The objective of the present study is to examine cardiovascular protective action of a newly developed transdermal patch by incorporating bisoprolol and isosorbide dinitrate in spontaneously hypertensive rats. As the ...The objective of the present study is to examine cardiovascular protective action of a newly developed transdermal patch by incorporating bisoprolol and isosorbide dinitrate in spontaneously hypertensive rats. As the combination therapy with these two synergistic drugs at low doses through a suitable form of administration could provide optimal therapeutic benefit, we further evaluated the effects of a 42 d period of anti-hypertensive treatment in spontaneously hypertensive rats. Rats were divided into the following five groups： control （blank patch）, bisoprolol fumarate tablets （BP-FT, 20.0 mg/kg, i.g.）, bisoprolol transdermal patch （BP-TP, 20.0 mg/kg）, isosorbide dinitrate transdermal patch （ISDN-TP, 20.0 mg/kg）, and the combination of BP and ISDN in a transdermal patch at low doses （8 and 12 mg/kg, respectively）. The effects of treatment were evaluated via biochemical indicators related to cardiovascular protection, structure and function. The combination therapy had synergistic anti-hypertensive effects and significantly reduced blood pressure with the benefit of controlling blood pressure variability compared to BP-FT and BP-TP. The combined treatment also reduced heart rate as well as BP-FT and BP-TP, while ISDN-TP had no evident effects on blood pressure, heart rate, and cardiovascular protection. Combination therapy was superior to BP-TP and BP-FT at increasing blood atrial natriuretic peptide and nitric oxide, while also reducing cardiac hydroxyproline and endothelin-1 with no difference in blood endothelin-1 and cardiac malondialdehyde levels. Cardiovascular remodeling differed among the groups, with the combination therapy reducing cardiac hypertrophy and the aortic media/lumen ratio. The consequential improvements in relaxation in response to cumulative concentrations of acetylcholine may explain the associated improvement in endothelial function. Combi- nation treatment with a transdermal patch exhibited a synergistic therapeutic effect. Such favorable cardiovascular effects with nitric oxide donors and β-blockade combination through a transdermal patch may provide long-term cardiovascular protection during anti-hypertensive treatment.展开更多
AIM: To investigate the tolerance development against the relaxant effect of nitric oxide donating drug isosorbide dinitrate (ISDN) and sodium nitropruside (SNP) in internal anal sphincter (IAS) smooth muscle. METHODS...AIM: To investigate the tolerance development against the relaxant effect of nitric oxide donating drug isosorbide dinitrate (ISDN) and sodium nitropruside (SNP) in internal anal sphincter (IAS) smooth muscle. METHODS: Relaxation responses of ISDN, and electrical fi eld stimulation (EFS) were obtained before and after tolerance induction by ISDN incubation. RESULTS: ISDN (10-7-10-4 mol/L) and SNP (10-8-10-4 mol/L) caused a concentration-dependent relaxation on the basal tonus of the isolated rabbit IAS strips. After a period of 2 h incubation of the 6 x 10-4 mol/L ISDN the relaxation effects of ISDN and SNP did not change compared to control strips. EFS evoked frequency-dependent relaxation in internal anal sphincter smooth muscle and Emax obtained from control strips were not changed in ISDN tolerance-inducing condition. In this study nitrate tolerance was not observed in rabbit IAS smooth muscle. CONCLUSION: This result shows that nitric oxide donating drugs relaxes the internal anal sphincter of the rabbits without the development of tolerance.展开更多
Objectives To evaluate the anti- ischemic effect of ISDN on the patients with coronary heart disease . The change in the size of the defect area as percentage of the entire myocardium as determined by the unfolded sur...Objectives To evaluate the anti- ischemic effect of ISDN on the patients with coronary heart disease . The change in the size of the defect area as percentage of the entire myocardium as determined by the unfolded surface mapping between the baseline and after ISDN infusion reflects the anti-ischemic effect of ISDN. Methods and Results 99m Tc-MIBI myocardial perfusion SPECT images were acquired, and reconstruction of the bull's eye map and unfolded surface mapping were performed according to the dates of tomography