2.Simultaneous determination of amlodipine, benazepril and benazeprilat in human plasma by LC-HESI/MS/MS method.
Hua-Ling PAN ; Li-Shan LIN ; Jue-Fang DING ; Xiao-Yan CHEN ; Da-Fang ZHONG
Acta Pharmaceutica Sinica 2014;49(1):95-100
The study aims to develop a rapid, sensitive and specified method of liquid chromatography with heated electrospray ionization tandem mass spectrometry (LC-HESI/MS/MS) for simultaneous determination of amlodipine, benazepril and benazeprilat in human plasma using amlodipine-d4 and ubenimex as internal standards (ISs). Selected reaction monitoring (SRM) with heated electrospray ionization (HESI) was used in the positive mode for mass spectrometric detection. Analytes and ISs were extracted from plasma by simple protein precipitation. The reconstituted samples were chromatographed on a C18 (100 mm x 4.6 mm, 5 microm) column with mixture of methanol-acetonitrile-5 mmol.L- ammonium acetate-formic acid (30 : 30 : 40 : 0.1) as mobile phase at a flow rate of 0.6 mL.min-1. The standard curves were demonstrated to be linear in the range of 0.02 to 6.00 ng.mL-1 for amlodipine, 0.2 to 1,500 ng.mL-1 for benazepril and benazeprilat with r2>0.99 for each analyte. The lower limit of quantitation was identifiable and reproducible at 0.02, 0.2 and 0.2 ng mL-1 for amlodipine, benazepril and benazeprilat, respectively. The intra-day and inter-day precision and accuracy results were within the acceptable limit across all concentrations. The plasma samples were stable after four freeze-thaw cycles and being stored for 93 days at -20 degrees C. The method was applied to a pharmacokinetic study of a fixed-dose combination of amlodipine and benazepril on Chinese healthy volunteers.
Administration, Oral
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Amlodipine
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administration & dosage
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blood
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Benzazepines
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administration & dosage
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blood
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Chromatography, Liquid
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Humans
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Sensitivity and Specificity
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Spectrometry, Mass, Electrospray Ionization
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Tandem Mass Spectrometry
3.99Tcm-MIBI myocardial perfusion imaging for evaluation of the myocardial blood supply in patients with metabolic syndrome
Xiao-shan, GUO ; Zhi-fang, WU ; Jian-zhong, LIU ; Guang, HU ; Jin, WANG ; Si-jin, LI
Chinese Journal of Nuclear Medicine 2011;31(3):174-177
Objective To evaluate the myocardial blood supply in patients with metabolic syndrome (MS) using 99Tcm-MIBI SPECT MPI. Methods A total of 342 patients were divided into four groups according to the number of abnormal metabolic indices: no abnormal metabolic index (Group 1), one abnormal index (Group 2), two abnormal indices (Group 3), three or more abnormal indices (Group 4). Each patient underwent two-day protocol of gated stress and rest 99Tcm-MIBI MPI. One hundred and three of the 342 patients were clinically diagnosed as MS and underwent CAG within 1 month after MPI. χ2test was used to evaluate the difference among the four groups and Kappa test to analyze the correlation between MPI and CAG. Results Compared with CAG, the diagnostic sensitivity, specificity, positive and negative predictive values by 99Tcm-MIBI SPECT MPI for coronary artery diseases (CAD) in 103 MS patients were 80.5% (33/41), 85.5% (53/62), 78.6% (33/42) and 86.9% (53/61), respectively. The correlation coefficient between MPI and CAG was 0.657 (P<0.001). The abnormal MPI rates in group 1, 2, 3 and 4 were 23.3% (10/43), 32.9% (26/79), 54.4% (56/103), and 57.3% (67/117), respectively (χ2=23.22, P<0.001). Conclusions In MS patients,99Tcm-MIBI SPECT MPI can be useful for evaluating myocardial blood supply and the myocardial ischemia rates may correlate positively with the number of abnormal metabolic indices.
