A new compound (1) named as winchic acid and eight known ones were isolated from the stem barks of Winchia colophylla A. DC. (collected in Xishuangbanna, Yunnan Province of China). The new compound 1 was identified as...A new compound (1) named as winchic acid and eight known ones were isolated from the stem barks of Winchia colophylla A. DC. (collected in Xishuangbanna, Yunnan Province of China). The new compound 1 was identified as 3beta-hydroxy-27-(4-hydroxy-3-methoxy-E-cinnamoyloxy)-lup-20(29)-en-28-oic acid on the basis of 1D and 2D NMR experiments. The eight known compounds were determined to be lupenone, lupenyl acetate, betulinic acid, alpha-amyrin acetate, ursolic acid, ptiloepoxide, beta-amyrin and cycloeucalenol, respectively.展开更多
A novel floating osmotic pump controlled release system （FOP） and traditional matrix sustained release tablets （MT） of dipyridamole （DIP） were characterized in terms of pharmacokinetics, drug release, and in vit...A novel floating osmotic pump controlled release system （FOP） and traditional matrix sustained release tablets （MT） of dipyridamole （DIP） were characterized in terms of pharmacokinetics, drug release, and in vitro-in vivo correlation. In vivo study was performed by a three-crossover study in six beagle dogs relative to the conventional tablet （CT）. A HPLC method for the determination of DIP in the plasma was developed. Cumulative percent of absorption fraction was compared to that of in vitro cumulative release. Both FOP and MT displayed obvious extended release characteristic in vivo while FOP showed a better extended release behavior. The bioavailability of FOP was higher than that of MT and a zero-order release linear correlation of DIP between fraction absorbed in vivo and fraction dissolved in vitro was established for FOP while not for MT. The results indicated the existence of an absorption window in upper part of the GI track of DIP, which meant that floating system could be excellent for the drug delivery. In addition, the in vitro model was a good choice for depicting in vivo absorption and for optimization of the formulation of FOP if it is needed to be bio-equivalent to MT.展开更多
Chandrasekran-paul (1982) made an equation of drug release from matrix system as follows:In this paper a simplified expression has been deduced from it within ordinary range of experimental time and with appropriate v...Chandrasekran-paul (1982) made an equation of drug release from matrix system as follows:In this paper a simplified expression has been deduced from it within ordinary range of experimental time and with appropriate values of K. The cumulative amount of drug release may vary in directproportion to the square root of time with an intercept,that is,The release behaviour of both nifedipine patch and propranolol patch has fit the expression with good correlation coefficient.The re0lease data of hydrocortisone creams (Shah,1989)also can be described by the same expression.Compared with Higuchi’s equation,the presence of the intercept,A〃,may be relative to drug dissolution characteristics展开更多
Background Rotational atherectomy （RA） could facilitate the percutaneous coronary intervention （PCI） in heavily coronary calcified patients. The effectiveness and safety of this technique needs to be further evalu...Background Rotational atherectomy （RA） could facilitate the percutaneous coronary intervention （PCI） in heavily coronary calcified patients. The effectiveness and safety of this technique needs to be further evaluated. Methods ＆ Results Eighty patients who underwent RA in our center from September 2011 to June 2014 were enrolled. The mean age was 72.4 ± 10.4 years. The left ventricular ejection frac- tion （LVEF） was average 52.3% ± 8.48% and the estimated glomerular filtration rate was 73.2 ± 3.20 mL/min per 1.73 m2. The coronary lesions were complex, with Syntax score 29.5 ± 9.86. The diameter of reference vessel was 3.4 ± 0.45 mm and the average diameter stenosis of target vessels was 80% ~ 10%. All the patients were deployed with drug eluting stents （DES） successfully aiter RA. The patients were followed up for 12-18 months. Kaplan-Meier plots estimated the survival rate was 93.4% and the cumulative incidence of major adverse cardiac and cerebral events （MACCE） was 25.4%. Bleeding and procedural-related complications were quite low. COX proportional hazards model for multivariate analysis demonstrated that diabetes, LVEF and maximum pressure of postdilatation were the predictors of MACCE. Conclusions RA followed by implantation of DES was effective and safe for heavily coronary calcified patients. Diabetes, LVEF and maximum pressure ofpostdilatation were predictive for MACCE.展开更多
