Purinergic P2Y Receptor Antagonists ; Consensus ; Cardiovascular System ; Cardiology ; Asia

Licorice has long been regarded as one of the most popular herbs, with a very wide clinical application range. Whether being used alone or as an ingredient in prescription, it has an important role which cannot be ignored. However, the efficacy and chemical constituents of licorice will change after honey-processing. Therefore, it is necessary to find quality markers before and after honey-processing to lay the foundation for a comprehensive evaluation of the differences between raw and processed licorice pieces. HPLC-DAD was employed to establish fingerprints of raw and processed licorice. Multivariate statistical analysis methods including principal component analysis(PCA) and orthogonal partial least squares discrimination analysis(OPLS-DA) were applied to screen out the differential components before and after processing of licorice. Based on network pharmacology, the targets and pathways corresponding to the differential components were analyzed with databases such as Swiss Target Prediction and Metascape, and the "component-target-pathway" diagram was constructed with Cytoscape 3.6.0 software to predict the potential quality markers. A total of 17 common peaks were successfully identified in the established fingerprint, and seven differential components were selected as potential quality markers(licoricesaponin G2, glycyrrhizic acid, liquiritigenin, liquiritin, isoliquiritin, liquiritin apioside and isoliquiritigenin). The HPLC fingerprint method proposed in this study was efficient and feasible. The above seven differential chemical components screened out as potential quality markers of licorice can help to improve and promote the overall quality. These researches offer more sufficient theoretical basis for scientific application of licorice and its corresponding products.
Chromatography, High Pressure Liquid ; Drugs, Chinese Herbal ; Glycyrrhiza ; Glycyrrhizic Acid/analysis* ; Honey/analysis*

AIM To establish an HPLC method for the simultaneous content determination of seven constituents in Gnaphalium affine D.Don.METHODS The analysis of 80％ methanol of G.affine was performed on a 30 ℃ Atlantis (C) T3 column (4.6 mm× 250 mm,5 μm),with the mobile phase comprising of acetonitrile-formic acid flowing at 1.0 mL/min in a gradient elution manner,and the detection wavelength was set at 288 nm.RESULTS Seven constituents showed good linear relationships within their own ranges (R2 ≥0.999 8),whose average recoveries were 98.58％-103.8％ with the RSDs of 0.88％-1.74％.CONCLUSION This accurate,stable and reproducible method can be used for the quality control of G.affine.

AIM To study the chemical constituents from Lonicera similes Hemsl.METHODS The 80％ ethanol extract from L.similes was isolated and purified by silica,antiphase silica and polyamide column,then the structures of obtained compounds were identified by physicochemical properties and spectral data.RESULTS Nine compounds were isolated and identified as amentoflavone (1),luteolin (2),rutin (3),oleanolic acid (4),chlorogenic acid (5),aesculetin (6),inositol (7),glucose (8),β-sitosterol (9).CONCLUSION Compounds 1,3,4,6,7,8 are isolated from this plant for the first time.