images. In the group (99mTc-MIBI was injected at 30 minutes after the start of ISDN iv drip) : at the 65% threshold value, the percentage of the defect area size in the whole ventricle was 33.01 ± 5.35% at baseline, (28.9 ±5.23)% after ISDN was infused (P < 0.05); at the 55% threshold value, the percentage of the defect area size in the whole ventricle was (22.06±5.58)% at baseline, (19.60±4.07)% after ISDN was infused (P < 0.05); the sum of defect blood ST segments is 60 at baseline, 51 after ISDN was infused. In the group (99mTc-MIBI was injected at 60 minutes after the start of ISDN iv drip): at the 65% threshold value, the percentage of the defect area size in the whole ventricle was (29.20±5.08)% at baseline, (20.81±4.16)% after ISDN was infused (P < 0.001); at the 55% threshold value, the percentage of the defect area size in the whole ventricle was (21.2 ± 5.49)% at baseline, (17.52±5.59)% after ISDN was infused (P < 0.001); the sum of defect blood ST segments is 58 at baseline, 47 after ISDN was infused. In the group (99mTc-MIBI was injected at 150 minutes after the start of ISDN iv drip) : at the 65% threshold value, the percentage of the defect area size in the whole ventricle was (32.87 ±6.46)% at baseline, (20.81±4.16)% after ISDN was infused (P < 0.001); at the 55% threshold value, the percentage of the defect area size in the whole ventricle was (18.42± 5.17)% at baseline, (14.18±3.61)% after ISDN was infused (P< 0.001); the sum of defect blood ST segments was 64 at baseline, 41 after ISDN was infused. Conclusions The unfolded surface mapping of 99mTc- MIBI myocardial perfusion image can be used as a method of quantitatively evaluating the anti-ischemic effect of drugs and ISDN iv drip can improve the blood flow in myocardium (myocardium perfusion).展开更多
The thermal behavior and kinetic parameters of the decomposition reaction of triethylene glycol dinitrate (TEGDN) in a temperature-programmed mode at different pressures (0.1, 2, 4 and 6 MPa) have been investigated by...The thermal behavior and kinetic parameters of the decomposition reaction of triethylene glycol dinitrate (TEGDN) in a temperature-programmed mode at different pressures (0.1, 2, 4 and 6 MPa) have been investigated by means of DSC and TG-DTG. The results show that the properties of the thermal decomposition of TEGDN are affected by the change of pressure, and the kinetic model function, the apparent activation energy Ea and pre-exponential factor A of this reaction are []122(1)ln(1)aa---, 106.54 kJ昺ol-1 and 109.17 s-1 at 0.1 MPa, and 120.82 kJ昺ol-1 and 1010.56 s-1 at 2 MPa, respectively. The critical temperature of thermal explosion of TEGDN obtained by the values Teo and Tpo of the onset temperature Te and the peak temperature TP when the heat-ing rate tends to zero are 191.05, 209.86 ℃ at 0.1 MPa, 207.59 and 221.65 ℃ at 2 MPa, respectively.展开更多
Nitrate explosive is hard to detect due to lack of aromatic ring and weak interaction with fluorescence probe.More challenging is even to differentiate the dinitrates with multiple nitrate explosives based on photo in...Nitrate explosive is hard to detect due to lack of aromatic ring and weak interaction with fluorescence probe.More challenging is even to differentiate the dinitrates with multiple nitrate explosives based on photo induced electron transfer or aggregation caused fluorescence change mechanism.A highly selective dinitrate explosive probe was designed based on a new strategy-stepwise aggregation of multiple anchored fluorene dimer 8Py-2 F.Compared with its monomer counterpart 2Py-F,8Py-2 F showed a selective and stepwise fluorescence quenching to dinitrate explosives-ethylene glycol(EGDN)and triethylene glycol dinitrate(TEGDN).The limits of detection(LODs)are 2.72μM for TEGDN and 0.46μM for EGDN,which is three orders of magnitude lower than those of 2Py-F.The stepwise quenching process is well matched with the stepwise aggregation process as evidence by scanning electron microscopy(SEM).Nuclear magnetic resonance(NMR)and quantum chemical calculation proved the interaction force between the dinitrate and 8Py-2 F is hydron bonding interaction,and interaction distance is far less than that of the multiple nitrates coming from the flexibility of the chain and steric hinderance,which resulted in a self-adaptive interaction and higher selectivity.The new strategy is beneficial for the differentiation of the chemicals with similar energy level which is difficult to realize via other method,and the new method provides fluorometric probe for dinitrate explosive detection and makes it an ideal candidate for chemical detection and analysis in public safety and environmental monitoring.展开更多