4.Comparison of anti-inflammatory effects with lotrprednol - tobramycin and tobramysin - dexamethasone eyedrops after phacoemulsification
Xiao-Shan, FANG ; Hong-Chang, YANG ; Jie-Ke, YU ; Bo-Jian, HUANG
International Eye Science 2015;(5):887-889
?AlM:To compare the anti-inflammatory effects with lotrprednol-tobramycin and tobramysin-dexamethasone eyedrops after phacoemulsification combined intraocular lens implantation.
? METHODS: ln this prospective, comparative, randomized controlled trial, patients with senile cataract who underwent phacoemulsification combined intraocular lens implantation in our hospital from January 2014 to October 2014 were enrolled, which were randomly divided into two groups. Patients were given lotrprednol -tobramycin ( LE/T group ) and dexamethasone-tobramysin ( D/T group ) eyedrops respectively. Preoperative and postoperative intraocular pressure, malnutrition inflammation score, bruggrmann comfort scale were observed.
?RESULTS:A total of 143 eyes of 143 cases were enrolled, of them 81 cases were in the LE/T group and 62 in the D/T group. There were no statistically significant differences between the two groups in malnutrition inflammation score and bruggrmann comfort scale. The average intraocular pressure was 16. 5±3. 1mmHg in D/T group after 14d postoperation, which was obviously higher than LE/T group ( 14. 7± 3. 7mmHg, P = 0. 004 ). After 14d postoperation, the intraocular pressure of 2 cases were > 21mmHg, which were back to normal after drug withdrawal.
? CONCLUSlON: The anti - inflammatory effects lotrprednol-tobramycin and tobramysin-dexamethasone eyedrops are similar after phacoemulsification. However, lotrprednol-tobramycin has little influence in intraocular pressure, and more safety.
5.Analysis of Compatibility Laws for Acupoint Selection of Acupuncture in Treating Diabetic Gastroparasis.
Fang CAO ; Tie LI ; Li-juan HA ; Chun-xiao SHAN ; Mu-jun ZHI ; Fu-chun WANG
Chinese Journal of Integrated Traditional and Western Medicine 2016;36(5):549-552
OBJECTIVETo summarize and analyze the compatibility laws for acupoint selection of acupuncture in treating diabetic gastroparasis (DGP) in modern literatures of clinical researches.
METHODSRetrieved were literatures related to treating DGP by acupuncture or acupuncture combined other therapies from PubMed, CNKI, and WF from 1982 to 2014. Analyzed were frequency of acupoint use, meridians selected acupoints belonged to, regions selected, association laws of selected compatible acupoints.
RESULTSRetrieved were 35 with compatibility frequencies more than 15 listed as follows: compatibility frequency of Zusanli (ST36) and Zhongwan (CV12) was 33 (94.29%); compatibility frequency of Zusanli (ST36) and Neiguan (PC6) was 23 (65.71%), compatibility frequency of Zhongwan (CV12) and Neiguan (PC6) was 22 (62.86%), compatibility frequency of Zusanli (ST36), Zhongwan (CV12), and Neiguan (PC6) was 22 (62.86%); compatibility frequency of Zusanli (ST36) and Sanyinjiao (SP6) was 16 (45.71%); compatibility frequency of Zhongwan (CV12) and Sanyinjiao (SP6) was 16 (45.71%); compatibility frequency of Zusanli (ST36), Zhongwan (CV12), and Sanyinjiao (SP6) was 15 (42.86%). Meridians selected acupoints belonged to were sequenced as Foot Yangming Stomach channel, Ren channel, Foot Taiyang Bladder channel, and so on. Acupoints selected were mainly in lower limbs, chest and abdomen, waist and back. The compatibility of Zusanli (ST36) and Zhongwan (CV12) was the most often used with the highest frequency.
CONCLUSIONSThe compatibility laws for acupoint selection of acupuncture in treating DGP were mainly dominated as upper-lower selection, three regions selection, local selection, anterior-posterior selection. The compatibility laws for acupoint selection of acupuncture along meridians were mainly dominated as the convergence points and exterior-interior meridian points.
