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 effects of recombinant human erythropeietin(rh-EPO)on Bid mRNA and caspase-3 activity in the brain after hypoxic-ischemic brain damage(HIBD)in neonatal rats and the possible mechanism of the neuroprotective effect of rh-EPO.Methods Ninety 7 day old male SD rats weighing 12-18 g were randomly divided into 3 groups(n=30 each):group Ⅰ sham operation(S);group Ⅱ hypoxia-ischemia group(HI)and group Ⅲ rh-EPO.The animals were anesthetized with ether.Left common carotid artery was ligated with 4-0 silk and 3 days later the animals were placed in a 2 L airtisht vessel filled with 8%O2-92%N2 at 2-3 L/min for 2 h in group Ⅱ and Ⅲ.rh-EPO 3 000 IU/kg in 4 ml/kg normal saline(NS)was administered intraperitoneally after induction of hypoxia-ischemia(HI)in group Ⅲ while in group Ⅱ NS 4 ml/kg was given IP instead.Six animals in each group were killed at 6,12,24,48 and 72 h(T1-5)respectively after IP NS or rh-EPO.Their brains were removed for determination of Bid mRNA expression(by RT-PCR)and caspase-3 activity(by colorimetric method).Results The expression of Bid mRNA was up-regulated and caspase-3 activity was significantly increased in the brain at T1-5 in HIBD group(group Ⅱ)as compared with sham operation group.rh-EPO administration significantly reduced the increase in Bid mRNA expression and caspase-3 activity in the brain induced by hypoxia-ischemia.The expression of Bid mRNA was positively correlated with the caspase-3 activity.Conclusion rh-EPO has protective effects on the brain against hypoxia and ischemia by decreasing the expression of Bid mRNA and caspase-3 activity in the brain.

Edema, as one of common clinical diseases, could be treated by taking medicines and adopting external therapies with traditional Chinese medicines (TCM). In recent years, there have been many clinical and basic studies concerning external therapies with TCM on edema Data showed that the external therapies are mostly composed of such purgating drugs as Rhei Radix et Rhizoma, Natrii Sulfas and Pharbitidis Semen, heat-clearing drug such as Phellodendri Chinensis Cortex and resuscitation-inducing drug such as Borneolum Syntheticum. The study showed that ingredients of external therapies did not pass through hilum and hepatic system, and thus avoided the first pass effect of livers. They enabled effective components of drugs to be rapidly absorbed through pores and skins, strengthened the effect against edema, shortened the treatment course, decreased side effects, and were convenient and inexpensive. External therapies with TCM could play unique advantages in inhibiting edema in the future clinical studies.
Animals ; Drugs, Chinese Herbal ; administration & dosage ; Edema ; drug therapy ; Humans

Objective To evaluate the role of the expression of protein kinase Cγ and Cα in spinal dorsal horn in the metabotropic glutamate receptor subtype 5 (mGluR5)'s participation in the development of morphine tolerance in rats. Methods Thirty-two male SD rats in which the intrathecal (IT) catheter was successfully placed were randomly divided into 4 groups (n = 8 each): control group (group C), morphine tolerance group (group M), antisense oligodeoxynucleotide (ODN) plus morphine group (group ANT) and mismatch ODN plus morphine group (group MIS). Rats in group M received 0.9% normal saline (NS) 5 μl twice a day for 8 days, and IT morphine 15 μg was injected simultaneously at 6, 7 and 8 days twice a day. Rats in group ANT and MIS received IT antisense and mismatch ODN 30 nmol (in 0.9% NS 5 μl) twice a day for 8 days respectively and IT morphine 15 μg was injected simultaneously at 6, 7 and 8 days twice a day. Rats in group C received NS instead twice a day for 8 days. Paw-withdrawl threshold (PWT) to thermal and mechanical stimulation was measured at 6, 7 and 8 days after ODN injection (T1-3). The animals were killed on 9th day (T4) and the lumbar segment of the spinal cord was removed for determination of the expression of mGluR5, PKCα and PKCγ mRNA (by RT-PCR), PKCαand PKCγ ( by Western blot). Results PWT to thermal and mechanical stimulation was significantly higher at T1.2in group M and MIS and at T1.3 in group ANT, the expression of mGluR5 mRNA, PKCα and PKCγ was significantly higher at T4 in group M and MIS, and mGluR5 mRNA expression was significantly lower at T4 in group ANT than in group C ( P ＜ 0.05). PWT to thermal and mechanical stimulation was significantly higher at T2.3, while the expression of mGluR5 mRNA, PKCα and PKCγ lower at T4 in group ANT than in group M ( P ＜ 0.05). Conclusion The expression of protein kinase C in spinal dorsal horn plays an important role in the mGluR5's participation in the development of morphine tolerance in rats.