The transition metal complexes of triaminoguanidine(TAG-M,where M=Cobalt(Co)or Iron(Fe))have been prepared.The catalytic effect of these complexes on the thermolysis of energetic composite based on nitrocellulose and ...The transition metal complexes of triaminoguanidine(TAG-M,where M=Cobalt(Co)or Iron(Fe))have been prepared.The catalytic effect of these complexes on the thermolysis of energetic composite based on nitrocellulose and diethylene glycol dinitrate,has been investigated.Extensive characterization of the resulting energetic composites was carried out using scanning electron microscopy(SEM),X-ray diffraction(XRD),Fourier transform infrared spectroscopy(FTIR),and differential scanning calorimetry(DSC).Isoconversional kinetic analysis was performed to determine the Arrhenius parameters associated with the thermolysis of the elaborated energetic formulations.It is found that TAG-M complexes have strong catalytic effect on the thermo-kinetic decomposition of NC/DEGDN by decreasing the apparent activation energy and significantly increased the total heat release.The models that govern the decomposition processes are also studied,and it is revealed that different reaction processes are accomplished by introduction metal complexes of triaminoguanidine.Overall,this study serves as a valuable reference for future research focused on the investigation of catalytic combustion features of solid propellants.展开更多
AIM: To evaluate the effects of nitroester drugs on human sphincter of Oddi (SO) motility and their antagonistic effects against morphine which shows excitatory effect on Oddi's sphincter motility.METHODS: The eff...AIM: To evaluate the effects of nitroester drugs on human sphincter of Oddi (SO) motility and their antagonistic effects against morphine which shows excitatory effect on Oddi's sphincter motility.METHODS: The effects of these drugs on SO were evaluated by means of choledochofiberoscopy manometry.A total of 67 patients having T-tubes after cholecystectomy and choledochotomy were involved in the study, they were randomly divided into glyceryl trinitrate (GTN) group,isosorbide dinitrate (ISDN) group, pentaerythritol tetranitrate (PTN) group, morphine associated with GTN group, morphine associated with ISDN group and morphine associated with PTN group. Basal pressure of Oddi's sphincter (BPOS), amplitude of phasic contractions (SOCA), frequency of phasic contractions (SOF), duration of phasic contractions (SOD), duodenal pressure (DP) and common bile duct pressure (CBDP) were scored and analyzed. Morphine was given intramuscularly while nitroester drugs were applied sublingually.RESULTS: BPOS and SOCA decreased significantly after administration of ISDN and GTN, BPOS reduced from 10.95±7.49 mmHg to 5.92±4.04 mmHg (P＜0.05) evidently after application of PTN. BPOS increased from 7.37±5.58mmHg to 16.60±13.87 mmHg, SOCA increased from 54.09±38.37 mmHg to 100.70±43.51 mmHg, SOF increased from 7.15±3.20 mmHg to 10.38±2.93 mmHg and CBDP increased 3.75±1.95 mmHg to 10.49±8.21 mmHg (P＜0.01)evidently after injection of morphine. After associated application of ISDN and GTN, the four indications above decreased obviously. As for application associated with PTN,SOCA and SOF decreased separately from 100.64±44.99mmHg to 66.17±35.88 mmHg and from 10.70±2.76 mmHg to 9.04±1.71 mmHg (P＜0.05) markedly.CONCLUSION: The regular dose of GTN, ISDN and PTN showed inhibitory effect on SO motility, morphine showed excitatory effect on SO while GTN, ISDN and PTN could antagonize the effect of morphine. Among the three nitroester drugs, the effect of ISDN on SO was most significant.展开更多