Acupuncture Points ; Acupuncture Therapy ; Diabetes Complications ; drug therapy ; Diabetes Mellitus ; drug therapy ; Humans ; Meridians ; Stomach ; physiopathology ; Stomach Diseases ; drug therapy
6.Pharmacokinetic effect of combined administration on spinosin and ferulic acid in monarch drug Ziziphi Spinosae Semen kernel.
Rong GAO ; Shan LI ; Xian-jin CHEN ; Xiao-feng WANG ; Shi-xiang WANG ; Min-feng FANG
China Journal of Chinese Materia Medica 2015;40(16):3293-3297
To study the pharmacokinetic effect of different combined administration with monarch drug Ziziphi Spinosae Semen on its main components in rats. Sprague-Dawley (SD) rats were randomly divided into Ziziphi Spinosae Semen group, Ziziphi Spinosae Semen-Fructus Schisandrae Chinensis group, Ziziphi spinosae Semen-Salviae Miltiorrhize Radix et Rhizoma group and Zaoren Ansheng prescription group. After oral administration, HPLC was eluted with the mobile phase of acetonitrle-0.03% phosphate acid water in a gradient mode. The detection wavelength was 280 nm. The pharmacokinetic parameters of spinosin and ferulic acid were calculated by DAS 2. 0 software. Compared with Ziziphi Spinosae Semen group, Ziziphi Spinosae Semen-Fructus Schisandrae Chinensis group, Ziziphi Spinosae Semen-Salviae miltiorrhizae Radix et Rhizoma group showed a lower maximum plasma concentration (C(max)) and area under curve (AUC(0-t)) for spinosin and ferulic acid but higher clearance speed (CL/F); whereas the Zaoren Ansheng prescription group showed higher maximum plasma concentration (C(max)) and area under curve (AUC(0-t)) for spinosin and ferulic acid but lower clearance speed (CL/F). Compared with Ziziphi Spinosae Semen group, prescription group showed slower metabolism of spinosin and ferulic
Animals
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Chromatography, High Pressure Liquid
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Coumaric Acids
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administration & dosage
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blood
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pharmacokinetics
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Drug Interactions
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Drugs, Chinese Herbal
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administration & dosage
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analysis
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pharmacokinetics
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Female
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Flavonoids
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administration & dosage
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blood
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pharmacokinetics
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Humans
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Male
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Rats
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Rats, Sprague-Dawley
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Ziziphus
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chemistry
8.Research on application of determination of MMP-13 in osteoarthritis.
Wen-Xiao CHEN ; Fang-Jun SHAN ; Hong-Ting JIN ; Ping-Er WANG ; Lu-Wei XIAO ; Pei-Jian TONG
China Journal of Orthopaedics and Traumatology 2014;27(7):617-620
Osteoarthritis (OA) is a complex chronic progressive disease attacked by biological and mechanical factors and a result from the anabolic and catabolic imbalance in chondrocyte, subchondral bone and extracellular matrix(ECM). Etiology and pathological of OA are not yet entirely clear. The degradation and destruction of collagen II caused by matrix metalloproteinase -13 (MMP-13) is considered the core factor in the occurrence and development of OA. The research of MMP-13 inhibitor provide ideas and methods for the treatment of OA. In this article,the role and determination of MMP-13 in OA and the development prospect of MMP-13 inhibitor in the treatment of OA research progress were reviewed.
Animals
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Collagen
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metabolism
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Humans
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Matrix Metalloproteinase 13
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analysis
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physiology
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Matrix Metalloproteinase Inhibitors
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therapeutic use
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Osteoarthritis
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drug therapy
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etiology
9.A new indole alkaloid from the stems of Brucea mollis.
