Objective:To develop an HPLC-MS/MS method for the determination of rosuvastatin in plasma and study the relative bioavailability and bioequivalence of the capsules and tablets in Chinese healthy volunteers. Methods: A single oral dose (20 mg of the test or reference preparation) was given to 24 male healthy volunteers in a randomized crossover study. The plasma concentration of rosuvastatin was determined by HPLC-MS/MS. The pharmacokinetic parameters were calculated and the bioavailability and bioequiva-lence of the two preparations were evaluated by DAS 3. 0 software. Results:After a single dose, the pharmacokinetic parameters of ro-suvastatin capsules and tablets were as follows:Tmax was (3. 56 ± 1. 68) h and (3. 63 ± 1. 56) h, Cmax was (21. 17 ± 13. 74) ng· ml-1 and (26.33 ±23.22) ng·ml-1, t1/2 was (10.68 ±5.50) h and (9.04 ±6.00) h, AUC0-t was (219.31 ±146.09) ng·h· ml-1 and (252. 43 ± 194. 96) ng·h·ml-1 , AUC0-∞ was (225. 32 ± 146. 76) ng·h·ml-1 and (257. 24 ± 194. 61) ng·h·ml-1 , respectively. The 90% confidential interval of AUC0-t, AUC0-∞ and Cmax was 81. 1%-106% , 81. 8%-105. 4% and 77. 9%-104. 5%, respectively. The mean relative bioavailability of the test preparation(the capsules) to the reference preparation(the tablets) was (100. 7 ± 54. 1)%. Conclusion:The test and reference preparations are bioequivalent.

OBJECTIVE:To evaluate the bioequivalence of two preparations of gemfibrozil.METHODS:A single oral dose of gemfibrozil enteric capsule(test preparation)and capsule(reference preparation)was given to20volunteers in an open ran?domized crossover way to study the pharmacokinetics and relative bioavailability.The plasma gemfibrozil concentrations were determined by HPLC method.RESULTS:The pharmacokinetic parameters of test and reference preparations were as follows:T max ,(2.4?0.6)h and(2.3?0.7)h;C max ,(21.8?7.3)?g/ml and(23.7?5.9)?g/ml;T 1/2 ,(2.0?0.4)h and(2.0?0.5)h;AUC 0～12 ,(68.1?13.7)(?g?h)/ml and(68.9?17.4)(?g?h)/ml;AUC 0～∞ (69.7?13.9)(?g?h)/ml and(70.6?17.8)(?g?h)/ml respectively.The relative bioavailability of test preparation was(100.8?15.0)%.The result of statistical analysis on above parameters showed that there was no significant difference between two preparations.CONCLUSION:The two prepa?rations were bioequivalent.

OBJECTIVE:To study the pharmacokinetics and relative bioavailability of compound rifampicin tablets MET_HODS:Plasma levels of rifampicin(RFP),isoniazid(INH)and pyrazinamid(PZA) at different time were determined by HPLC methods,then we drew the time-concentration curves and got the pharmacokinetic parameters and relative bioavailability of test-tablets based on the curves RESULTS:The main pharmacokinetic parameters of RFP,INH and PZA in test-tablets were:Tmax,(1 69?0 60)h,(0 94?0 57)h and(2 36?1 10)h;Cmax,(9 86?2 09)?g/ml,(5 36?1 77)?g/ml and (16 20?4 85)?g/ml;T1/2,(3 43?0 72)h,(2 98?0 75)h and(9 26?1 58)h;AUC0～t,(59 34?13 17)?g/(ml?h),(21 87?14 29)?g/(ml?h) and(212 97?71 52)?g/(ml?h) respectively The main pharmacokinetic parameters of RFP,INH and PZA in control tablets were Tmax,(1 83?0 66)h,(0 86?0 38)h and (2 08?0 97)h;Cmax,(9 98?1 63)?g/ml,(5 60?2 01)?g/ml and (17 79?4 57)?g/ml;T1/2,(3 97?1 58)h,(3 15?0 88)h and (9 36?1 85)h;AUC0～t,(62 46?14 02)?g?h/ml,(21 39?14 53)?g/(ml?h) and (227 09?70 91)?g/(ml?h) respectively The relative bioavailability of test-tablets were (98 47?15 00)%,(103 76?15 80)% and (94 38?12 07)% CONCLUSION:The results of two one-sided tests and rank sum test showed that two formulae were statistically bioequivalent

OBJECTIVE:A HPLC method has been developed to determine the concentration of isoniazid in plasma.METH_ODS:The Eclipse XDB-C18 column was used as fix phase and acetonitrile-0.05mol/L ammonium dihydrogen phosphate as mo_bile phase,detection wavelength was 280nm.The plasma sample was injected directly for determination after being deproteinized with 10% trichloroacetic acid and reacted with cinnamaldehyde and abstracted with ether.RESULTS:Good linear relationship was shown from 0.10 to 12.0?g/ml and the averge recovery of isoniazid was 95%～105%.CONCLUSION:The method is rapid,sensitive and is rarely interfered so it can be used in study of pharmacokinetics of isoniazid.