Background The benefit/risk ratio of stenting in acute ST-segment elevation myocardial infarction （STEMI） patients with single vessel intermediate stenosis culprit lesions merits further study, therefore the subject...Background The benefit/risk ratio of stenting in acute ST-segment elevation myocardial infarction （STEMI） patients with single vessel intermediate stenosis culprit lesions merits further study, therefore the subject of the present study. Methods and results It was a pro- spective, multicenter, randomized controlled trial. Between April 2012 and July 2015, 399 acute STEMI patients with single vessel disease and intermediate （40%-70%） stenosis of the culprit lesion before or after aspiration thrombectomy and/or intracoronary tirofiban （15 pg/kg） were enrolled and were randomly assigned （h 1） to stenting group （n = 201） and non-stenting group （n = 198）. In stenting group, patients received pharmacologic therapy plus standard percutaneous coronary intervention （PCI） with stent implantation. In non-stenting group, pa- tients received pharmacologic therapy and PCI （thrombectomy）, but without dilatation or stenting. Primary endpoint was 12-month rate of major adverse cardiac and eerebrovascular events （MACCE）, a composite of cardiac death, non-fatal myocardial infarction （M1）, repeat re- vascularization and stroke. Secondary endpoints were 12-month rates of all cause death, ischemia driven admission and bleeding complica- tion. Median follow-up time was 12.4 ~ 3.1 months. At 12 months, MACCE occurred in 8.0% of the patients in stenting group, as compared with 15.2% in the non-stenting group （adjusted HR： 0.42, 95% Ch 0.19-0.89, P = 0.02）. The stenting group had lower non-fatal MI rate than non-stenting group, （1.5% vs. 5.5%, P = 0.03）. The two groups shared similar cardiac death, repeat revascularization, stroke, all cause death, ischemia driven readmission and bleeding rates at 12 months. Conclusions Stent implantation had better efficacy and safety in reducing MACCE risks among acute STEMI patients with single vessel intermediate stenosis culprit lesions.展开更多
Objective To compare the short- and long-term clinical outcomes between sirolimus-eluting stent （ Cypher stent） and paclitaxel-eluting stent （TAXUS stent） in patients with in-stent restenosis （ISR） lesions of th...Objective To compare the short- and long-term clinical outcomes between sirolimus-eluting stent （ Cypher stent） and paclitaxel-eluting stent （TAXUS stent） in patients with in-stent restenosis （ISR） lesions of the coronary arteries. Methods From December 2002 to March 2005, 253 patients with ISR lesions of the coronary arteries were selected and divided into two groups. Cypher group （152 cases） was treated with Cypher or Cypher Select stents, and TAXUS group （101 cases） with TAXUS stents. A total of 262 ISR lesions in these patients were treated with 308 drog-eluring stents （DESs）, including 176 Cypher or Cypher Select stents and 132 TAXUS stents. All patients were followed up for 10 months. Procedure success rates of DES implantation in both groups were observed. Major adverse cardiac events （MACE） rates in hospital and at 10 months follow-up, as well as in-DES restenosis observed using coronary angiography at follow-up were compared between two groups. Results Success rate of DES implantation was 100% in both groups. No significant difference in MACE rate during hospitalization was found between the two groups. However, at 10 months follow-up, MACE rate was higher in TAXUS group than in Cypher group （ 16.00% vs. 6.67%, P =0. 031 ）. As for coronary angiography at 10 months follow-up, we observed an increasing tendency of in-DES restenosis rate in TAXUS group compared with Cypher group （29.41% vs. 14.04%, P=0.075）. Conclusions Cypher and TAXUS DESs both have good short- and long-term outcomes in treating ISR. Cypher DES proved better long-term clinical outcome than TAXUS DES.展开更多