Objective To observe the clinical efficacy and safety of ilaprazole enteric-coated tablets combined with clarithromycin tablets and furazolidone tablets in the treatment of elderly peptic ulcer.Methods Ninety-six elderly patients with peptic ulcer were randomly divided into control and treatment groups with 48 cases per group.Control group was treated with omeprazole enteric-coated capsules 40 mg per time,bid,orally + clarithromycin tablets 0.5 g per time,bid,orally + furazolidone tablets 100 mg per time,qd,orally,continuous treatment for 10 days.Treatment group was treated with ilaprazole enteric-coated tablets 5 mg per time,bid,orally + clarithromycin tablets 0.5 g per time,bid,orally,continuous treatment for 5 days,then treated with ilaprazole enteric-coated tablets 5 mg per time,bid,orally + furazolidone tablet 100 mg per time,qd,orally,continuous treatment for 5 days.The clinical efficacy,Helicobacter Pylori (Hp) positive rate,serum vascular endothelial cell growth factor (VEGF),basic fibtroblast growth factor (bFGF),nitric oxide (NO) and adverse drug reactions were compared between two groups.Results After treatment,the total effective rates of treatment and control groups were 95.83％ (46 cases/48 cases) and 72.92％ (35 cases/48 cases) with significant difference (P ＜0.05).After treatment,the main indexes in treatment and control groups were compared:the Hp positive rates were 4.17％ (2 cases/48 cases) and 20.83％ (10 cases/48 cases),the VEGF were(167.28 ± 12.94) and (145.26 ± 17.87) pg · mL-1,the bFGF were (144.38 ± 14.80) and (123.29 ± 14.46) pg · mL-1,the NO were (31.81 ± 3.50) and (40.92 ± 6.32) μmol · L-1,the differences were statistically significant (all P ＜ 0.05).The adverse drug reactions in the treatment group were dizziness,vomiting and constipation,which in control group were dizziness,rash and diarrhea.The total incidences of adverse drug reactions in treatment and control groups were 8.33％ and 16.67％ without significant difference (P ＞ 0.05).Conclusion Ilaprazole enteric-coated tablets combined with clarithromycin tablets and furazolidone tablets have a definitive clinical efficacy in the treatment of elderly peptic ulcer,which can regulate the levels of serum VEGF,bFGF and NO,without increasing the incidence of adverse drug reactions.

Objective To analyze the status of quality indicators(QI) on specimen acceptability and establish preliminary qual ity specification.Methods Web based External Quality Assessment system was used to collect data of laboratories partici pated in "Medical quality control indicators in clinical laboratory" from 2015 to 2017,including once in 2015 and 2017 and twice in 2016.Rate and sigma scales were used to evaluate incorrect sample type,incorrect sample container,incorrect fill level and anticoagulant sample clotted.The 25th percentile (P25) and 75th percentile (P75) of the distribution of each QI were employed to establish the high,medium and low specification.Results 5 346,7 593,5 950 and 6 874 laboratories sub mitted the survey results respectively.The P50 of biochemistry (except incorrect fill level),immunology and microbiology reach to 6σ.The P50 of clinical laboratory is 4 to 6σ except for incorrect sample container.There is no significant change of the continuous survey results.Based on results in 2017 to establish the quality specification,the P25 and P75 of the four QIs is 0 and 0.084 4 ％,0 and 0.047 6 ％,0 and 0.114 2 ％,0 and 0.078 4 ％,respectively.Conclusion According to the results of the survey,most laboratories had a faire performance in biochemistry,immunology and microbiology,and clinical laboratory needs to be strengthened.Laboratories should strengthen the laboratory information system construction to ensure the actual and reliable data collection,and make a long time monitoring to achieve a better quality.

To study the characteristics and stability of new S(-) pantoprazole sodium hydrates.The X-ray single crystal diffractometer (SXRD), X-ray powder diffractometer (PXRD), thermogravimetric analysis (TG) and infrared spectrometry (IR) were used to characterize S(-) pantoprazole sodium hydrates. The stability of the hydrates was evaluated by high temperature test,affecting factors test and accelerated test.The crystalline water in S(-) pantoprazole sodium hydrates were very easy to lose and obtain, but crystal structure was not changed significantly. The transition from S(-) pantoprazole sodium trihydrate to S(-) pantoprazole sodium hemipentahydrate occurred at approximately 40 ℃ and reversible transitions from hemipentahydrate to trihydrate occurred at high humidity. Two hydrates had no significant difference in accelerated test.The crystal structure of the two hydrates are almost the same, hemipentahydrate is more stable than trihydrates at high temperature or at exposure to light(at 4500 ± 500 lx).

