risk factors of FSD. Body Mass Index (BMI) also had influence in the diabetes group.

CONCLUSIONFindings from this study showed that there are more FDS in Chinese type 2 diabetic women than in their non-diabetic counterparts, especially in pre-menopause participants.

Adult ; Asian Continental Ancestry Group ; Diabetes Mellitus, Type 2 ; complications ; Female ; Humans ; Middle Aged ; Sexual Dysfunction, Physiological ; etiology

The present study was to evaluate feasibility of a limited sampling strategy (LSS) in the prediction of inhibited hepatic CYP3A activity with systemic clearance of midazolam (MDZ), a hepatic CYP3A activity phenotyping probe. Rats were pretreated with a serial doses of ketoconazole, a selective inhibitor on CYP3A. Blood samples were collected and detected for MDZ at specified time points after intravenous injection of MDZ. Stepwise regression analysis and a Jack-knife validation procedures were performed in one group of rats as training set to establish the most informative LSS model for accurately estimating the clearance of MDZ. Another group of rats with same treatment was used as validation set to estimate the individual clearance based on predictive equations derived from the training set. Bland-Altman plots showed a good agreement between the systemic clearance calculated from DAS (CLobs) and corresponding parameter that was derived from three LSS models (CLest). LSS models derived from two or three sampling time points, including 60, 90 min, 30, 60, 90 min and 30, 60, 120 min, exhibited a good accuracy and acceptable error for estimating the CLobs of MDZ to evaluate hepatic CYP3A activity, especially the 60, 90 min LSS model is most accurate and convenient. The results supported that limited plasma sampling to predict the systemic clearance of MDZ is easier than the usual method for estimating CYP3A phenotyping when the hepatic activity of CYP3A is reduced in the rat. The present study provided theoretical basis and laboratory evidence for LSS to clinically evaluate metabolizing function of liver and
Animals ; Area Under Curve ; Aryl Hydrocarbon Hydroxylases ; antagonists & inhibitors ; genetics ; metabolism ; Cytochrome P-450 CYP3A ; genetics ; metabolism ; Cytochrome P-450 CYP3A Inhibitors ; Dose-Response Relationship, Drug ; Enzyme Inhibitors ; pharmacology ; Injections, Intravenous ; Ketoconazole ; administration & dosage ; pharmacology ; Male ; Metabolic Clearance Rate ; Midazolam ; blood ; pharmacokinetics ; Phenotype ; Random Allocation ; Rats ; Rats, Wistar

AIMTo explore the effects of noninvasive limb ischemic preconditioning on the anti-stress ability in mice.

METHODSMice were divided into: normal group, control group, preconditioning group and drug group. Hypoxia tolerance test, swimming with weight loading, cold tolerance test and thermostable test were performed, and tolerance time in all the stringent state were observed. SOD activity of serum in hypoxia tolerance test and lactic acid of serum in swimming with weight loading test were determined.

RESULTSThe time of hypoxia tolerance in preconditioning group was markedly increased, and SOD activity of preconditioning group mice was significantly higher than those of control group, while they were both shorter than drug group. The average time of swimming in preconditioning group was markedly increased and the level of increasing the swimming time of preconditioning was the same as caffeine. Preconditioning could increase the survival time on high temperature markedly, and there was no significantly difference in the level of increasing the survival time between preconditioning group and chlorpromazine group. Preconditioning could increase the time of cold tolerance markedly compared with normal group.

CONCLUSIONNoninvasive limb ischemic preconditioning can improve the ability of anti-hypoxia, anti-fatigue, thermoresistance and cold-resistance in mice.