Hui CHEN ; M A SHUANG-GANG ; Zhen-Feng FANG ; Gui-Jie ZHANG ; Shi-Shan YU ; Xiao-Guang CHEN
Acta Pharmaceutica Sinica 2014;49(2):225-229
Eight compounds were isolated from the stems of Brucea mollis by various chromatographic techniques such as column chromatography on silica gel and Sephadex LH-20, and preparative HPLC, and their structures were elucidated as bruceolline O (1), 1-(1-beta-glucopyranosyl)-1H-indole-3-carbaldehyde (2), canthin-6-one (3), 11-hydroxycanthin-6-one (4), 9-methoxycanthin-6-one (5), 4-methoxycanthin-6-one (6), infractin (7), and beta-carboline-1-propionic acid (8). The cytotoxic activities of compounds 1-8 against HCT-8 and A549 human cell lines were determined, but none of them exhibited significant activity (IC 50 > 10 micromol x L(-1)). Among them, compound 1 is a new indole alkaloid, and compounds 2 and 5-7 were isolated from this plant for the first time.
Antineoplastic Agents, Phytogenic
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chemistry
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isolation & purification
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pharmacology
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Brucea
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chemistry
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Carbolines
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chemistry
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isolation & purification
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pharmacology
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Cell Line, Tumor
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Humans
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Indole Alkaloids
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chemistry
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isolation & purification
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pharmacology
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Molecular Structure
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Plant Stems
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chemistry
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Plants, Medicinal
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chemistry
10.Effect of Jiawei Foshou San and its compatibility on hepatic P450 enzyme activity and hepatocyte morphology in rats.
Fang-hong SHANG ; Shan FENG ; Fei-yan ZHANG ; Qian CHEN ; Xian-jin CHEN ; Ji-fen ZHANG ; Xiao-yu XU
China Journal of Chinese Materia Medica 2015;40(10):2030-2036
To investigate the effect of Jiawei Foshou San and its various combined administration on hepatic P450 enzyme activity and hepatocyte morphology in rats. Rats were orally administered with drugs for four weeks and then sacrificed to prepare liver microsomes. The liver microsomes were incubated with the cocktail method; The metabolites were determined with the rapid liquid chromatography with tandem mass spectrometry (LC-MS/MS) to investigate the hepatocyte P450 enzyme activity. In addition, the hepatic pathological changes were observed by using the hematoxylin and eosin (HE) staining. Compared with the control group, the enzyme activity of CYP1A2 and CYP3A4 in the Jiawei Foshou san group showed a significant rise (P < 0.05); the enzyme activity of CYP1A2, CYP2C9, CYP2D6, CYP2E1 and CYP3A4 in the ferulic acid + ligustrazine group and the ligustrazine + tetrahydropalmatine group showed a significant rise (P < 0.05) ; the enzyme activity of CYP1A2, CYP2D6 and CYP2E1 in the ligustrazine group showed a significant rise (P < 0.05); the enzyme activity of CYP3A4 in the ferulic acid group showed a significant reduction (P < 0.05). After the administration with various drugs, the hepatocyte morphologies in the ferulic acid group and the ligustrazine group were normal. The pathological changes were observed in the tetrahydropalmatine group, such as unclear boundary of hepatic lobules, disordered hepatic cell arrangement, blurred edge, anisokaryosis and infiltration of inflammatory cells. The ferulic acid + tetrahydropalmatine group, the ligustrazine + tetrahydropalmatine group and the Jiawei Foshou San group also showed inflammatory infiltration, but with less pathological changes, particularly the Jiawei Foshou San group. The study result shows that Jiawei Foshou San can induce the enzyme activity of CYP1A2 and CYP3A4, and ligustrazine may be the effective substance for inducing CYP1A2. Its combination with ferulic acid and ligustrazine can significantly reduce the liver toxicity of tetrahydropalmatine.
Animals
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Cytochrome P-450 Enzyme System
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metabolism
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Drugs, Chinese Herbal
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administration & dosage
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Female
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Hepatocytes
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drug effects
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enzymology
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Microsomes, Liver
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drug effects
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enzymology
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Rats
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Rats, Sprague-Dawley