OBJECTIVE:To evaluate the relative bioavailability of2kinds of preparations of cefaclor capsules.METH?ODS:The subjects'blood concentrations were determined by HPLC at different time after administered randomly crossover with single oral dose of cefaclor testing preparation or reference preparation.The actual values of C max and T max were adopted;AUC was calculated by trapezoid planimetry;the bioequiavailability of the2preparations were evaluated by two-sides and one-side t-test.RESULTS:The AUC 0～4 of the testing preparation and reference preparation were respectively(13.44?3.06)(?g?h)/ml and(14.19?3.28)(?g?h)/ml;their respective AUC 0～∞ were(13.80?3.08)(?g?h)/ml and(14.62?3.33)(?g?h)/ml;their respective C max were(11.65?2.39)?g/ml and(12.37?2.41)?g/ml;their respective t max were(0.57?0.24)h and(0.66?0.19)h.The relative bioavailability of testing preparation was(95.62?13.51)%.CON?CLUSION:The2preparations are bioequivalent.

Nrf2,a key transcriptional factor in regulating endog-enous antioxidant signaling pathway,maintains the redox bal-ance by controlling the expression of a battery of antioxidant en-zymes,phase-Ⅱ detoxification enzymes and phase-Ⅲ transport-ers.Furthermore,Nrf2 regulates inflammation.Recent resear-ches have confirmed that Nrf2 provides a vital physiological role in kidney diseases,activation of Nrf2 enhances the antioxidant and anti-inflammatory ability in cellular and tissue levels,thusalleviates renal injury.Here,this article aims to summarize the protective effect of Nrf2 on various models of kidney impairment and explore the potential of Nrf2 as a therapeutic target to pre-vent kidney diseases.

OBJECTIVE:To estabilish a HPLC-MS method for determining enalapril in human plasma METHODS:Alprozalam was added into plasma sample as an internal standard,then supernate of the sample was extracted through solid-phase extration column,washed with methanol and detected by HPLC-MS method:column,ODS C18;mobile phase,methanol-0 01% formic acid(45∶55);flow rate,0 8ml/min;capillary voltage,3 81kV;cone voltage,39 0V The selected ion was determined by EST RESULTS:The calibration curve was linear within the range of 2 5～400ng/ml r=0 9 996,the recovery was 102 2%,RSDs of intra -day and inter-day were 4 0% and 5 4%,respectively CONCLUSION:The method is accurate and sensitive with no endogenous interference It can be applied to studying the pharmacokinetics and bioavailability of enalapril tablets in humans

Objective To investigate the effect of lidocaine on Staphylococcus aureus exotoxin-stimulated peripheral blood mononuclear cells (PBMCs) from patients with atopic dermatitis (AD).Methods Peripheral blood samples were collected from 6 patients with AD,and PBMCs were isolated by a routine method.Then,the PBMCs were stimulated by the Staphylococcus aureus exotoxin toxic shock syndrome toxin-1 (TSST-1) in the absence or presence of lidocaine at varying concentrations.The 3H-TdR incorporation method was performed to detect the proliferation of monocytes,and enzyme-linked immunosorbent assay (ELISA) to quantify the levels of T helper type 1 (Th1) and Th2 cytokines released by PBMCs.Human HaCaT keratinocytes were co-cultured with lidocaine-and TSST-1-stimulated PBMCs from patients with AD for 72 hours,then,Western blot was conducted to examine the expression of filaggrin protein in HaCaT cells.Results TSST-1 (100 μg/L) significantly enhanced the proliferation of PBMCs from patients with AD (stimulation index =75 ± 2.12,P ＜ 0.05),as well as the release of tumor necrosis factor-α (TNF-α),interferon (IFN)-γ,interleukin (IL)-2,IL-12,IL-4,IL-5 and IL-13 by the PBMCs (all P ＜ 0.05).Compared with the blank control group,100 μmol/L lidocaine significantly inhibited the TSST-1-stimulated proliferation of PBMCs from patients with AD (stimulation index =58 ± 3.14,P＜ 0.05),as well as the release of IL-4,IL-5,IL-13,TNF-α and IFN-γ by the stimulated PBMCs (all P ＜ 0.05).Western blot showed that 100 μmol/L lidocaine significantly blocked the down-regulation of filaggrin expression in HaCaT cells (P ＜ 0.01).Conclusion Lidocaine has a significant inhibitory effect on the activation of TSST-1-stimulated PBMCs from patients with AD.