Adaptation, Physiological ; physiology ; Animals ; Extremities ; blood supply ; Fatigue ; prevention & control ; Female ; Hypoxia ; prevention & control ; Ischemic Preconditioning ; methods ; Male ; Mice ; Stress, Physiological ; physiology

The present study was to estimate pharmacokinetic parameters of metformin hydrochloride in 20 Chinese healthy volunteers with a limited sampling strategy (LSS), which will provide scientific data for bioequivalence and clinical application. A single dose of metformin was administrated to 20 healthy volunteers. The concentration of metformin in whole blood was determined by validated high performance liquid chromatography (HPLC) method. Multi-linear regression analysis was performed to establish a model to estimate AUC(0-24 h) and Cmax of metformin by LSS method. The LSS models were validated by the Jackknife method. The result indicated: the linearity relationship between AUC(0-24 h) or Cmax and single concentration point was poor. Several models for metformin AUC(0-24 h) or Cmax, estimation were better (r2 > 0.9, P < 0.05). Validation tests indicated that most informative sampling points (C2, C6 for AUC(0-24 h), C1.5, C2 for Cmax) provided accurate estimations of these parameters. So, a multi-linear regression model for estimation pharmacokinetic parameters of metformin by using LSS method is feasible.
Adult ; Area Under Curve ; Chromatography, High Pressure Liquid ; methods ; Humans ; Hypoglycemic Agents ; administration & dosage ; pharmacokinetics ; Linear Models ; Male ; Metformin ; administration & dosage ; pharmacokinetics ; Sample Size ; Therapeutic Equivalency ; Young Adult

OBJECTIVETo investigate the effects of the decoction of Rhizoma Dioscorea septemlobae (RD) on the bone metabolism in ovariectomized rats.

METHODThirty female, 3-month-old Wistar rats without pregnancy and deliver were randomly divided into 6 groups: sham (sham-operation), ovariectomy (OVX), OVX + diethylstilbestrol, OVX + high dose RD (4 g x kg(-1) x d(-1)), OVX + middle dose RD (2 g x kg(-1) x d(-1)) and OVX + low dose RD (1 g x kg(-1) x d(-1)) (n = 5 in every group). After 12-week period of continuous treatment, the urinary samples and blood samples were collected for the determination of serum estrodiol (E2), calcium (Ca), phosphorus (P), bone glaprotein (BGP), alkaline phosphatase (ALP), urinary calcium/creatinine (Ca/Cr), phosphorus/ creatinine (P/Cr) and deoxypyridioline/creatinine (DPD/Cr). The uteri were removed and weighed. The bone mineral density (BMD) and the biomechanical parameters of the femur of the rats in every group were determined, respectively.

RESULTThe coefficient of uteri in every dose group of OVX + RD was significantly higher than that in the OVX group (P < 0.01). The concentration of serum ALP, BGP and urinary DPD/Cr, Ca/Cr in the OVX group was significantly higher than that in the sham group (P < 0.05), respectively, However, that in the every dose of OVX + RD was lower than that in the OVX group, respectively. There was no significan difference in the concentration of serum Ca, P and urinary P/Cr in every group, respectively. The bone mineral density (BMD) in the OVX group was (0.032 +/- 0.007) g x cm(-2) and was significantly lower than that in the sham group (P < 0.01). However, the value in the group of every dose OVX + RD was significantly higher than that in the OVX group (P < 0.05, P < 0.01), respectively. The maximum loading, deflection and the maximum strain of the femur in the OVX group were (125.78 +/- 15.48) N, (1.87 +/- 0.22) mm, (9.34 +/- 1.10) % and were significantly lower than those in the sham group (P < 0.05, P < 0.01), respectively. The maximum loading and maximum stress were increased in different extent in the every dose group of OVX + RD, respectively.

CONCLUSIONThe decoction of RD can inhibit bone absorption, decline bone turnover and improve the loss of bone in ovariectomized rats.

Alkaline Phosphatase ; blood ; Animals ; Bone Density ; drug effects ; Bone Remodeling ; drug effects ; Bone Resorption ; blood ; physiopathology ; urine ; Calcium ; urine ; Creatinine ; urine ; Dioscorea ; chemistry ; Drugs, Chinese Herbal ; isolation & purification ; pharmacology ; Estradiol ; blood ; Female ; Femur ; drug effects ; metabolism ; physiopathology ; Osteocalcin ; blood ; Osteoporosis ; blood ; physiopathology ; urine ; Ovariectomy ; Plants, Medicinal ; chemistry ; Random Allocation ; Rats ; Rats, Wistar ; Weight-Bearing