Aim The pharmacokinetic parameters and relative bioavailability of capsule A(Maiwei Pharmaceutical Co Ltd, Beijing, China) and capsule B (Xianjing Pharmaceu-tical, Hunan, China) were studied. Methods A single oral dose of 600 mg gemfibrozilof these two kinds of capsules was given to 12 chinese healthy male volunteers in anopen, randomized crossover study. Plasma levels were determined with HPLC-UVmethod. Results The plasma concentration-time curve was fitted to 1-compartmentopen model with a first order and lag time absorption and the major pharmacokineticparameters of capsules A and B were shown respectively as following: C max(32. 69?5. 67 )and (29. 41?2. 60) mg?L-1; Tmax (1. 01?0. 14) and (1. 13?0. 37) h, t1/2ka(0. 46 ? 0. 18) and (0. 62 ? 0. 20) h; C max (1. 11 ? 0. 32) and (1. 32 ? 0. 26) h; MRT(2. 14 ? 0.27) and (2. 37 ? 0.26) h; AUC (91.7 ? 13.2) and (82.2 ? 7. 38) mg?h? L-1. There were no significantly differences between the pharmacokinetic parame-ters of capsule A and B. The relative bioavailability of the capsule A was (110 ? 9) % ascompared to the capsule B. Conclusion The two kinds of capsules have the equivalentbiological effects.

Objective To investigate the effect of ultrasound-guided transversus abdominis plane (TAP)block on the efficacy of postoperative analgesia in parturients undergoing selective cesar-ean delivery.Methods Eighty ASA Ⅰ or Ⅱ parturients recruited for selective cesarean delivery under combined spinal-epidural anesthesia were randomly divided into two groups(n =40 each):TAP group (group T)and control group(group C).After cesarean delivery,bilateral of ultrasound-guided TAP block were performed,20 ml of 0.5% ropivacaine was injected in each side in group T,while TAP was not done in group C.Both groups received patient-controlled intravenous analgesia (PCIA)after cesarean delivery.The resting and exercise visual analogue scale (VAS)scores,Ramsay sedation score and the Bruggrmann comfort scale(BCS)score were evaluated at 2,4,6,8 and 24 h after operation. The consumption of sufentanil within 24 h after operation,the number of successfully delivered doses (D1 )and the number of attempts (D2 )within 24 hr after operation were recorded.D1/D2 was calculated.The parturients satisfaction and the adverse reactions were also recorded.Each parturient was assessed postoperatively by a blinded investigator.Results The consumption of sufentanil within 24 hr after operation,the resting and exercise VAS scores at 2,4,6 hr after surgery were significant-ly lower,while the BCS score,the value of Dl/D2 and the degree of satisfaction were higher in group T than those in group C (P <0.05).There were no adverse reactions in both groups.Conclusion Ultra-sound-guided TAP block reduces the postoperative sufentanil consumption,enhances the efficacy of post-cesarean analgesia of the parturients.Comfort and satisfaction are achieved in the parturients of the group T.

Objective To explore the application of bumetanide to inhibition of tumor cell proliferation.Methods In different cell lines, the expression of natrium,kalium, chloride cotransporter 1 ( NKCC1) was detected by Western blotting while the proliferation of different tumor cells was examined by CCK-8 kit.Results The target protein NKCC1 expression in lung cancer cell line ( A549 ) and colorectal cancer cell line ( HCT116 ) was significantly higher than that in chronic myelogenous leukemia cell line (K562), esophageal cancer cell line (Eca109), cervical carcinoma cell line (HeLa), T lymphocytic leukemia cell line (Jurkat) and breast cancer cell line (MCF7).IC50 Values of bumetanide were significantly lower in A549 and HCT116 than in K562, Eca109,HeLa,Jurkat and MCF7.Furthermore, the inhibiory rate and the target protein expression level were positively correlated.Conclusion Bumetanide can inhibit tumor cell proliferation and NKCC1 can serve as a potential target of anticancer drugs.

