This study aimed to investigate the transport characteristics of aripiprazole.A human intestinal epithelial cell model Caco-2 cell in vitro cultured had been applied to study the transport of aripiprazole.The effects of time,concentration of donor solutions,pH,temperature and P-glycoprotein inhibitor on the transport of aripiprazole were investigated.The determination of aripiprazole was performed by HPLC.It is concluded that aripiprazole is transported through the intestinal mucosa via a passive diffusion mechanism primarily,coex- isting with a carrier-mediated transport.The transport of aripiprazole is positively correlated to transport time, concentrations.The P-glycoprotein inhibitor cyclosporine A significantly enhanced the transport amount of aripiprazole.

Objective To determine the optimized self micro-emulsifying drug delivery system (SMEDDS) formulation of probucol. Methods According to the indexes of mean particle size, zeta-potential, solubility of probucol in blank SMEDDS and the dissolution percentage in 5 minutes of the preparations, the optimized formulation was determined by the central composite design-response surface methodology. Results When the correspondent percentage of olive oil in oil phase (W/W) was 0.33, the percentage of oil phase in formulation (W/W) was 0.5, and the ratio of surfactant to co-surfactant (W/W) was 2.0, respectively. The mean particle size, zeta-potential, solubility of probucol and dissolution percentage in 5 minutes of micro-emulsion was 92.7 nm, -17.38 mV, 65.17 mg/mL and 63.46%, respectively. Conclusions The optimized formulation of the probucol SMEDDS was obtained quickly and conveniently by the central composite design-response surface methodology. The method had a reliable predictability.

OBJECTIVETo investigate the protect effects of sodium ferulate (SF) on the daunormbicin(DNR-induced cardiotoxicity in juvenile rats.

METHODSForty male juvenile SD rats were randomly divided into control group (Control), daunorubicin group (DNR), sodium ferudate treatment group (DNR + SF), sodium ferudate group (SF) (n = 10) . Juvenile rats were intraperitoneally treated with DNR (2.5 mg/kg every week for a cumulative dose of 10 mg/kg) preparation immature myocardial injury model in presence with SF (60 mg/kg) oral treat- ment for 25 days. The left ventricular pressure and its response to isoproterenol were measured using left ventricular catheter. Rat myocardium myocardial pathology specimens and ultrastructure changes were also observed. The expression of cardiac Troponin I (cTNI) was detected by Western blot and RT-PCR. Results: SF treatment could inhibit the decreasing of heart rates induced by DNR damage (P < 0.05); it could increase the left ventrivular end diastolic pressure(LVEDP), heart rate, the maximal left ventrivular systolic speed(LVP + dp/dtmax) and the maximal left ventrivular diastolic speed (LVP-dp/dtmax) responding to isoproterenol stimulation(P < 0.01); SF also could improve the myocardial ultrastructure injuries and inhibit the decreasing of cTNI expression caused by DNR damages (P < 0.05).

CONCLUSIONSF treatment could alleviate the decreasing of cardiac reservation induced by DNR damages in juvenile rats, which might be related to its reversing the effects on the cardiac systolic and diastolic function injuries and its inhibiting effects on the decreasing of cTNI expression caused by DNR. The mechanism of SF preventing daunorubicin-induced cardiotoxicity in juvenile rats is relevant to inhabited cardiac Troponin I expression.

Animals ; Blood Pressure ; Cardiotoxicity ; drug therapy ; Coumaric Acids ; pharmacology ; Daunorubicin ; toxicity ; Heart ; physiopathology ; Heart Rate ; Isoproterenol ; Male ; Myocardium ; pathology ; Protective Agents ; pharmacology ; Rats ; Rats, Sprague-Dawley ; Troponin I ; metabolism

Animals ; Animals, Newborn ; Chronic Disease ; Daunorubicin ; adverse effects ; Disease Models, Animal ; Heart Failure ; chemically induced ; Rats ; Rats, Sprague-Dawley

In order to study the susceptibility of murine vaginal mucosa to Candida albicans under different conditions, vaginal lavage fluid and vaginal tissue of mice were observed and compared between murine models with normal immune system (estrogen-treated mice) and immunosuppressed murine model, and between primary infection model of vaginal candidiasis and secondary infection one. The average level of colony forming unit (CFU) from the immuosuppressed group was higher than that from estrogen-treated group at each time point and the peak time was delayed. The differences between the two groups were statistically significant (P < 0.05) from the fourth day after inoculation. A significant difference existed in the average level of CFU between the control group and the estrogen-treated group (P < 0.05), and between the control group and the immuosuppressed group (P < 0.01). It was concluded that the vaginal mucosa from the immunosuppressed mice is more susceptible to Candida albicans and no difference is found in susceptibility between mice with primary infection and secondary infection.
Candida albicans/drug effects ; Candidiasis, Vulvovaginal/*etiology ; Candidiasis, Vulvovaginal/*immunology ; Disease Susceptibility ; Estrogens/*pharmacology ; Immunocompromised Host ; Mice, Inbred ICR ; Random Allocation ; Vagina/microbiology

