Objective To evaluate the efficacy and safety of levalbuterol hydrochloride in the treatment of mild - moderate asthma. Methods Randomized double -blind, control clinical study was carried out. One hundred twenty- two mild- moderate asthma patients were randomized to enroll the study. Trial group was treated with oral Ievalbuterol hydrochlo-ride tablets 1.15 nag thrice daily. Control group was treated with oral sal-butamol sulphate tablets 2 mg thrice daily. The therapy window is ( 14 ±2) d. Results Comparison with baseline, the first forced expiratory vol-ume vs predicted( FEV1% ), the first forced expiratory volume (FEV1)and the first forced expiratory volume vs the forced vital capacity (FEV1/FVC) were obviously improved in trial group. There is significantly statis-ties difference (P≤0. 05 ). Control group has no significant variance pre and post treatment. Drug adverse reaction of trial group and control group is 12.5% and 15.3% ,respectively. There is no marked difference between two groups. Conclusion Two groups are equivalent in the treatment of mild to moderate asthma, moreover, lung function has been more improved greatly in trial group compared with control group.

Objective To evaluate the effect of calcium dobesilate cap-sule combining compound dansen dropping pill treating diabetic retinopa-thy and diabetic nephyopathy. Methods Sixty -five patients with dia-betic retinopathy and diabetic nephyopathy were randomlied into two groups, control group ( compound dansen dropping pill po 500 mg, rid, n = 32) ; trial group ( compound dansen dropping pill po 500 mg + calciumdobesilate po 270 mg, tid, n = 33 ) for three months. The change of eye ground,blood rheology, serum creatinine, urea nitrogen,24 hours urine protein were Observe. Results Trial group were obviously mult than control group about eye ground improved, ang aggravated obviously re-dueed. (P<0.01 ). Trial group degrade blood rheology and urine pro-tein, discharge degrade serum creatinine and urea nitrogen, to lessen kid-ney damage, protection kidney were more obviously than control group.Conclusion The effect of treating diabetic retinopathy and diabetic nephyopathy by combining calcium dobesilate pill and compound dansen dropping pill were good than take compound dansen dropping pill alone.

Objective To investigate the pharmacokinetics of fluoroura-cil (5-Fu) sustained release implant (FSRI) administered intrapleural-ly or intraperitoneally in the patients with malignant pleural effusions or ascites. Methods Twelve patients with moderate or large malignant pleural effusions or ascites were enrolled. FSRI was administered intra-pleurally or intraperitoneally at a fixed dosage of 1500 mg. The pleural or peritoneal effusions and plasma samples were obtained before and after administration. Concentrations of 5-Fu were measured by HPLC. Phar-macokinetic parameters were calculated. Results In the pleural(perito-neal) effusions, 5-Fu concentration was significantly higher than that in plasma (P<0.05 ). Drugs released slowly, and the concentrations in the effusions were still more than the effective concentration at the 15th day.Conclusion When administered intrapleurally or intraperitoneally flu-orouracil sustained release implant had a long elimination and high localconcentrations.

Objective To investigate on influence of CYP2D6 genetic polymorphism on pharmacokinetics of tramadol in Chinese volunteers.Methods Adult healthy Chinese volunteers with different CYP2D6 genotypes were categorized into the following four groups: group 1:CYP2D6 * 2W * 10W, group 2:CYP2D6 * 2M * 10W, group 3:CYP2D6 * 2M * 10H, group 4 : CYP2D6 * 2M * 10M. After oral ad-ministration of 100 mg tramadol, plasma and urine samples were col-lected from each subject at different time within 32 h. The plasma and urine concentrations of tramadol and its metabolite O - desmethyltramad-ol (M1) were determined by HPLC with fluorescence detection. Re-suits The main pharmacokinetic parameters of tramadol and M, in group 2 were not significantly different from those in group 1. There are significant difference for the main pharmacokinetic parameters of tram-adol and M1 between group 3 and group 1, group 4 and group 1, group 4 and group 3, respectively (P<0.05 ). Conclusion The present re-sults shown that CYP2D6 * 2 has no influence on the pharmacokinetics of tramadol, but CYP2D6 * 10 reduces CYP2D6 activity which leads to the change of phenotype, and the homozygotes has more significant in-fluence on the pharmacokinetics of tramadol than the heterozygotes in Chinese population.