The thermal decomposition behavior and nonisothermal reaction kinetics of the double-base gun propellants containing the mixed ester of triethyleneglycol dinitrate（TEGDN） and nitroglycerin（NG） were investigated by...The thermal decomposition behavior and nonisothermal reaction kinetics of the double-base gun propellants containing the mixed ester of triethyleneglycol dinitrate（TEGDN） and nitroglycerin（NG） were investigated by thermogravimetry（TG） and differential thermogravimetry（DTG）, and differential scanning calorimetry（DSC） under the high-pressure dynamic ambience. The results show that the thermal decomposition processes of the mixed nitric ester gun propellants have two mass-loss stages. Nitric ester evaporates and decomposes in the first stage, and nitrocellulose and centralite II（C2） decompose in the second stage. The mass loss, the DTG peak points, and the terminated temperatures of the two stages are changeable with the difference of the mass ratio of TEGDN to NG. There is only one obvious exothermic peak in the DSC curves under the different pressures. With the increase in the furnace pressure, the peak temperature decreases, and the decomposition heat increases. With the increase in the content of TEGDN, the decomposition heat decreases at 0.1 MPa and rises at high pressure. The variety of mass ratio of TEGDN to NG makes few effect on the exothermic peak temperatures in the DSC curves at different pressures. The kinetic equation of the main exothermal decomposition reaction of the gun propellant TG0601 was determined as： dα/dt=1021.59（1-α）3e-2.60×104/T. The reaction mechanism of the process can be classified as chemical reaction. The critical temperatures of the thermal explosion（Tbe and Tbp） obtained from the onset temperature（Te） and the peak temperature（Tp） are 456.46 and 473.40 K, respectively. ΔS≠, ΔH≠, and ΔG≠ of the decomposition reaction are 163.57 J·mol^-1·K^-1, 209.54 kJ·mol^-1, and 133.55 kJ·mol^-1, respectively.展开更多
36 cases of coronary heart disease with silent myocardial ischemia (SMI) were treated sequentially with Tong Xin Luo (TXL) capsule and isosorbide dinitrate in random order. The results showed that both drugs were effe...36 cases of coronary heart disease with silent myocardial ischemia (SMI) were treated sequentially with Tong Xin Luo (TXL) capsule and isosorbide dinitrate in random order. The results showed that both drugs were effective in decreasing episodes of SMI and shortening the duration of asymptomatic myocardial ischemia. TXL, however, was found with a better action and was superior to isosorbide dinitrate. It was also found that TXL could improve diastolic function of the left ventricle as well.展开更多
基金‘863'High Technology R&D Project of Ministry of Science and Technology of China(Grant No.2004AA2Z3073).
文摘The objective of the present study is to examine cardiovascular protective action of a newly developed transdermal patch by incorporating bisoprolol and isosorbide dinitrate in spontaneously hypertensive rats. As the combination therapy with these two synergistic drugs at low doses through a suitable form of administration could provide optimal therapeutic benefit, we further evaluated the effects of a 42 d period of anti-hypertensive treatment in spontaneously hypertensive rats. Rats were divided into the following five groups： control （blank patch）, bisoprolol fumarate tablets （BP-FT, 20.0 mg/kg, i.g.）, bisoprolol transdermal patch （BP-TP, 20.0 mg/kg）, isosorbide dinitrate transdermal patch （ISDN-TP, 20.0 mg/kg）, and the combination of BP and ISDN in a transdermal patch at low doses （8 and 12 mg/kg, respectively）. The effects of treatment were evaluated via biochemical indicators related to cardiovascular protection, structure and function. The combination therapy had synergistic anti-hypertensive effects and significantly reduced blood pressure with the benefit of controlling blood pressure variability compared to BP-FT and BP-TP. The combined treatment also reduced heart rate as well as BP-FT and BP-TP, while ISDN-TP had no evident effects on blood pressure, heart rate, and cardiovascular protection. Combination therapy was superior to BP-TP and BP-FT at increasing blood atrial natriuretic peptide and nitric oxide, while also reducing cardiac hydroxyproline and endothelin-1 with no difference in blood endothelin-1 and cardiac malondialdehyde levels. Cardiovascular remodeling differed among the groups, with the combination therapy reducing cardiac hypertrophy and the aortic media/lumen ratio. The consequential improvements in relaxation in response to cumulative concentrations of acetylcholine may explain the associated improvement in endothelial function. Combi- nation treatment with a transdermal patch exhibited a synergistic therapeutic effect. Such favorable cardiovascular effects with nitric oxide donors and β-blockade combination through a transdermal patch may provide long-term cardiovascular protection during anti-hypertensive treatment.