Phospholipase A_2 (PLA_2) inhibitor quinacrine was used to explore protective effect on multiple organ dysfunction (MOD) caused by intestinal ischemia-reperfusion (I/R) in rats. Gut I/R caused the increase of gut PLA_2 activity and induced endotoxemia and bacteriemia. Pretreatment with intravenous quinacrine 10mg?kg~(-1) attenuated bacteria and endotoxin translocation,markedly lowered the levels of thromboxane A_2 and prostacyclin I_2 in blood,and provided protection from the development of vital organs dysfunction. As a result,the survival rate in pretreatment group increased by 25%. The results demonstrate that gut I/R promotes gut barrier failure,then contributes to the development of MOD by allowing bacteria or endotoxin reaching the circulation. PLA_2 and PLA_2-dependent lipid mediators play an important role in the development of gut I/R injury and MOD. Intravenous quinacrine has protection against MOD resulting from gut I/R.

Objective: We investigated experimentally the changes of intestinal immunity following shock and resuscitation after trauma. Method:The experimental model was made in rats, which underwent laparotomy, then bleeding and reinfusing through the right fetmoral artery. Result: The concentration of IgA following shock and resuscitation were significantly higher than that before shock.. The concentration of IgA 24 h following resuscitation was the lowest, and was significantly lower than that at the end of shock.. The endotoxin in portal vein following shock and resuscitation were higher than that before shock.. The endotoxin level 24 h following resuscitation was the highest, and markedly higher than that at the end of shock. Conclusion: The traumatic shock and resuscitation are capable of causing intestinal immunosuppression and endotoxemia.

Objective:To determine the pharmacokinetics of continuously infused midazolam in patients during intensive care. Method: The study involved six critically ill patients who required sedation to facilitate controlled ventilatory support. The infusion rate of midazolam was adjusted individually to achieve an appropriate level of sedation. Blood samples were taken during and after the continuous infusion of midazolam to measure plasma concentration of midazolain with high performance liquid chromatography,and pharmacokinetic parameters were calculated. Result:The mean value of elimination half-life was 5.09 h(range: 3.19-7.30h), and the volume of distribution was 64.45L(range: 10.41-135.25L). The clearance was 7.29L/h, Conclusion:Clinical pharmacokinetics of midazolam in critically ill patients is highly variable. The increased volume of distribution in the patients is the major determinant for the slower elimination of midazolam.

Objective: To investigate the effects of pentoxifylline (PTX) on oxygen free radicals induced myocardial injury. Method: An in vivo myocardial impairment model was developed in SD rat with exogenous oxygen free radicals. The changes cardiac performance and serum malonylaldehyde (MDA), lactic acid, cretine phosphokinase (CK) levels were tested before and at different interval after I. V. administration of oxygen free redieal. Result: Myocardial performance after oxygen free radicals administration was significantly depressed compared to the baseline values (P

0.05 ),the O- 2 production increased significantly (P

Objective To evaluate the efficacy of PTX on the global cerebral ischemia reperfusion injuryMethods The global cerebral ischemia of gerbils was induced by clamping bilateral carotid arteries for 30 min , then declamping with the reperfusion lasting 90 min At the beginning of ischemia , PTX 25mg?kg -1 or 50mg?kg -1 was administered intravenously by mini infusion pump In another group , PTX 25mg?kg -1 was infused at the beginning of reperfusion In sham operated and control groups the same volume of 0 9% NaCl were infused 0 2% Even's blue 1ml?100g -1 was injected intraperitoneally At the end of experiment , The gerbils were decapitated to be preserved at -70℃ for measurement of water contents of whole hemispheres , cerebral superoxide dimutase (SOD) activity, malonyldialdehyde (MDA) content and Even's blue content Results As compared with those in control group, at the beginning of ischemia or reperfusion ,the administration with PTX 25mg?kg -1 significantly reduced the cerebral water content (P

Objective To investigate the effects of propofol on learning and amnesia in the old miceMethods The normal Kunming mice were trained in a one-trial, step-through, light-dark passive avoidance paradigm Propofol (50 or 100 mg/kg) was administered intraperitoneally 15 min before training ,and propofol (100 or 200 mg/kg) separately 30 min and 6 h in the immediate post-training period The latency of escaping into a darkened chamber and the wrong number of entering darkened chamber were recorded Animals were tested for recall at 24th h post-training time The activity of acetyltransferase was determined with radiommunoassay in the brain 3h after administrationResults All control animals were liable to learn the task as judged by their increased latencies to enter the darkened chamber at 24th h post-training time After administration with propofol 50 mg/kg or 100 mg/kg, the latencies were reduced (246 and 208,repectively), compared with control (P