Objective To explore the pharmacokinetics of single and multiple oral 20 mg escitalopram in healthy Chinese volunteers. Methods A total of 12 subjects participated in the study. Escitalopram 20 mg was given orally once on day 1 and days 8 to 14 in the fast condition. Sequen-tial blood samples were collected over 144 hours on day 1 and 14 and a predose sample was obtained on day 12 to 14. Escitalopram concentrations in plasma were determined by a validated HPLC fluorescence method. The pharmacokinetic parameters were calculated with DAS software. Results Escitalopram disposition on oral administration is characterized by a two-compartment pharmacokinetic model. The mean t1/2 is 41.09 h, Cavis (76.4±26.8) μg·L-1, AUCss is (1832.4±642.4) μg·h ·L-1,AUC0-t, and AUC0-∞are (4765.9±2171.0) and (5385.6±2851.2) μg ·h·L-1, respectively; tmaxis (3.2±1.3) h;t1/2 is (41.1±17.7) h;CLis 5.0 L·h1. The mean accumulation index of AUC ( RAUC) is ( 1.2 ±0.3 ). Conclusion Escitalopram pharmacokinetics in healthy Chinese subjects given 20 mg once daily dosing regimen were characterized by a two-compartment pharmacokinetic model. The state -concentration oc-curre after 7 days of continuously dosing. There is no accumulation after continuously dosing.

Objective To study the pharmacokinetics and bioequiva-lence of risperidone film-coated tablets in healthy volunteers. Meth-ods A single administration of 2 mg risperidone of test and reference formulation was given to 23 healthy male volunteers according to an open, randomized, cross-over design. The concentration of risperi-done and 9-hydrorisperidone were determined by HPLC - MS/MS.The main pharmacokinetics were calculated and bioequivalence of two formulations were evaluated. Results The main pharmacokinetic pa-rameters of test and reference formulation were as follows, rispcridone:AUC0-twere(94.76±82.93 ) and( 103.05 ± 117.71 )ng · h · mL-1,AUC0～1 were ( 96.72 ± 84.52 ) and ( 105.19 ± 119.36 )ng·h·mL-1,Cmax were (15.91±5.63) and(16.21 ± 11.56)ng·mL-1, tmaxwere (1.14±0. 73) and(1.15 ± 0.54)h, t1/2 were (7.32±5.94) and (7.44 ± 6.50 ) h, respectively. The relative bioavailability of risperi-done was ( 106.68 ± 40.21 ) % ; 9 - hydrorisperidone: AUC0～96hwere(268.56±85.20) and(279.64 ± 117.86) ng·h·mL-1, AUC0-∞were (282.74 ± 87.46 ) and (294.28 ± 120.32 ) ng · h · mL-1, Cmax were ( 10.84 ± 4.69 ) and ( 11.11 ± 4.80 ) ng·mL-1, tmaxwere (3.35 ± 2.32) and(4.48 ± 2.76) h, t1/2 were (23.18 ± 3.26) and ( 23.12 ± 4.31 ) h, respec-tively. The relative bioavailability of 9 - hydrorisperidone was( 101.37 ± 27.23 ) %. Conclusion The two formula-tions were bioequivalent.