Child ; Hemofiltration ; Humans ; Male ; Paraquat ; poisoning ; Poisoning ; therapy ; Treatment Outcome

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 investigate the serum therapeutic concentration of tramadol during intravenous analgesia for postoperative pain relief. Methods Twenty adult patients ASA Ⅰ-Ⅱ (10 male, 10 female) undergoing elective radical operation for cancer of stomach were treated with intravenous tramadol for postoperative pain relief. Patients addicted to any drug or tolerant to opioid and patients with epilepsy or liver and/or renal dysfunction were excluded. All patients were premedicated with intramuscular phenobarbital 0.1g and atropine 0.5mg. Anesthesia was induced with midazolam 0. 1mg/kg and fentanyl 5 μg/kg and intubation was facilitated with vecuronium 0.16mg/kg. Anesthesia was maintained with continuous intravenous infusion of propofol 4-6 mg@ kg 1 @ h 1, fentanyl 2-3 μg@ kg-1 @ h-1 and vecuronium 0.1mg@ kg-1@ h-1 combined with inhalation of 1% isoflurane. After surgery in ICU when patients felt slight pain (VAS 1-2), intravenous tramadol 1.5mg/kg was given as initial dose. Whenever patients felt slight pain (VAS 1-2) again, a bolus of tramadol 20 mg was given intravenously every 10 min until VAS was 0. The onset time (from the end of iv injection of initial dose of tramadol to VAS 0), the duration of action (from VAS 0 to VAS 1-2) and the time when accumulated dose of tramadol amounted to twice the initial dose were recorded. HR, MAP, respiratory rate (RR) and SpO2 were monitored and recorded before and 10, 20, 30 min after administration of tramadol. Venous blood samples were taken before each additional tramadol administration on demand for determination of serum tramadol concentration by high performance liquid chromatography. Results The mean serum therapeutic level of tramadol during period of analgesia was (370±148)ng/ml(248.6-615.7ng/ml). The mean onset time of the initial dose was (9.2± 2.1 )min. The mean duration of action was (2.3 ± 1.0)h. The time when accumulated dose of tramadol amounted to twice the initial dose was (6.4 ± 2.7)h on average. There were no significant changes in HR,MAP, RR and SpO2 after tramadol. Conclusions It is safe and effective to give intravenous tramadol for postoperative pain relief. Serum therapeutic concentration of tramadol varies greatly from patient to patient,so the dose of tramadol should be individulized.[Key Words] Pain, postoperative; Tramadol; Plasma concentration; Injections, intravenous

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.

Objective To explore the value of left parasternal anterior mediastinaotomy (Chamberlain procedure) in the diagnosis of mediastinal lymph node enlargement with unknown causes and anterior mediastinal space-taking lesions. Methods By using the Chamberlain procedure, biopsy was performed in 32 cases of enlarged mediastinal lymph nodes with unknown causes or mediastinal space-taking lesions, which were found by CT scans. Results All of the 32 cases were pathologically diagnosed, with a diagnostic accuracy of 100%. Three patients with pericardial effusion received concurrent pericardial fenestration and then their symptoms relieved. Four patients underwent concurrent lung biopsy. The operating time was (48?15) min, the blood lose was ( 40.6?23.5) ml, and the postoperative hospital stay (3.6?1.4) days. No deaths or postoperative complications occurred. Conclusions Chamberlain procedure is a safe and valuable method in the diagnosis of mediastinal space-taking lesions with unknown causes or enlargement of the fifth and sixth groups of mediastinal lymph nodes, which routine mediastinoscope cannot reach. Some other simple therapies, such as lung biopsy or pericardial fenestration, can also be employed at the same time.

To study the growth, expansion and differentiation of bone marrow stromal cells (BMSC) of rhesus monkey, the BMSC were isolated from adult rhesus monkeys, cultured and induced with a special medium confected in our lab. Identification was performed with immunochemichemistry method. The results showed that BMSC could proliferate and generate clone when culturing in vitro. These cells grow rapidly and differentiated into neuron like cells and astrocyte like cells. The cell clones proliferated from stem cell could express Nestin antigen and the differentiated cells expressing GFAP or NSE antigen respectively. In this study, we did not observe RA, BFGF and EGF remarkably influencing the induction and differentiation of the BMSC. It is suggested that the BMSC from rhesus monkey have the self renewal and differentiation abilities. They might differentiate into neuron like and astrocyte like cells which express GFAP or NSE. As available easily, the BMSC could be considered as the ideal seed cells of the neural stem cells.