Background Although radial access for drug-eluting stent （DES） combined with rotational atherectomy （RA） in patients with calcified coronary lesions may be associated with a lower risk of major bleeding complicati...Background Although radial access for drug-eluting stent （DES） combined with rotational atherectomy （RA） in patients with calcified coronary lesions may be associated with a lower risk of major bleeding complications and obtain favorable clinical results compared with femoral access, the long-term outcome data of this approach were limited in contemporary DES era. Methods ＆ Results This retrospective study sought to compare in-hospital and long-term outcomes for patients undergoing RA via the transradial （TR） and transfemoral （TF） route in 126 consecutive patients （59 radial, 67 femoral） from 2009 to 2014. TR RA procedures were performed in 44/62 （71%） by the three TR operators, compared with 15/64 （23%） by the four TF operators in the present study. Significantly smaller diameter guide catheters and burrs （1.39 ± 0.16 mm vs. 1.53 ± 0.24 mm, P = 0.001） were used in the TR group. Procedural success rates were similar in both TR and TF groups. There was a significantly less major access site bleeding complications in favor of radial artery access （2% vs. 16%, P = 0.012）. The incidence of in-hospital death or myocardial infarction was low in both groups. Although a trend of lower adverse event rate was demonstrated in the TR group compared with the TF one, no statistical significance （21% vs. 27%, P = 0.135） was detected. Conclusions Radial access, a useful alternative to femoral access for RA and DES, can be safely and successfully performed on up to 71% of the patients with heavily calcified coronary lesions needing RA by experienced TR operators.展开更多
Objective Study of bupropion hydrochloride gel matrix sustained release tablet and the preparation method, test the skeleton material of hydroxypropyl methyl cellulose influencing drug release for evaluation, explore ...Objective Study of bupropion hydrochloride gel matrix sustained release tablet and the preparation method, test the skeleton material of hydroxypropyl methyl cellulose influencing drug release for evaluation, explore the preparation of sustained release tablets of optimization method. Method With hydroxypropyl methyl cellulose as skeleton material, according to the different prescription preparation of bupmpion hydrochloride sustained release tablets. Different HPMC viscosity, Consumption, particle size, compression pressure and slurry rotational speed and other factors, analysis the influence on drug release rate.Through the release of test evaluation of sustained release effect, and the preliminary study on the drug release characteristic. With hydroxypropyl methyl cellulose （ HPMC ） as skeleton material, with citric acid citrate as a porogenic agent, direct powder tabletting method of bupropion hydrochloride sustained release tablets; by using single factor and orthogonal experiment method to investigate HPMC different viscosity, different Consumption, different particle size, different compression pressure, different pulp rotational speed and other factors on the release of delivery rate. Result Select HPMC-K100M for bupropion hydrochloride sustained release tablets of the skeleton materials; reinforcing materials of high viscosity HPMC K100M and main drug quality ratio of 1： 1; HPMC particle diameter of 125p m, make use of these conditions to preparation of bupropion hydrochloride sustained release tablets for optimal prescription conditions. Conclusion bupropion hydroehloride sustained release tablets on the drug release rate is mainly affected by HPMC viscosity and dosage effect. Along with the tablet of HPMC viscosity increased, the drug is released slowly. HPMC viscosity, dosage on the drug release rate has significant influence.展开更多
In-stent thrombosis after cessation of antiplatelet medications in patients with drug-eluting stents （DES） is a significant problem in medical practice, particularly in the perioperative period. We report a case of ...In-stent thrombosis after cessation of antiplatelet medications in patients with drug-eluting stents （DES） is a significant problem in medical practice, particularly in the perioperative period. We report a case of an 87-year-old man with a medical history of hypertension, coronary artery disease and chronic atrophic gastritis. Very late thrombosis of a sirolimus-eluting stent occurred 1207 days after implantation, seven months after discontinuation of clopidogrel, and the interruption of aspirin 13 days in preparation of an elective endoscopic gastroin-testinal procedure presented with acute myocardial infarction. The patient was treated with thrombectomy and successfully revascularized with superimposition of two sirolimus-eluting stents. Medications administered in the catheterization laboratory included low