文摘AIM: To investigate the tolerance development against the relaxant effect of nitric oxide donating drug isosorbide dinitrate (ISDN) and sodium nitropruside (SNP) in internal anal sphincter (IAS) smooth muscle. METHODS: Relaxation responses of ISDN, and electrical fi eld stimulation (EFS) were obtained before and after tolerance induction by ISDN incubation. RESULTS: ISDN (10-7-10-4 mol/L) and SNP (10-8-10-4 mol/L) caused a concentration-dependent relaxation on the basal tonus of the isolated rabbit IAS strips. After a period of 2 h incubation of the 6 x 10-4 mol/L ISDN the relaxation effects of ISDN and SNP did not change compared to control strips. EFS evoked frequency-dependent relaxation in internal anal sphincter smooth muscle and Emax obtained from control strips were not changed in ISDN tolerance-inducing condition. In this study nitrate tolerance was not observed in rabbit IAS smooth muscle. CONCLUSION: This result shows that nitric oxide donating drugs relaxes the internal anal sphincter of the rabbits without the development of tolerance.
文摘Objectives To evaluate the anti- ischemic effect of ISDN on the patients with coronary heart disease . The change in the size of the defect area as percentage of the entire myocardium as determined by the unfolded surface mapping between the baseline and after ISDN infusion reflects the anti-ischemic effect of ISDN. Methods and Results 99m Tc-MIBI myocardial perfusion SPECT images were acquired, and reconstruction of the bull's eye map and unfolded surface mapping were performed according to the dates of tomography images. In the group (99mTc-MIBI was injected at 30 minutes after the start of ISDN iv drip) : at the 65% threshold value, the percentage of the defect area size in the whole ventricle was 33.01 ± 5.35% at baseline, (28.9 ±5.23)% after ISDN was infused (P < 0.05); at the 55% threshold value, the percentage of the defect area size in the whole ventricle was (22.06±5.58)% at baseline, (19.60±4.07)% after ISDN was infused (P < 0.05); the sum of defect blood ST segments is 60 at baseline, 51 after ISDN was infused. In the group (99mTc-MIBI was injected at 60 minutes after the start of ISDN iv drip): at the 65% threshold value, the percentage of the defect area size in the whole ventricle was (29.20±5.08)% at baseline, (20.81±4.16)% after ISDN was infused (P < 0.001); at the 55% threshold value, the percentage of the defect area size in the whole ventricle was (21.2 ± 5.49)% at baseline, (17.52±5.59)% after ISDN was infused (P < 0.001); the sum of defect blood ST segments is 58 at baseline, 47 after ISDN was infused. In the group (99mTc-MIBI was injected at 150 minutes after the start of ISDN iv drip) : at the 65% threshold value, the percentage of the defect area size in the whole ventricle was (32.87 ±6.46)% at baseline, (20.81±4.16)% after ISDN was infused (P < 0.001); at the 55% threshold value, the percentage of the defect area size in the whole ventricle was (18.42± 5.17)% at baseline, (14.18±3.61)% after ISDN was infused (P< 0.001); the sum of defect blood ST segments was 64 at baseline, 41 after ISDN was infused. Conclusions The unfolded surface mapping of 99mTc- MIBI myocardial perfusion image can be used as a method of quantitatively evaluating the anti-ischemic effect of drugs and ISDN iv drip can improve the blood flow in myocardium (myocardium perfusion).