Objective To explore the correlation between lower urinary tract symptoms (LUTS) with prostate volume and peak flow rate in aging staff men with benign prostatic hyperplasia (BPH). Methods A total of 180 elderly patients were randomly enrolled. They were diagnosed with BPH by rectal touch and transected ultrasound from April 2008 to December 2008. The international prostate symptom score (IPSS), prostate volume (PV) as well as peak flow rate (QMAX)were analyzed respectively. Results IPSS were ( 9. 1 ± 0. 7 ) scores, ( 12. 1 ± 0. 7 ) scores and (14.0±1.3) scores in 60-69 years old group, 70-79 years old group and more than 80 years old group. PV were (40. 6±1.9) ml, (42. 4±1.9) ml and (48. 7±2.8) ml in corresponding groups, and PV was elevated along with aging (F= 5. 705, 2. 983, P＜0. 05). QMAX were ( 14.7 ± 0. 6) ml/s,(14.0±0. 5) ml/s and (12.6±0.9) ml/s, and QMAX was decreased along with aging (F=2. 131, P＞0. 05). Along with aggravation of LUTS, PV (ml) increased (39. 2±18. 1 vs. 45.7±16.9 vs. 47. 9± 16. 5) and QMAX (ml/s) decreased ( 15.0 ± 4.8 vs. 13. 5 ± 5.06 vs. 11.5 ± 4. 7, F= 3. 427, 4. 742, P ＜0.05). Conclusions The LUTS of patients with BPH is aggravated with aging, at the same time, the degree of LUTS increases with PV and decreases with QMAX. If get active treatment of drugs if available, they may improve their quality of life.

Animals ; Brain-Derived Neurotrophic Factor ; pharmacology ; Cell Movement ; drug effects ; Cell Proliferation ; drug effects ; Cells, Cultured ; Chick Embryo ; Chorioallantoic Membrane ; blood supply ; Endothelial Cells ; cytology ; drug effects ; physiology ; Female ; Humans ; Mice ; Mice, Inbred C57BL ; Neovascularization, Physiologic ; drug effects ; Vascular Endothelial Growth Factor A ; pharmacology

This study aimed to investigate the transport characteristics of aripiprazole. A human intestinal epithelial cell model Caco-2 cell in vitro cultured had been applied to study the transport of aripiprazole. The effects of time, concentration of donor solutions, pH, temperature and P-glycoprotein inhibitor on the transport of aripiprazole were investigated. The determination of aripiprazole was performed by HPLC. It is concluded that aripiprazole is transported through the intestinal mucosa via a passive diffusion mechanism primarily, coexisting with a carrier-mediated transport. The transport of aripiprazole is positively correlated to transport time, pH, and temperature. Papp increased with donor concentrations up to 10 microg x mL(-1), and then decreased for higher concentrations. The P-glycoprotein inhibitor cyclosporine A significantly enhanced the transport amount of aripiprazole.
ATP-Binding Cassette, Sub-Family B, Member 1 ; antagonists & inhibitors ; Antipsychotic Agents ; administration & dosage ; pharmacokinetics ; Aripiprazole ; Biological Transport ; drug effects ; Caco-2 Cells ; Cyclosporine ; pharmacology ; Dose-Response Relationship, Drug ; Humans ; Hydrogen-Ion Concentration ; Piperazines ; administration & dosage ; pharmacokinetics ; Quinolones ; administration & dosage ; pharmacokinetics ; Temperature ; Time Factors

Objective: To test applicability of the Center for Epidemiological Studies Depression Scale (CES-D) in different age groups in urban China, and to develop age norms. Methods: In this cross-sectional study, the CES-D was administrated to 16047 community participants with average age of (37.7±21.3) years (age ranged 11～100) in 21 provinces, who were as the norming sample. Criterion validity was tested in 349 psychiatric patients with average age of (32.0±12.1) years (age ranged 16～81) in 4 cities. A subsample (199 workers, 100 col-lege students, and 30 teachers in Beijing, Dongguan, and Baotou) was drawn from the national sample to provide 8 week interval test-retest reliability. Results: The Cronbach α was 0.90 for the scale, and 0.68～0.86 for its fac-tors. The 8 week interval test-retest correlation was 0.49 for the scale (P <0.01) and 0.39～0.51 for factors (P<0.01) . The result of confirmatory factor analysis supported the original 4-factor structure (RMSEA=0.057, CFI =0.976, GFI=0.948) . Patients scored higher than community sample [(21.72±13.39 ) vs.(13.24±10.33),P <0.01], and depression patients scored the highest [(27.82±14.42), P<0.01] . Age difference was signifi-cant. Age groups over 60-year-old scored higher than all the other age groups under 60-year-old (P<0.01). Con-clusion: The Chinese version of CES-D shows good refiability and validity across all ages in urban population-

Objective To compare the relative efficacy and quality of extraction of human fecal DNA using four methods.Methods Real-time PCR were utilized for analysis both quantification and quality of the fecal targeted bacteria(including gut all eubaeterium,Bacteriodes-PrevoteUa group,Bifidobacterium spp Enterobacteriaceae and Enterococcus spp)by using 16s rRNA gene-targeted genus or group-specific primer sets.Results The negative rat of PCR product from method 3(phenol-chloroform plus bead-beating) was about 40%(4/10)by using universal primers,the PCR inhibition disappeared after fecal DNA purified with column.The total fecal 16s rRNA gene copy numbers(per gram of wet weight of feces)as well as the numbers of Bacteriodes-Prevotella group from method 1(QIAamp~DNA stool mini kit)and 4(QIAamp~ DNA stool mini kit combined with bead-beating)was higher significantly than that from method 2(FastDNA ~Kit,Biol01)and 3(P