molecular weight heparin and nitroglycerin. Flow was defined as grade 2 according to the thrombolysis in myocardial infarction scale. Electrocardio-gram after the procedure revealed persistent, but decreased, ST-segment elevation in the anterolateral leads. The patient recovered and was discharged on aspirin and clopidogrel indefinitely. There was no cardiac event during the two year follow-up period. This case underlines the importance of maintaining the balance of thrombosis and bleeding during perioperation of non-cardiac procedure and the possible need for continuation of aspirin therapy during periendoscopic procedures among patients with low bleeding risks who received DES.展开更多
文摘A new compound (1) named as winchic acid and eight known ones were isolated from the stem barks of Winchia colophylla A. DC. (collected in Xishuangbanna, Yunnan Province of China). The new compound 1 was identified as 3beta-hydroxy-27-(4-hydroxy-3-methoxy-E-cinnamoyloxy)-lup-20(29)-en-28-oic acid on the basis of 1D and 2D NMR experiments. The eight known compounds were determined to be lupenone, lupenyl acetate, betulinic acid, alpha-amyrin acetate, ursolic acid, ptiloepoxide, beta-amyrin and cycloeucalenol, respectively.
文摘A novel floating osmotic pump controlled release system （FOP） and traditional matrix sustained release tablets （MT） of dipyridamole （DIP） were characterized in terms of pharmacokinetics, drug release, and in vitro-in vivo correlation. In vivo study was performed by a three-crossover study in six beagle dogs relative to the conventional tablet （CT）. A HPLC method for the determination of DIP in the plasma was developed. Cumulative percent of absorption fraction was compared to that of in vitro cumulative release. Both FOP and MT displayed obvious extended release characteristic in vivo while FOP showed a better extended release behavior. The bioavailability of FOP was higher than that of MT and a zero-order release linear correlation of DIP between fraction absorbed in vivo and fraction dissolved in vitro was established for FOP while not for MT. The results indicated the existence of an absorption window in upper part of the GI track of DIP, which meant that floating system could be excellent for the drug delivery. In addition, the in vitro model was a good choice for depicting in vivo absorption and for optimization of the formulation of FOP if it is needed to be bio-equivalent to MT.
文摘Chandrasekran-paul (1982) made an equation of drug release from matrix system as follows:In this paper a simplified expression has been deduced from it within ordinary range of experimental time and with appropriate values of K. The cumulative amount of drug release may vary in directproportion to the square root of time with an intercept,that is,The release behaviour of both nifedipine patch and propranolol patch has fit the expression with good correlation coefficient.The re0lease data of hydrocortisone creams (Shah,1989)also can be described by the same expression.Compared with Higuchi’s equation,the presence of the intercept,A〃,may be relative to drug dissolution characteristics
文摘Background Rotational atherectomy （RA） could facilitate the percutaneous coronary intervention （PCI） in heavily coronary calcified patients. The effectiveness and safety of this technique needs to be further evaluated. Methods ＆ Results Eighty patients who underwent RA in our center from September 2011 to June 2014 were enrolled. The mean age was 72.4 ± 10.4 years. The left ventricular ejection frac- tion （LVEF） was average 52.3% ± 8.48% and the estimated glomerular filtration rate was 73.2 ± 3.20 mL/min per 1.73 m2. The coronary lesions were complex, with Syntax score 29.5 ± 9.86. The diameter of reference vessel was 3.4 ± 0.45 mm and the average diameter stenosis of target vessels was 80% ~ 10%. All the patients were deployed with drug eluting stents （DES） successfully aiter RA. The patients were followed up for 12-18 months. Kaplan-Meier plots estimated the survival rate was 93.4% and the cumulative incidence of major adverse cardiac and cerebral events （MACCE） was 25.4%. Bleeding and procedural-related complications were quite low. COX proportional hazards model for multivariate analysis demonstrated that diabetes, LVEF and maximum pressure of postdilatation were the predictors of MACCE. Conclusions RA followed by implantation of DES was effective and safe for heavily coronary calcified patients. Diabetes, LVEF and maximum pressure ofpostdilatation were predictive for MACCE.