基金Project supported by the Science and Technology Foundation of the National Defense Key Laboratory of Propellant and Explosive Combustion of China (No. 51455030101ZS3505).
文摘The thermal behavior and kinetic parameters of the decomposition reaction of triethylene glycol dinitrate (TEGDN) in a temperature-programmed mode at different pressures (0.1, 2, 4 and 6 MPa) have been investigated by means of DSC and TG-DTG. The results show that the properties of the thermal decomposition of TEGDN are affected by the change of pressure, and the kinetic model function, the apparent activation energy Ea and pre-exponential factor A of this reaction are []122(1)ln(1)aa---, 106.54 kJ昺ol-1 and 109.17 s-1 at 0.1 MPa, and 120.82 kJ昺ol-1 and 1010.56 s-1 at 2 MPa, respectively. The critical temperature of thermal explosion of TEGDN obtained by the values Teo and Tpo of the onset temperature Te and the peak temperature TP when the heat-ing rate tends to zero are 191.05, 209.86 ℃ at 0.1 MPa, 207.59 and 221.65 ℃ at 2 MPa, respectively.
基金supported by the research program from the Ministry of Science and Technology(2017YFC0821100)the National Natural Science Foundation of China(61731016,61771460)a grant from the Youth Innovation Promotion Association CAS(2015190)
文摘Nitrate explosive is hard to detect due to lack of aromatic ring and weak interaction with fluorescence probe.More challenging is even to differentiate the dinitrates with multiple nitrate explosives based on photo induced electron transfer or aggregation caused fluorescence change mechanism.A highly selective dinitrate explosive probe was designed based on a new strategy-stepwise aggregation of multiple anchored fluorene dimer 8Py-2 F.Compared with its monomer counterpart 2Py-F,8Py-2 F showed a selective and stepwise fluorescence quenching to dinitrate explosives-ethylene glycol(EGDN)and triethylene glycol dinitrate(TEGDN).The limits of detection(LODs)are 2.72μM for TEGDN and 0.46μM for EGDN,which is three orders of magnitude lower than those of 2Py-F.The stepwise quenching process is well matched with the stepwise aggregation process as evidence by scanning electron microscopy(SEM).Nuclear magnetic resonance(NMR)and quantum chemical calculation proved the interaction force between the dinitrate and 8Py-2 F is hydron bonding interaction,and interaction distance is far less than that of the multiple nitrates coming from the flexibility of the chain and steric hinderance,which resulted in a self-adaptive interaction and higher selectivity.The new strategy is beneficial for the differentiation of the chemicals with similar energy level which is difficult to realize via other method,and the new method provides fluorometric probe for dinitrate explosive detection and makes it an ideal candidate for chemical detection and analysis in public safety and environmental monitoring.
文摘The transition metal complexes of triaminoguanidine(TAG-M,where M=Cobalt(Co)or Iron(Fe))have been prepared.The catalytic effect of these complexes on the thermolysis of energetic composite based on nitrocellulose and diethylene glycol dinitrate,has been investigated.Extensive characterization of the resulting energetic composites was carried out using scanning electron microscopy(SEM),X-ray diffraction(XRD),Fourier transform infrared spectroscopy(FTIR),and differential scanning calorimetry(DSC).Isoconversional kinetic analysis was performed to determine the Arrhenius parameters associated with the thermolysis of the elaborated energetic formulations.It is found that TAG-M complexes have strong catalytic effect on the thermo-kinetic decomposition of NC/DEGDN by decreasing the apparent activation energy and significantly increased the total heat release.The models that govern the decomposition processes are also studied,and it is revealed that different reaction processes are accomplished by introduction metal complexes of triaminoguanidine.Overall,this study serves as a valuable reference for future research focused on the investigation of catalytic combustion features of solid propellants.
