Objective: To preliminarily explore the clinical characteristics and gender difference of patients with variant angina (VA) in China. Methods: A total of 312 patients with spontaneous attack of VA admitted in our hospital from 2003-01 to 2009-12 without stimulation test were retrospectively studied. The clinical features were compared between male and female patients to reveal the similarities and differences of VA by genders. Results: The predilection of VA was in male gender (274/312, 87.8%), the common risk factors including smoking, hypertension and hyperlipidemia; 55/312 (17.6%) patients had allergy history. There were 59/312 (18.9%) patients combining arrhythmia while VA attack; coronary angiography (CAG) found that 155/283 (54.8%) patients were with ifxed coronary stenosis and 22/312 (7.1%) combining coronary myocardial bridge. Nitrates, calcium antagonist and stent implantation may effectively control VA attack. Compared with male, female patients had the lower ratio of smokers (10.5% vs 78.8%),P<0.01, higher ratios of family history of coronary artery disease (CAD) (31.6% vs 11.3%),P<0.01, ventricular tachycardia (13.2% vs 3.6%)P<0.05 and ventricular ifbrillation (7.9% vs 1.8%),P<0.05. Conclusion: VA is a cardiac ischemia caused by coronary artery spasm with high incidence for combining arrhythmia, without in time treatment it may incur myocardial infarction even sudden death. VA patients should receive routine CAG and stent implantation according to the severity of stenosis. Female patients were with less smokers while higher ratios in family history of CAD, ventricular tachycardia and ventricular ifbrillation.

An analytical method was developed for the simultaneous extraction and determination of eighteen fluoroquinolones (FQs), tetracyclines (TCs) and sulfonamides (SAs) antibiotics from soils using solid phaseextraction and liquid chromatography tandem mass spectrometry.Soil sample was firstly extracted by phosphate buffer at pH 3 in combination with 50% of organic modifier acetonitrile, then purified and concentrated by SAX and HLB column.Qualitative and quantitative analysis were carried out for the analyte under the MRM mode after the chromatography separation on Kromasil C_(18)(250 mm x4.6 mm, 5 μm) column.The range of recoveries (in percent) for FQs, TCs, SAs, in the soil matrix was 67.20%-88.98%, 62.23%-85.36%, 55.76%-97.37% with 1.1%-17.2% of relative standard deviation respectively in two different concentra tions.The limits of quantification (LOQ, S/N = 3) were 3.36-8.88 jig/kg, 0.56-0.91 μg/kg and 0.07-1.85 μg/kg for FQs, TCs and SAs, respectively.This method was successfully used to detect 18 anti biotics in 6 soil samples with different land types in Tianjin.Results showed some of the antibiotics in the arable soil were detected, with concentrations of 1.72-119.57 μg/kg.

Objective: To explore the safety and efficacy of lipoprotein apheresis (LA) in treating the patients with familial hypercholesterolemia (FH).
Methods: A total of 12 FH patients treated in our hospital from 2015-02 to 2016-10 were retrospectively studied. Based on intensive cholesterol lowering therapy with rosuvastatin (10-20) mg Qd and Ezetimibe 10 mg Qd, the patients received LA by double ifltration plasma pheresis (DFPP) via bilateral elbow central vein or femoral vein. The changes of lipid level were compared at before and after LA treatment.
Results: For pre- and immediately after LA treatment, the average total cholesterol (TC) was (9.42±3.65) mmol/L vs (2.84±0.83) mmol/L, low density lipoprotein cholesterol (LDL-C) was (7.31±3.46) mmol/L vs (1.95±0.82) mmol/L; at 1, 3, 7 and 30 days after treatment, TC and LDL-C levels showed increasing trend, while they were still lower than they were before treatment, allP<0.01. For pre- and immediately, 1 day, 3 days after treatment, the average HDL-C level was (0.96±0.31) mmol/L, (0.63±0.17) mmol/L, (0.56±0.15) mmol/L and (0.68±0.22) mmol/L respectively,P<0.05-0.01. For pre- and immediately after LA treatment, the average TG level was (1.90±0.86) mmol/L vs (0.88±0.38) mmol/L,P<0.05. Only 1 patient had the symptoms of hypotension, nausea and sweat, the patient was relieved by expectant treatment.
Conclusion: LA therapy may decrease blood levels of TC and LDL-C at short term in FH patients with good tolerance;even TC and LDL-C could slowly increase after treatment, while combining with lipid lowering therapy, it has been a safe and effective method for treating relevant patients.