Objective To investigate the effects of tetramethylprazine (TMP) on left ventricular hypertrophy and the regulation of nicotinamide-adenine dinucleotide(NADPH) oxidases in renovascular hypertension of rat.Methods Hypertensive rats were obtained by using two-kidney-two-clip (2K2C) method.Rats were classified into sham-operated group,model group,low,high dose experimental groups (TMP,30,60 mg · kg-1 · d-1) and control group (candesartan,10 mg · kg-1 · d-1).The drugs were continuously administered for 2 weeks.Left ventricular (LV) hemodynamic parameters,serum superoxide ismutase (SOD),dmalondialdehyde (MDA) and hydrogen peroxide(H2O2)levels were measured.The ratio of LV weight to body weight (LVW/BW) was calculated.Hematoxylin-eosin(HE) staining was used for morphological analysis.RT-polymerase chain reaction and Western-blot were performed to investigate the protein expressions of brain natriuretic peptide (BNP),β-myosin heavy chain(β-MHC) and NADPH oxidases(Nox2,Nox4 and P47phox).Results Compared with model group,aortic systolic pressure (AoSP),aortic diastolic pressure (AoDP),LV end-systolic pressure (LVESP),LV end-diastolic pressure(LVEDP) significantly decreased in low,high dose experimental groups with siginificanly (all P ＜ 0.05) while (+ dp/dtmax) and (-dp/dtmax) increased in low,high dose experimental groups with siginificanly (P ＜ 0.05).Compared with model group on LVW/BW (2.8 ± 0.3) mg · g-1,LVW/BW of (1.9 ± 0.2),(1.7 ± 0.4) mg · g-1 in low,high dose experimental groups significantly decreased (P ＜ 0.05).Compared with model group SOD significantly increased while MDA and H2O2 decreased in low,high dose experimental groups with significandy (all P ＜ 0.05).The protein expressions of Nox2 in low,high experimental groups and model group were 0.82 ± 0.08,0.57 ± 0.05,0.30 ± 0.13;the protein expressions of Nox4 in above three groups were 1.00±0.10,0.79 ± 0.07,1.32 ± 0.15 and the protein expressions of P47phox in above three groups were 0.88 ± 0.08,0.65 ± 0.06,1.23 ± 0.15,compared with model group,the protein expression significantly decreased in low,high dose experimental groups with significantly (all P ＜ 0.05).Conclusion TMP attenuated cardiac hypertrophy possibly through decreasing NADPH oxidases (Nox2,Nox4,P47phox) expressions and oxidative stress in renovascular hypertensive rats.

