1.Elementary studies on intrinsic inhibitor that retards germinaton of seed of Astragalus membranaceus
Chinese Traditional and Herbal Drugs 1994;0(07):-
Object An attempt to seek after an intrinsic inhibitor present in the seed of Astragalus membranaceus (Fisch.) Bge.. Methods Crude ethereal extract of the seed was prepared and treated on paper chromatography. Inhibitory effects of different fractions with different Rf value were tested on Brassica chinensis L. and wheat germination. Effect of steeping the seed in warm water at 41 ℃ or 45 ℃ for different periods of time was also studied.Results Seed of A. membranaceus does contain strong intrinsic inhibitor. The portion of its ethereal extract with Rf 0.9 showed the most strong inhibition for the germination of Brassica, and the fraction with Rf 1.0 can inhibit the growth of the tender Brassica root, steeping with warm water can remove most of the intrinsic inhibitor, which also inhibits the growth of both aerial and underground parts of wheat sprouts, but without effect on its seed germination. It also showed strong inhibition of seed germination and growth of tender root of A. membranaceus. Conclusion Besides the low water permeability of the seed peel, the intrinsic inhibitor present in A. membranaceus is another essential factor that retard its germination.
5.Clinical Significance of Changes in NT-proBNP, Hcy and Partial Coagulation-Fibrinolytic Indexes with Acute Cerebral Infarction
Yu WANG ; Xiue LI ; Man ZHAO ; Ya ZHAO ; Ning LI
Journal of Modern Laboratory Medicine 2017;32(3):89-91
Objective To Analyze the examination meaning of b-type brain natriuretic peptide precursor (NT-proBNP),homocysteine and coagulation-fibrinolysis indexes for patients with acute cerebral infarction.Methods Selected 40 patients with acute cerebral infarction (experimental group) to hospital from March 2014 to May 2015 and 40 healthy check-up cases (control group).Then,compared the indicators in blood between the two groups of patients,namely homocysteine (Hcy),NT-proBNP,activated clotting time live enzymes enzyme (APTT),original activator inhibitory factor (PAI-1) and tissuetype fibrinolytic enzyme original activator (tPA).Meanwhile,also compared these indicators for the experimental group before and after treatment.Results Before treatment,the levels of Hcy,t-PA,NT-proBNP,PAI-1 and ATPP for experiment group were 17.7±3.6 μmol/L,29.4±7.9 μmol/L,3 212.8±2 511.4 ng/L,130.1±17.8 μmol/L and 37.8±4.5 s,respectively.The levels of Hey,t-PA,NT-proBNP,PAI-1 and ATPP for control group were 7.2± 2.1 μmol/L,15.1 ± 3.7 μmol/ L,198.7 ± 1 14.8 ng/L,67.8 ± 7.9 μmol/L and 37.8 ± 4.5 s,respectively.After treatment,the levels of Hcy,t-PA,NT-proBNP,PAI-1 and ATPP for experiment group were 12.2±1.5 μmol/L,18.2±2.3 μmol/L,348.7±194.8 ng/L,78.6±9.8 μmol/L and 32.2±4.5 s,respectively.Before treatment,the indicator of APTT for experiment patients was significantly shorter than it after treatment and that of the control group.The other four indicators were significantly higher than them after treatment and those of the control group.The differences were statistically significant (P <0.05).Conclusion Hcy,NT-proBNP,APTT,PAI-1,and t-PA had closely relation with the occurrence of acute cerebral infarction development,and they can be helpful to evaluate disease progression and predict prognosis for patients with acute cerebral infarction.
6.Quantification of sitagliptin in human plasma and urine by LC-MS/MS method and its application.
Qian ZHAO ; Bo-ya WANG ; Ji JIANG ; Pei HU
Acta Pharmaceutica Sinica 2015;50(6):714-718
A rapid and sensitive liquid chromatography-mass spectrometry/mass spectrometry (LC-MS/MS) method for quantification of sitagliptin in human plasma and urine had been developed. This method was applied to the pharmacokinetics study of sitagliptin tablet after single- and multiple-dosing in Chinese population. Plasma samples were prepared by a liquid-liquid extracted method, and urine samples were diluted. Compounds were analyzed by multiple reaction monitoring (MRM) mode with a electrospray ionization (ESI) interface. Mobile phase consisted of methanol and water (85 : 15, v/v). The linear concentration range of calibration curve was 0.5-1 000 ng.mL-1. and 0.2-100 µg.mL , intra-run/between-run accuracy was 98.98%-103.69% and 97.63%-102.29%, intra-run/between-run precision was <5.51% and 4.26% for plasma and urine sample, respectively. The stability of sitagliptin stock solution was tested for 55 days at -30 °C. Sitagliptin was stable when stored under the following conditions: 24 hours in the autosampler after sample preparation; 24 hours at room temperature, after 3 freeze and thaw cycles (from -30 °C to room temperature), 40 days at -30 °C for plasma and urine samples. The absolute recovery in plasma was 71.1%, and no matrix effect was founded. This method was proved simple, specific, sensitive, rapid and suitable for pharmacokinetics study of sitagliptin in human being.