Objective To investigate the incidence, imaging and clinical characteristics in elderly patients with coronary artery ectasia (CAE). Methods A retrospective analysis was conducted on patients with CAE who underwent coronary angiography between January 2006 and December 2012. According to age, the enrolled patients were divided into two groups (elderly group, age≥ 65 years; non-elderly group, age < 65 years). The clinical feature, imaging characteristics and the 5-year survival rate of the two groups were compared.Results The preva-lence of CAE in elderly patients was 0.33%. Patients in elderly group were found to have significantly higher proportion of female (30.1%vs. 10.1%,P< 0.001), three-vessel disease (60.5%vs. 45.2%,P = 0.003) and localized ectasia (55.0%vs. 40.2%,P = 0.003). In addition, body mass index (20.90 ± 2.71 kg/m2vs. 22.31 ± 2.98 kg/m2,P < 0.001) and percentage of current smokers (45.0%vs. 64.6%,P < 0.001) were significantly lower in elderly group. Cumulative survival curves demonstrated reduced 5-year cumulative survival at the follow-up in the elderly group compared with the non-elderly group (88.0%vs. 96.0%,P = 0.002). But the 5-year event free survival rate failed to show a significant difference between the two groups (31.0%vs. 35.0%,P= 0.311).ConclusionThe prevalence of CAE in elderly patients was 0.33%, which was about 1/3 of the entire numbers of CAE patients. There were significant differences between the elderly and the non-elderly patients with CAE in terms of coronary artery disease risk factors and coronary artery ectatic characteristics. CAE might be asso-ciated with increased mortality risk in the elderly.

To provide a scientific basis for the selection of the appropriate drying method for Mentha Haplocalyx Herba (MHH), determine 2 monoterpenes, 4 phenolic acids and 5 flavonoids in MHH by GC-MS and UPLC-TQ-MS methods, and investigate the effects of the drying methods on the changes in contents of these analytes. The qualities of products obtained with different drying methods were evaluated by the multivariate statistical method of Technique for Order Preference by Similarity to Ideal Solution (TOPSIS). Results showed that the drying methods had the greatest impact on menthol, caffeic acid, and rosemary acid, which were followed by chlorogenic acid and diosmetin-7-O-glucoside. The contents in these analytes processed with hot-air-drying method were higher than those with microwave-drying and infrared-drying methods at the same temperatures. The contents in these analytes processed under low temperature (40-45 °C) were higher than those under higher temperature (60-70 °C). Above all, the contents in phenolic acids processed with microwave fixation (exposed under microwave at 100 °C for several minutes) were obviously higher than those of not being processed, showing an inhibition of some enzymes in samples after fixation. The TOPSIS evaluation showed that the variable temperature drying method of 'Hot-Air 45-60 °C' was the most suitable approach for the primary drying processing of MHH. The results could provide the scientific basis for the selection of appropriate drying method for MHH, and helpful reference for the primary drying proces of herbs containing volatile chemical components.
Desiccation ; methods ; Flavonoids ; analysis ; Hydroxybenzoates ; analysis ; Mentha ; chemistry ; Monoterpenes ; analysis

Antibody-drug conjugate (ADC) is a new class of therapeutics composed of a monoclonal antibody and small cytotoxin moieties conjugated through a chemical linker. ADC molecules bind to the target antigens expressed on the tumor cell surfaces guided by the monoclonal antibody component. The binding ADC molecules can be internalized and subsequently the toxin moieties can be released within the tumor cells via chemical and/or enzymatic reactions to kill the target cells. The conjugation combines the merits of both components, i.e., the high target specificity of the monoclonal antibody and the highly potent cell killing activity of the cytotoxin moieties. However, such complexities make the pharmacokinetic and metabolic studies of ADCs highly challenging. The major challenges should include characterization of absorption, distribution, metabolism and excretion, investigation of underlying mechanisms, assessment of pharmacokinetic- pharmacodynamic relationship, and analytical method development of ADC drugs. This review will discuss common pharmacokinetic issues and considerations, as well as tools and strategies that can be utilized to characterize the pharmacokinetic and metabolic properties of ADCs.
Antibodies, Monoclonal ; pharmacokinetics ; Cytotoxins ; pharmacokinetics ; Humans ; Immunoconjugates ; pharmacokinetics ; Neoplasms ; drug therapy