Objective To evaluate the in vitro activity of cefazolin penta-hydrate and other common used antimicrobial agents against clinical pathogens isolated within last 3 years. Method MIC values were deter-mined by standard twofold agar dilution method. Time kill curves were il-lustrated by colony form unit (cfu) count method. Totally , MICs of 604 isolates within last 3 years from 19 hospitals were tested. Result The results indicated that for Gram - positive aerobic pathogens, cafazolin pentahydrate showed satisfied in vitro activity against methicillin suscepti-ble Staphylococcus aureus ( MSSA), methicillin susceptibel Staphylococcus epidemidis (MSSE), penicillin susceptible Streptococcus pneumonies (PSSP) and Streptococcus spp. β-hemolytic group. MIC90 was ≤ 4 mg · L-1 For Gram- negative bacilli, cefazolin pentahydrate also showed antibacterial activity. MIC values was ≤ 8 mg · L-1 for non- ESBLs Enterobacteriaceae bacteria. Time- kill curves test results indicated that cefazolin pentahydrate typically is of time dependent profile against staph-ylococci, but for E. coli, the bactericidal activity slight increased with drug concentration increased. Conclution Compared with contrast drugs, the activities of cefazolin pentahydrate against G+ bacteria were better than cephalexin, clindamycin, clarithromycin, and silght better than cefotiam, and similar with amoxicillin/clavulanic acid, cefuroxime and levofloxacin. For non - ESBLs Enterobacteriaceae, the activies of cefazolin pentahydrate were better than cephalexin, and similar with amoxicillin/clavulanic acid and cefuroxime.

Objective To investigate the different roles of metabolism of baicalein in rat,especial liver and intestine. Methods The enzyme re-actions by microsome incubations were employed. The content of baica-lein and baicalein- glucuronide were determined by HPLC. The glucu-ronidation rates of baicalein at different time points and at various con-centrations were measured by using 5 UGT microsomes. Results Five different microsomes are important common microsomes for glucuronida-tion of baicalein with the manner of time and concentration-dependences.Furthermore, the results also showed that jejunum microsome is the main microsome for metabolizing baicalein, and the colon microsome would be a weakest microsome for the contribution of baicalein metabolism. Con-clusion Different microsomes are responsible for the metabolism of ba-icalein in different organs/regions of the digestive system. The glucuroni-dation of baicalein in the intestine contributes significantly to that of ba-icalein in the liver.

Objective To observe the pharmacological effect of Mansh-enling granules on chronic renal failure (CRF) induced by daunorubicin in rats. Methods CRF was induced with injecting daunorubicin repeat-edly after uninephrectomy. In addition normal group, the CRF Wistar rats were randomly divided in to 5 groups: model group, control group (Niaoduqing granules 2.3 g·kg-1 ), and large, middle, small dose ( Manshenling granules 2.70、1.35,0. 68 g·kg-1) test groups. The ne-phroprotective effects of Manshenling granules was investigated. Results In large and middle groups, serum creatinine, BUN and urinary protein were significantly decreased than those in model group. Glomerul- cell prolifera-tion and glomerular sclerosis level were slighter than in model group. Con-clusion Manshenling granules can reduce the injury of renal in CRF rats.

Objective To evaluate the necessarity of therapeutic drug monitoring (TDM) of vancomycin in clinical use. Methods Different databases were searched including the Cochrane Library, Pubmed,Medline, Embase, CBM and CNKI for randomized controlled trials a-bout TDM of vancomycin. Three clinical studies were involved into this systematic review, including 332 patients. The Cochrane Collaboration's RevMan 4.2.10 software was used for meta analysis. Results Meta analysis displayed that no significant difference was observed in the du-ration of therapy, the cumulative total dose, and creatinine clearance (CLcr). But two sub -groups were also divided as Cmax> 25 μg·mL-1 group and Cmax<25 μg·mL-1group. Compared to the two sub-groups, the significant differences were observed in duration therapy,cumulative total dose, and C-reactive protein (CRP). Conclusion There were no significant differences between TDM group and the non-TDM group on the efficacy and safety of vancomycin, but in the TDM group, between Cmax> 25 μg·mL-1 group and Cmax < 25 μg·mL-1group, the efficacy and safety were significantly different. The evidence currently availiable showed that TDM of vancomycin was not necessary only if the steady state concentrations of vaneomycin were maintained in-to a appropriate variation scope.