Calibration
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Chromatography, Liquid
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Humans
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Liquid-Liquid Extraction
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Sitagliptin Phosphate
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blood
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pharmacokinetics
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urine
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Tandem Mass Spectrometry
7.Investigation on pharmacokinetics and bioavailabiUty of insulin dry powder inhalation
Wei-Gang ZHAO ; Heng WANG ; Qi SUN ; Ya-Xiu DONG ;
Chinese Journal of Endocrinology and Metabolism 2001;0(05):-
Objective To study the characteristics of pharmacokinetics and pharmacodynamics of insulin dry powder inhalation and its relative bioavailability as compared with subcutaneous injection of regular insulin. Methods In this open,single-center,randomized,two-period,cross-over,euglycemic glucose clamp study,18 healthy volunteers(14 men and 4 women),aged(24.9?1.7)years,with body mass index(20.6?1.2)kg/m~2, received the insulin dry powder inhalatin(80 U)or regular insulin(15 U)subcutaneous administration.The blood samples of this study at 0,20,30,40,50,60,70,80,90,100,110,120,135,150,165,180,195, 210,225,240,270,300,330,360,390,420,450 and 480 rain were taken for serum insulin measurement, meanwhile,glucose infusion rates(GIR)were determined per 5 minutes over a period of 8 hours.Results The C_(max)were(57.9?17.8 vs 114.5?29.7)mU/L(tested vs reference preparation),T_(max)were(46.7?45.6 vs 107.8?33.7)min,GIR_(max)were(3.35?0.98 vs 5.17?1.75)mg?kg~(-1)?min~(-1)and T_(GIRmax)were(88.3?17.0 vs 151.9?34.6)min.The relative bioavailability was(10.26?2.25)%,and the relative bioefficacy was(14.33?7.26)%.Conclusion The study shows that insulin dry powder inhalation is absorbed via lungs and its action sets in earlier than that of the regular insulin injected subcutaneously.These pharmacokinetie and pharmacodynamic data may provide a reliabe guide for further clinical trial.
8.Effects of valsartan on L-type calcium current in ventricular myocytes of rabbits after myocardial infarction
Ya ZHONG ; Congxin HUANG ; Qingyan ZHAO ; Teng WANG ; Feng CAO
Chinese Journal of Emergency Medicine 2010;19(9):949-952
Objective To determine the effects of valsartan, a specific angiotensin Ⅱ type 1 receptor blockade, on arrhythmia in rabbits after myocardial infarction and to discuss the mechanism. Method Twentyfour rabbits were randomly (random number) divided into sham operated (SO) group ( n = 8), myocardial infarction (MI) group ( n = 8) and valsartan (VAL) group ( n = 8). The rabbits of SO group were operated upon with median stemotomy without left ventricular coronary artery hgature. The rabbits of MI group and VAL group had median stemotomy with left ventricular coronary artery ligature. After MI, the rabbits of VAL group were fed with border zone of infracted left ventricular wall and the L-type calcium current was recorded by whole-cell patch clamp technique. Results Ventricular tachycardia or fibrillation (VT/VF) episodes were markedly decreased in VAL group than that in MI group [(3.2 ± 0. 6) vs. ( 11.7 ± 1.8)] after 12 weeks. The density of Ica-L current was higher in MI group than that in SO group and VAL group [( - 9.12 ± 0.73) pA/pF vs. ( - 6.29 ± 0.65) pA/pF and ( - 6.75 ± 0.64) pA/pF], ( P < 0.05), however, there were no significant differences in Ica-L current between So group and VAL group ( P > 0.05). Conclusions Valsartan reduces the VT/VF episodes in rabbits after MI. The effects of valsartan may be attributed to the inhibited electrical remodeling after MI.
9.Pancreatitis in patients with primary hyperparathyroidism
Ya HU ; Quan LIAO ; Zheyu NIU ; Mengyi WANG ; Yupei ZHAO
Chinese Journal of Endocrine Surgery 2016;10(1):33-36
Objective To investigate the clinical characters of pancreatitis in patients with primary hyperparathyroidism (PHPT).Methods The clinical data of patients with PHPT undergoing parathyroidectomy from Jan.2009 to May.2014 in Peking Union Medical College Hospital were retrospectively analyzed for coexistent pancreatitis.Results 571 patients received parathyroidectomy due to PHPT during this period.Thirteen patients (2.3%)with PHPT were confirmed with coexistent pancreatitis by clinical manifestation and abdominal imaging evaluation,including acute pancreatitis in 9 patients and chronic pancreatitis in 4 patients.PHPT with pancreatitis was associated with preoperative serum intact parathyroid hormone(iPTH)higher than 500 pg/ml (P=0.025)and occurrence of hypercalcemic crisis (P=0.013).The age and sex of patients,preoperative serum calcium,gallstones,urinary calculi and bone fracture were not related with pancreatitis in this group.The average follow-up period for these patients was 34(ranging from 13 to 68)months.All patients were free from hyperparathyroidism recurrence.Only one young lady with chronic pancreatitis suffered from repeated pancreatitis after surgery.Conclusions Serum iPTH higher than 500 pg/ml and occurrence of hypercalcemic crisis were possible risk factor of pancreatitis in patients with PHPT.Parathyroidectomy can help to prevent the recurrence of pancreatitis in these patients.