To establish the water dynamics model for drying process of Angelicae Sinensis Radix, the Weibull distribution model was applied to study the moisture ratio variation curves, and compared the drying rate and drying activation energy with the drying methods of temperature controllable air drying, infrared drying under different temperatures (50, 60, 70 degrees C). The Weibull distribution model could well describe the drying curves, for the moisture ratio vs. drying time profiled of the model showed high correlation (R2 = 0. 994-0. 999). The result proved that the drying process of Angelicae Sinensis Radix belonged to falling-rate drying period. For the drying process, the scale parameter (a) was related to the drying temperature, and decreased as the temperature increases. The shape parameter (β) for the same drying method, drying temperature had little impact on the shape parameter. The moisture diffusion coefficient increase along with temperature increasing from 0.425 x 10(-9) m2 x s(-1) to 2.260 x 10(-9) m2 x s(-1). The activation energy for moisture diffusion was 68.82, 29.60 kJ x mol(-1) by temperature controllable air drying and infrared drying, respectively. Therefore, the Weibull distribution model can be used to predict the moisture removal of Angelicae Sinensis Radix in the drying process, which is great significance for the drying process of prediction, control and process optimization. The results provide the technical basis for the use of modern drying technology for industrial drying of Angelicae Sinensis Radix.
Angelica sinensis ; chemistry ; Desiccation ; methods ; Models, Theoretical ; Water

This article is report the study of the pharmacokinetics and metabolic disposition of exogenous phosphocreatine (PCr) in rats by means of an ion-pair HPLC-UV assay. PCr and its metabolite creatine (Cr) and related-ATP in rat plasma and red blood cell (RBC) were simultaneously determined. A blank plasma and RBC were initially run for baseline subtraction. Plasma and RBC samples were deproteinized with 6% PCA prior to HPLC. Following i.v. administration of PCr 500 mg x kg(-1) and 1 000 mg x kg(-1) the C-T curve could be described by the two-compartment model with t1/2beta 22.5-23.3 min, V(d) 0.956 4-0.978 6 L x kg(-1), CL 0.029 L. kg(-1) x min(-1). The Cr as PCr degraded product appeared as early as 2 min post i.v. dosing with t(max) 20 min, t1/2kappa (m) 40.6-42.7 min and f(m) 60%-76%. After po administration of PCr, the parent drug in plasma was undetectable, but the metabolite Cr was detected with t(max) 65-95 min, t1/2kappa (m) 56.0-57.7 min, metabolite-based bioavailability F(m) 55.02%-62.31%. PCr i.v. administration resulted in significant elevation of ATP level in RBC but not in plasma, the related-ATP in RBC was characterized by t(max) 68-83 min, t1/2kappa 49-52 min. In RBC no exogenous PCr was found but Cr was detected following i.v. administration of PCr, with the t(max) 120 min and t1/2k (m) 70 min for Cr. The above results indicate that PCr eliminates and bio-transforms in body very rapidly; K > K(m) confers ERL, instead of FRL, type upon the metabolic disposition of Cr. Following po administration of PCr, the degraded product Cr is absorbed but not the parent drug PCr. The formed Cr can be accounted for by most of i.v. and po PCr. Intravenous dosing leads apparently increased and sustained Cr and related-ATP concentration in RBC.
Adenosine Triphosphate ; blood ; pharmacokinetics ; Administration, Oral ; Animals ; Area Under Curve ; Biological Availability ; Biotransformation ; Cardiotonic Agents ; administration & dosage ; blood ; pharmacokinetics ; Creatine ; administration & dosage ; metabolism ; pharmacokinetics ; Erythrocytes ; metabolism ; Injections, Intravenous ; Male ; Phosphocreatine ; administration & dosage ; blood ; pharmacokinetics ; Rats ; Rats, Sprague-Dawley