文摘Background The benefit/risk ratio of stenting in acute ST-segment elevation myocardial infarction （STEMI） patients with single vessel intermediate stenosis culprit lesions merits further study, therefore the subject of the present study. Methods and results It was a pro- spective, multicenter, randomized controlled trial. Between April 2012 and July 2015, 399 acute STEMI patients with single vessel disease and intermediate （40%-70%） stenosis of the culprit lesion before or after aspiration thrombectomy and/or intracoronary tirofiban （15 pg/kg） were enrolled and were randomly assigned （h 1） to stenting group （n = 201） and non-stenting group （n = 198）. In stenting group, patients received pharmacologic therapy plus standard percutaneous coronary intervention （PCI） with stent implantation. In non-stenting group, pa- tients received pharmacologic therapy and PCI （thrombectomy）, but without dilatation or stenting. Primary endpoint was 12-month rate of major adverse cardiac and eerebrovascular events （MACCE）, a composite of cardiac death, non-fatal myocardial infarction （M1）, repeat re- vascularization and stroke. Secondary endpoints were 12-month rates of all cause death, ischemia driven admission and bleeding complica- tion. Median follow-up time was 12.4 ~ 3.1 months. At 12 months, MACCE occurred in 8.0% of the patients in stenting group, as compared with 15.2% in the non-stenting group （adjusted HR： 0.42, 95% Ch 0.19-0.89, P = 0.02）. The stenting group had lower non-fatal MI rate than non-stenting group, （1.5% vs. 5.5%, P = 0.03）. The two groups shared similar cardiac death, repeat revascularization, stroke, all cause death, ischemia driven readmission and bleeding rates at 12 months. Conclusions Stent implantation had better efficacy and safety in reducing MACCE risks among acute STEMI patients with single vessel intermediate stenosis culprit lesions.
文摘Objective To compare the short- and long-term clinical outcomes between sirolimus-eluting stent （ Cypher stent） and paclitaxel-eluting stent （TAXUS stent） in patients with in-stent restenosis （ISR） lesions of the coronary arteries. Methods From December 2002 to March 2005, 253 patients with ISR lesions of the coronary arteries were selected and divided into two groups. Cypher group （152 cases） was treated with Cypher or Cypher Select stents, and TAXUS group （101 cases） with TAXUS stents. A total of 262 ISR lesions in these patients were treated with 308 drog-eluring stents （DESs）, including 176 Cypher or Cypher Select stents and 132 TAXUS stents. All patients were followed up for 10 months. Procedure success rates of DES implantation in both groups were observed. Major adverse cardiac events （MACE） rates in hospital and at 10 months follow-up, as well as in-DES restenosis observed using coronary angiography at follow-up were compared between two groups. Results Success rate of DES implantation was 100% in both groups. No significant difference in MACE rate during hospitalization was found between the two groups. However, at 10 months follow-up, MACE rate was higher in TAXUS group than in Cypher group （ 16.00% vs. 6.67%, P =0. 031 ）. As for coronary angiography at 10 months follow-up, we observed an increasing tendency of in-DES restenosis rate in TAXUS group compared with Cypher group （29.41% vs. 14.04%, P=0.075）. Conclusions Cypher and TAXUS DESs both have good short- and long-term outcomes in treating ISR. Cypher DES proved better long-term clinical outcome than TAXUS DES.