CD40/CD40L is a pair of complementary transmembrane glycoproteins, expressed on immune cells, endothelial cells, smooth muscle cells, platelets and other cells involved in regulation of immunity, inflammation, coagulation and other pathophysiologic states. A large number of researches have demonstrated that, when atherosclerosis occurs, CD40L ligates CD40; subsequently CD40 is activated and stimulates downstream signaling pathways, including nuclear factor-kappaB, with consequent up-regulation of proinflammatory and proatherogenic genes. Thus it plays an important role in the occurrence, development and plaque-rupture of atherosclerosis. CD40/CD40L is a bridge between immunity, inflammation, and a hypercoagulable state, and may be an important target for prevention and treatment of cardiovascular disease.
Animals ; Atherosclerosis ; genetics ; physiopathology ; CD40 Antigens ; genetics ; CD40 Ligand ; genetics ; Humans ; Immunity ; physiology ; Inflammation ; physiopathology ; NF-kappa B ; metabolism ; Polymorphism, Genetic ; Thrombophilia ; physiopathology

Endothelial progenitor cells (EPCs) are a kind of progenitor cells with high potential of proliferation, which exist in the bone marrow, umbilical cord blood, and peripheral blood. Under certain conditions, EPCs can differentiate into mature vascular endothelial cells. Many studies have shown that EPCs could delay the onset and development of atherosclerosis by promoting the repair of the endothelium and neovascularization. EPCs have also been considered to be a biological marker for cardiovascular diseases. Recent investigations demonstrate that EPCs can mediate the effect of some anti-atherosclerosis drugs. This paper reviews the role of EPCs in atherosclerosis and the influence of drugs on EPC function. The feasibility and the problem of using EPCs as a treatment strategy are also discussed.
Atherosclerosis ; drug therapy ; pathology ; Cell Differentiation ; Endothelial Cells ; cytology ; Humans ; Stem Cells ; cytology ; physiology

This paper described a rapid and se nsitive HPLC method to analyze (E)-3, 5,4'-trimethoxystilbene (BTM-0512) in rat plasma and tissues. The analysis used a BDS Hypersil C18 analytical column (250 mm×4.6 mm ID, 5 μm) and acetonitrile / water as the mobile phase. The UV detection wavelength was 319 nm. Proteins were precipitated with acetonitrile and diethylstilbestrol as internal standard. The method was validated according to State Food and Drug Administration of China and ICH of Technical Requirements for Registration of Pharmaceuticals for Human Use Guidelines. The limit of interday precision values (%RSD) were in the range of 2.6% -5.1% and 2.4% -4.8%, respectively.Mean accuracy and absolute recoveries of BTM-0512 ranged from 95.3% - 100. 1% and 95.9% -100.9% for plasma and tissues, respectively. This method can be quite useful for BTM-0512 pharmacokinetic and tissue distribution studies, for purpose which multiple plasma and tissue samples can be analyzed quickly with high reproducibility.

Objective To clarify the necessity of therapeutic drug monitoring (TDM ) of voriconazole ,and give relevant clinical tips ,by comparing the plasma concentration of different clinical specialties before and after adjustment of dose .Methods This is a retrospective study of voriconazole TDM data .It involves 435 cases voriconazole plasma trough concentration meas-urement results of 154 inpatients to make a preliminary assessment .Results 4 .3% plasma concentration were higher than 5 .5 μg/ml ,26 .5% plasma concentration were less than 1 .0 μg/ml in renal transplantation department ;while 52 .3% plasma concentration were higher than 5 .5 μg/ml ,no less than 1 .0 μg/ml in infectious disease department .Conclusions Therapeutic drug monitoring is necessary for rational use of voriconazole .The majority of plasma concentrations in renal transplantation pa-tients were <1 .0 μg/ml ,lower than recommended treatment concentration range ;while most infectious disease patients have> 5 .5 μg/ml ,higher than recommended treatment concentration range .Clinical pharmacists can be more closely involved in the clinical use of voriconazole based on the results of the therapeutic drug monitoring .

Recently, accumulating evidence suggests that high bilirubin level is involved in the pathophysiology of schizophrenia. High bilirubin level during early childhood may increase the risk of being suffered from schizophrenia after adulthood, and schizophrenia patients with high bilirubin level have aggravated psychiatric symptoms. As compared with other psychiatric patients and general population, schizophrenia patients usually have relatively higher bilirubin level; high bilirubin level is associated with acute psychotic states, positive symptoms, and poor prognosis in patients with schizophrenia. This article reviews the relation between bilirubin and schizophrenia and its potential pathophysiological mechanism in order to provide a new direction for the study of schizophrenia pathogenesis and auxiliary diagnosis.

Polymyxin B, which is a last-line antibiotic for extensively drug-resistant Gram-negative bacterial infections, became available in China in Dec. 2017. As dose adjustments are based solely on clinical experience of risk toxicity, treatment failure, and emergence of resistance, there is an urgent clinical need to perform therapeutic drug monitoring (TDM) to optimize the use of polymyxin B. It is thus necessary to standardize operating procedures to ensure the accuracy of TDM and provide evidence for their rational use. We report a consensus on TDM guidelines for polymyxin B, as endorsed by the Infection and Chemotherapy Committee of the Shanghai Medical Association and the Therapeutic Drug Monitoring Committee of the Chinese Pharmacological Society. The consensus panel was composed of clinicians, pharmacists, and microbiologists from different provinces in China and Australia who made recommendations regarding target concentrations, sample collection, reporting, and explanation of TDM results. The guidelines provide the first-ever consensus on conducting TDM of polymyxin B, and are intended to guide optimal clinical use.
Humans ; Anti-Bacterial Agents/therapeutic use* ; China ; Drug Monitoring/methods* ; Polymyxin B ; Practice Guidelines as Topic