LC-MS/MS method was used to simultaneously determine anti-oxidative active catechins EGCG, ECG, EGC and EC in plasma of rats treated with tea polyphenols (TP). The integrated plasma concentration (C') of TP was calculated by means of self-defined weighing coefficient based on percent AUC of individual components, thereby assessing integrated pharmacokinetic (PK) parameters of TP via log C'-T curve. The anti-free radical effects of TP were estimated using inhibitory rate of drug-containing serum collected at different times from rats against in vitro lipid peroxidation of mouse liver homogenate. The obtained E-T curves were used to calculate anti-free radical pharmacodynamic (PD) parameters of TP. E-logC and E-log C' plots and linear regression were carried out in order to obtain the correlation coefficient (R2). The results indicated that the log C'-T curves of TP, which could be best described by three-compartment model, corresponded to elimination rule of iv administration of drugs. The integrated PK parameters showed that TP was distributed in body rapidly and widely, and eliminated from deep compartment slowly. From comparison of R2 values and consistence of C'-T course and E-T course, it was evident that TP integrated PK behaviors correlated much better with its PD behaviors than individual active components, and thus demonstrated that integrated PK parameters could characterize to maximal extent holistic disposition of Chinese herbal drugs and reflect residence properties of holistic effective substances in biological body.
Animals ; Antioxidants ; pharmacokinetics ; pharmacology ; Area Under Curve ; Catechin ; analogs & derivatives ; pharmacokinetics ; Chromatography, Liquid ; Free Radical Scavengers ; blood ; pharmacokinetics ; pharmacology ; Free Radicals ; metabolism ; Injections, Intravenous ; Lipid Peroxidation ; drug effects ; Male ; Mice ; Polyphenols ; blood ; pharmacokinetics ; pharmacology ; Rats ; Rats, Sprague-Dawley ; Tandem Mass Spectrometry ; Tea ; chemistry

OBJECTIVETo evaluate the correlation of pesticide exposure with childhood acute leukemia.

METHODSAn exploratory case-control study was conducted among childhood acute leukemia patients under 15 years old in Shanghai, China. From January 1st, 2006 to December 31st, 2008, a total of 80 newly diagnosed acute leukemia patients were recruited from Shanghai Children's Medical Center for the case group. Another 96 age-matched patients who visited the hospital for health examination, pediatric treatment or osteological therapy excluding hematological system diseases and neoplastic disease, were recruited for the control group. A questionnaire survey was conducted in both groups; and a 30 - 40 ml random urine sample was collected from each participant. Five types of organophosphorus pesticide metabolites was then detected among the samples, using Gas Chromatography with Flame Spectrophotometry.

RESULTSAccording to result of the questionnaire survey, more participants (55.0% (44/80)) in case group than in the control group (33.3% (32/96)) reported using mosquitocidal, which might increase the risk of childhood acute leukemia (OR = 2.444; 95%CI: 1.326 - 4.506). At the same time, the detection showed that the concentration (median) of organophosphate metabolites diethyl phosphate, dimethyl phosphate, dimethyl thiophosphate, diethyl thiophosphate and diethyl dithiophosphate in case group were 0.0682, 0.0082, 0.0183, 0.0233, 0.4259 µg/g Cr, which were all significantly higher than in control group (0.0865, 0.0025, 0.0112, 0.0123, 0.1207 µg/g Cr) except the concentration of diethyl phosphate (Z = -1.081, P = 0.279). The difference showed statistical significance (Z = -5.752, -2.800, -3.316, -8.120, P < 0.05).

CONCLUSIONPesticide exposure may be one of the risk factors for childhood acute leukemia.

Acute Disease ; Adolescent ; Case-Control Studies ; Child ; Child, Preschool ; Environmental Exposure ; adverse effects ; Female ; Humans ; Infant ; Infant, Newborn ; Leukemia ; etiology ; Male ; Maternal Exposure ; Pesticides ; adverse effects ; Pregnancy ; Risk Factors