Objective To investigate the effect of sodium arsenite by Wnt signaling pathway on proliferation and apoptosis of oral squamous cell carcinoma.Methods Cell proliferation was detected after 1.25,2.5,5,10,20μmol/L sodium arsenite treatment human oral squamous cell carcinoma cell line Tca8113 for 24,48,72 hours by CCK8 experiment.0 and 14μmol/L sodium arsenite was used to treatment Tca8113 cells with 48h,cell apoptosis were detected by flow cytometry,Cleaved Caspase3,β-catenin,Cyclin D1 protein expression were detected by Western blot.Tca8113 cells were divided into control group,sodium arsenite group,activating agent+sodium arsenite group,all treated for 48hour,cell proliferation,apoptosis and Cleaved Caspase3,β-catenin,Cyclin D1 protein expression were detected by CCK8 assay,flow cytometry and Western blot.Results Tca8113 cell proliferation was inhibited significantly with the increase of treatment time and sodium arsenite concentration,and has a time and concentration dependent manner(P<0.05 or P<0.01).10μmol/L sodium arsenite as a follow-up study according to the IC50.Cell inhibition rate,apoptosis rate and Cleaved Caspase3 protein expression in 10μmol/L group were significantly higher than that of 0 mol/L group,the expression of β-catenin,Cyclin D1 protein was significantly lower than that of 0 mol/L group(P<0.01).Apoptosis rate,cell inhibition rate and Cleaved Caspase 3 protein expression in sodium arsenite group and activating agent+sodium arsenite group were significantly higher than control group,the expression of β-catenin and Cyclin D1 protein were significantly lower than control group(P<0.01).Apoptosis rate,cell inhibition rate and Cleaved Caspase 3 protein expression in activating agent + sodium arsenite group were significantly lower than that of sodium arsenite group,the expression of β-catenin and Cyclin D1 protein were significantly higher than that of sodium arsenite group(P<0.01).Conclusion Sodium arsenite can inhibit the proliferation of oral squamous cell carcinoma and promote apoptosis,and the mechanism was related to regulation of Wnt signaling pathway.

Objective To evaluate the incidence and severity of pulmonary embolism (PE) in patients with different leg deep vein thrombosis (DVT) by computed tomography pulmonary angiography (CTPA).Methods A total of 145 cases who had been confirmed DVT and undergone CTPA were retrospectively analyzed.The DVTs were divided into left side DVT,right side DVT,and bilateral lower DVT groups.The incidence of PE was compared among different groups.CT obstruction index (CTI) was used to estimate the severity of pulmonary artery obstruction.DVT/PEs with CTI were compared among different groups.Results The incidence of PE of the bilateral lower DVT group was 71.4％,which was higher than that in left side DVT group (39.2％).However,no significant difference was found between bilateral lower DVT group and right side DVT group (52.9％) (P ＞ 0.05).The CTI of the bilateral lower DVT (30.20±14.20)％ was higher than that of the left side DVT (19.26 ± 14.02)％ and the right side DVT (18.56 ±11.79) ％ (P ＜ 0.05).Conclusions The bilateral lower DVT was more likely complicated with PE than the left side DVT,the severity of pulmonary artery obstruction of the bilateral lower DVT with PE patient was higher than that of single side DVT with PE patient.

[Abstract ] Objective Bone marrow mesenchymal stem cells(BMSCs) can be induced to the differentiation into vascular smooth muscle cells in many induction conditions.We sought to explore the possibility of the differentiation of mesenchymal stem cells into vascular smooth muscle cells by continuous cell culture in vitro. Methods Rat BMSCs were isolated from the bilateral tibial and femoral bones by the method of whole bone marrow adherence, followed by ex vivo expansion.BMSCs were identified by flow cytometry and three-lineage differentiation.After continuous five days'cell culture of BMSCs, the specific surface antigens of VSMCs were detec-ted by immunofluorescence, western blot and real-time PCR. Results BMSCs expressed CD29、90, in contrast, they did not express CD45、34、49d.After induction of osteogenesis, adipogenesis and chondrogenesis, alizarin red、oil red and alcian blue staining pro-duced a strong reaction in cells.The expressions ofα-SMA、Calponin1、SM-MHC and SM22 in the cells of experimental group were no-tably increased, which indicated that BMSCs were differentiating towards VSMCs. Conclusion In the absence of exogenous stimula-tion, BMSCs can be successfully induced to differentiate into VSMCs by continuous cell culture.

OBJECTIVE:To explore the role of clinical pharmacists in cancer pain management. METHODS:The cases were presented to investigate the content and method of clinical pharmacists participating in cancer pain management. RESULTS:The clinical pharmacists could provide professional analgesic recommendations and participated in the formulation of individual analge-sic plan. By carrying out pharmaceutical care and patient education,clinical pharmacists could find potential medication risk,cor-rected medication errors and improved patient compliance. By carrying out patient family members training,clinical pharmacists could help to strengthen patient support system and improve cancer pain management effectiveness. CONCLUSIONS:Clinical phar-macists participating in cancer pain management can promote rational use of analgesics,guarantee the safety of drug use,and im-prove cancer pain management.

Thirteen novel oleanolic acid (OA) derivatives were designed and synthesized with modification at positions of C-3, C-12 and C-28 of OA. Their structures were confirmed by MS, 1H NMR and elemental analysis. Their in vitro cytotoxicities against various cancer cell lines (SGC7901, MCF-7 and A549) were evaluated by MTT assay. The results indicated that the tested derivatives were found to have stronger cell growth inhibitory activity than OA. Among them, compounds II2 and II3 showed more potent cytotoxicity on MCF-7 and A549 tumor cells than gefitinib (positive control). They are worthy to be studied further.
Antineoplastic Agents, Phytogenic ; chemical synthesis ; pharmacology ; Cell Line, Tumor ; drug effects ; Cell Proliferation ; Drug Design ; Humans ; Oleanolic Acid ; chemical synthesis ; pharmacology