文摘AIM: To evaluate the effects of nitroester drugs on human sphincter of Oddi (SO) motility and their antagonistic effects against morphine which shows excitatory effect on Oddi's sphincter motility.METHODS: The effects of these drugs on SO were evaluated by means of choledochofiberoscopy manometry.A total of 67 patients having T-tubes after cholecystectomy and choledochotomy were involved in the study, they were randomly divided into glyceryl trinitrate (GTN) group,isosorbide dinitrate (ISDN) group, pentaerythritol tetranitrate (PTN) group, morphine associated with GTN group, morphine associated with ISDN group and morphine associated with PTN group. Basal pressure of Oddi's sphincter (BPOS), amplitude of phasic contractions (SOCA), frequency of phasic contractions (SOF), duration of phasic contractions (SOD), duodenal pressure (DP) and common bile duct pressure (CBDP) were scored and analyzed. Morphine was given intramuscularly while nitroester drugs were applied sublingually.RESULTS: BPOS and SOCA decreased significantly after administration of ISDN and GTN, BPOS reduced from 10.95±7.49 mmHg to 5.92±4.04 mmHg (P＜0.05) evidently after application of PTN. BPOS increased from 7.37±5.58mmHg to 16.60±13.87 mmHg, SOCA increased from 54.09±38.37 mmHg to 100.70±43.51 mmHg, SOF increased from 7.15±3.20 mmHg to 10.38±2.93 mmHg and CBDP increased 3.75±1.95 mmHg to 10.49±8.21 mmHg (P＜0.01)evidently after injection of morphine. After associated application of ISDN and GTN, the four indications above decreased obviously. As for application associated with PTN,SOCA and SOF decreased separately from 100.64±44.99mmHg to 66.17±35.88 mmHg and from 10.70±2.76 mmHg to 9.04±1.71 mmHg (P＜0.05) markedly.CONCLUSION: The regular dose of GTN, ISDN and PTN showed inhibitory effect on SO motility, morphine showed excitatory effect on SO while GTN, ISDN and PTN could antagonize the effect of morphine. Among the three nitroester drugs, the effect of ISDN on SO was most significant.
基金the National Natural Science Foundation of China(No.20573098)the Foundation of Key Laboratory of Science and Technology for National Defence of Propellant and Explosive of China(No.9140C3503020605).
文摘The thermal decomposition behavior and nonisothermal reaction kinetics of the double-base gun propellants containing the mixed ester of triethyleneglycol dinitrate（TEGDN） and nitroglycerin（NG） were investigated by thermogravimetry（TG） and differential thermogravimetry（DTG）, and differential scanning calorimetry（DSC） under the high-pressure dynamic ambience. The results show that the thermal decomposition processes of the mixed nitric ester gun propellants have two mass-loss stages. Nitric ester evaporates and decomposes in the first stage, and nitrocellulose and centralite II（C2） decompose in the second stage. The mass loss, the DTG peak points, and the terminated temperatures of the two stages are changeable with the difference of the mass ratio of TEGDN to NG. There is only one obvious exothermic peak in the DSC curves under the different pressures. With the increase in the furnace pressure, the peak temperature decreases, and the decomposition heat increases. With the increase in the content of TEGDN, the decomposition heat decreases at 0.1 MPa and rises at high pressure. The variety of mass ratio of TEGDN to NG makes few effect on the exothermic peak temperatures in the DSC curves at different pressures. The kinetic equation of the main exothermal decomposition reaction of the gun propellant TG0601 was determined as： dα/dt=1021.59（1-α）3e-2.60×104/T. The reaction mechanism of the process can be classified as chemical reaction. The critical temperatures of the thermal explosion（Tbe and Tbp） obtained from the onset temperature（Te） and the peak temperature（Tp） are 456.46 and 473.40 K, respectively. ΔS≠, ΔH≠, and ΔG≠ of the decomposition reaction are 163.57 J·mol^-1·K^-1, 209.54 kJ·mol^-1, and 133.55 kJ·mol^-1, respectively.
文摘36 cases of coronary heart disease with silent myocardial ischemia (SMI) were treated sequentially with Tong Xin Luo (TXL) capsule and isosorbide dinitrate in random order. The results showed that both drugs were effective in decreasing episodes of SMI and shortening the duration of asymptomatic myocardial ischemia. TXL, however, was found with a better action and was superior to isosorbide dinitrate. It was also found that TXL could improve diastolic function of the left ventricle as well.