文摘Background Although radial access for drug-eluting stent （DES） combined with rotational atherectomy （RA） in patients with calcified coronary lesions may be associated with a lower risk of major bleeding complications and obtain favorable clinical results compared with femoral access, the long-term outcome data of this approach were limited in contemporary DES era. Methods ＆ Results This retrospective study sought to compare in-hospital and long-term outcomes for patients undergoing RA via the transradial （TR） and transfemoral （TF） route in 126 consecutive patients （59 radial, 67 femoral） from 2009 to 2014. TR RA procedures were performed in 44/62 （71%） by the three TR operators, compared with 15/64 （23%） by the four TF operators in the present study. Significantly smaller diameter guide catheters and burrs （1.39 ± 0.16 mm vs. 1.53 ± 0.24 mm, P = 0.001） were used in the TR group. Procedural success rates were similar in both TR and TF groups. There was a significantly less major access site bleeding complications in favor of radial artery access （2% vs. 16%, P = 0.012）. The incidence of in-hospital death or myocardial infarction was low in both groups. Although a trend of lower adverse event rate was demonstrated in the TR group compared with the TF one, no statistical significance （21% vs. 27%, P = 0.135） was detected. Conclusions Radial access, a useful alternative to femoral access for RA and DES, can be safely and successfully performed on up to 71% of the patients with heavily calcified coronary lesions needing RA by experienced TR operators.
文摘Objective Study of bupropion hydrochloride gel matrix sustained release tablet and the preparation method, test the skeleton material of hydroxypropyl methyl cellulose influencing drug release for evaluation, explore the preparation of sustained release tablets of optimization method. Method With hydroxypropyl methyl cellulose as skeleton material, according to the different prescription preparation of bupmpion hydrochloride sustained release tablets. Different HPMC viscosity, Consumption, particle size, compression pressure and slurry rotational speed and other factors, analysis the influence on drug release rate.Through the release of test evaluation of sustained release effect, and the preliminary study on the drug release characteristic. With hydroxypropyl methyl cellulose （ HPMC ） as skeleton material, with citric acid citrate as a porogenic agent, direct powder tabletting method of bupropion hydrochloride sustained release tablets; by using single factor and orthogonal experiment method to investigate HPMC different viscosity, different Consumption, different particle size, different compression pressure, different pulp rotational speed and other factors on the release of delivery rate. Result Select HPMC-K100M for bupropion hydrochloride sustained release tablets of the skeleton materials; reinforcing materials of high viscosity HPMC K100M and main drug quality ratio of 1： 1; HPMC particle diameter of 125p m, make use of these conditions to preparation of bupropion hydrochloride sustained release tablets for optimal prescription conditions. Conclusion bupropion hydroehloride sustained release tablets on the drug release rate is mainly affected by HPMC viscosity and dosage effect. Along with the tablet of HPMC viscosity increased, the drug is released slowly. HPMC viscosity, dosage on the drug release rate has significant influence.
文摘In-stent thrombosis after cessation of antiplatelet medications in patients with drug-eluting stents （DES） is a significant problem in medical practice, particularly in the perioperative period. We report a case of an 87-year-old man with a medical history of hypertension, coronary artery disease and chronic atrophic gastritis. Very late thrombosis of a sirolimus-eluting stent occurred 1207 days after implantation, seven months after discontinuation of clopidogrel, and the interruption of aspirin 13 days in preparation of an elective endoscopic gastroin-testinal procedure presented with acute myocardial infarction. The patient was treated with thrombectomy and successfully revascularized with superimposition of two sirolimus-eluting stents. Medications administered in the catheterization laboratory included low molecular weight heparin and nitroglycerin. Flow was defined as grade 2 according to the thrombolysis in myocardial infarction scale. Electrocardio-gram after the procedure revealed persistent, but decreased, ST-segment elevation in the anterolateral leads. The patient recovered and was discharged on aspirin and clopidogrel indefinitely. There was no cardiac event during the two year follow-up period. This case underlines the importance of maintaining the balance of thrombosis and bleeding during perioperation of non-cardiac procedure and the possible need for continuation of aspirin therapy during periendoscopic procedures among patients with low bleeding risks who received DES.