Objective To evaluate the pharmacokinetics of multiple dose of antofloxacin hydroehloride tablet under fast and food state in Chinese healthy subjects.Methods A randomized,open and multiple dose study was conducted.Three dose groups with 16 subjects per group were given the dose of 200,400 and 600 mg antofloxacin hydrochloride tablet,once daily for 7 days respectively.8 subjects (4 male and 4 female) were administrated under fast state and 8 subjects (4 male and 4 female) under food state in each dose.The concentrations of antofloxacin in plasma and urine were determined by HPLC method.Results The main pharmacokinetics parameters of three dose (200,400 and 600 mg) under fast at first day were as follows:Cmax were (2.23 ±0.38),(4.59 ± 1.40),(5.03 ±0.77)mg · L-1,t1/2βwere(11.99 ±3.31),(10.97 ±5.33),(14.39 ± 1.63)h,tmax were (1.37 ±0.78),(2.04 ± 1.42),(2.90 ±2.02)h,AUC0-t were (27.61 ±6.14),(51.77 ±22.09),(73.62 ±10.14)mg · L-1 · h,AUC0-∞ were (38.28 ± 13.49),(72.28 ± 42.80),(108.91 ± 13.26) mg · L-1 · h,V/F were (92.84 ± 12.98),(91.90±14.55),(116.28±22.62)L,CL/F were (5.73 ±1.71),(7.67 ±4.65),(5.58 ±0.66)L· h-1,respectively;under food state at first day,Cmax were (2.36 ± 0.43),(4.11 ± 1.53),(5.60 ± 1.00) mg · L-1,t1/2β were (14.37 ±4.34),(11.25 ±5.39),(15.53 ±2.94) h,tmax were (2.69 ± 1.62),(2.40 ± 1.50),(2.65 ±1.29)h,AUC0-t were (33.69 ±4.00),(48.07 ±22.19),(78.01 ±17.18)mg · L-1 · h,AUC0-∞ were (50.71 ± 8.86),(67.37 ± 41.98),(121.31.66 ± 33.54) mg · L-1 · h,V/F were (81.04 ± 16.35),(106.32 ±34.33),(114.08±20.00)L,CL/Fwere (4.07 ±0.82),(8.28 ±5.29),(5.23 ±1.18)L · h-1,respectively.After 7 days,the main pharmacokinetics parameters of three dose (200,400 and 600 mg) under fast were as follows:Cmax were (3.69 ± 1.39),(7.54 ± 2.95),(8.50 ± 0.93) mg · L-1,t1/2β were (25.22 ± 3.34),(19.56 ±12.47),(15.95 ±2.85)h,tmax were (1.64±1.29),(1.31 ±0.79),(1.60±1.07)h;AUC0-twere (72.29 ± 24.00),(142.96 ± 67.20),(180.81 ± 35.33) mg · L-1 · h,AUC0-∞ were (75.90 ± 25.46),(148.26 ±69.86),(183.30±35.11)mg · L-1 · h,V/F were (184.77 ±52.51),(119.22 ±53.92),(118.91 ±30.13) L,CL/F were (5.06 ± 1.18),(4.75 ± 1.72),(5.15 ±0.72)L · h-1;under food state,Cmax were (3.53 ± 1.06),(6.54 ±1.43),(8.52 ±1.80)mg · L-1,t1/2βwere (24.08 ±6.12),(20.64 ±9.16),(18.69 ±6.49)h,tmax were (2.94 ± 1.02),(1.96 ± 1.05),(2.69 ±0.96)h,AUC0-t were (94.71 ±31.03),(142.17 ±52.46),(211.34.01 ±52.99)mg · L-1 · h,AUC0-∞were (99.32 ±33.93),(149.77 ±55.19),(213.76 ±53.00)mg· L-1 · h,V/F were (139.40±37.39),(140.24±71.11),(130.20 ±71.09)L;CL/F were (4.11 ±1.13),(4.81 ± 1.17),(4.69 ± 0.88)L · h-1.Urinary recovery rates after 7 days doses from zero to 120 h were (67.24±13.56)％,(68.62±14.45)％ and (74.31 ±12.99)％,respectively.Conclusion Food had no obvious influence on pharmacokinetics parameters after multiple oral dose of 200,400 and 600 mg antofloxacin hydrochloride tablet under fast and food state,except that tmax increased.There was no accumulation in human body.It can be considered that food had no effect in the clinical use of antofloxacin hydrochloride tablet.

Objective To establish a HPLC to analyze the content of quercetin and kaempfer in the Camptotheca acuminata Decne leaves.Methods The sample of Camptotheca acuminata Dene leaves were obtained by 5％ hydrochloric acid-methanol The content of quercetin and kaempferol was measured by HPLC with chromatographic column:Hubble C18 (4.6 mm× 250 mm,5 μm),mobile phase:CH3 OH-0.2％ H3PO4(30:70),flow rate:1 mL·min-1,column temperature:30 ℃,detection wavelength:370 nm.The specificity,standard curve and limit of quantification (LOQ),precision and recovery,stability and repeatability were measured.Results The quercetin and kaempferol existed a good linear relation at 5.53-69.08 μg · mL-1 and 3.99-49.90 μg · mL-1,respectively.The LOQ of quercetin and kaempferol was 4.23 and 7.81 ng,respectively.And the average spotting recovery rate of quercetin and kaempferol was 98.94％ and 98.29％,respectively.The RSD values of inter-day and intra-day assays were lower than 0.89％ and 1.04％ for quercetin and kaempferol,respectively.Conclusion This method is an accurate,reliable and convenient method,which is suitable for the quality control of the leaves of Camptotheca acuminata Decne.