An improved and reliable ultra-performance liquid chromatography/tandem mass spectrometry (UPLC- MS/MS) method has been developed and validated for the determination of lercanidipine in human plasma. Plasma samples ...An improved and reliable ultra-performance liquid chromatography/tandem mass spectrometry (UPLC- MS/MS) method has been developed and validated for the determination of lercanidipine in human plasma. Plasma samples with lercanidipine-d3 as an internal standard (IS) were prepared by solid phase extraction on Phenomenex Strata-X cartridges using 100 μL of human plasma. Chromatographic analysis was performed on UPLC BEH C18 (50 mm × 2.1 mm, 1.7 μm) column under isocratic conditions. Linear calibration curves were obtained over a wide dynamic concentration range of 0.010-20.0 ng/mL. Matrix effect was assessed by post-column infusion, post-extraction spiking and standard-line slope methods. The mean extraction recovery was 〉 94% for the analyte and IS. Inter-batch and intra-hatch precision (% CV) across five quality controls was 〈 5.8%. Bioequivalence study was performed with 36 healthy sub- jects after oral administration of 10 mg of lercanidipine and the assay reproducibility was evaluated by reanalysis of 133 incurred samples.展开更多
AIM: To undertake a review of the evidence that nifedipine GITS and lercanidipine are therapeutically equivalent in the management of essential hypertension.METHODS: A systematic review of the published literature was...AIM: To undertake a review of the evidence that nifedipine GITS and lercanidipine are therapeutically equivalent in the management of essential hypertension.METHODS: A systematic review of the published literature was prompted by the findings of two meta-analyses which indicated that there was a lower incidence of peripheral(ankle) oedema with lercanidipine. However,neither meta-analysis gave detailed attention to comparative antihypertensive efficacy or cardiovascular protection. Accordingly,a systematic,detailed and critical review was undertaken of individual published papers. The review started with those studies incorporated into the 2 meta-analyses and then all other salient and directly relevant papers identified through the following search criteria: all randomized controlled trials in which the therapeutic profile and antihypertensive effects of lercanidipine were directly compared with those of nifedipine GITS(in hypertensive patients). The searchstrategy was focused on the reports of clinical trials of lercanidipine vs nifedipine GITS,which were identified through a systematic search of PubMed(from 1966 to October 2012),Embase(from 1980 to October 2012) and the Cochrane library(from 1 October 2008 to end October 2013). The search combined terms related to lercanidipine vs nifedipine GITS(including MeSH search using calcium antagonists,calcium channel blockers and dihydropyridines).RESULTS: With regard to blood pressure(BP) control and the consistency of BP control throughout 24-h,there is limited published evidence. However,two studies using 24 h ambulatory blood pressure monitoring clearly identified the dose-dependency of BP lowering with lercanidipine and its variably sustained 24-h efficacy. In contrast,there is evidence of a consistent antihypertensive effect throughout 24 h with nifedipine GITS. The incidence of the most common "side effect",i.e.,peripheral(ankle) oedema can be estimated as follows. For every 100 patients treated with lercanidipine,2.5 will report oedema compared to 6 patients treated with nifedipine GITS. However,98 or 99 patients will continue treatment with nifedipine GITS,compared with 99.5 patients on lercanidipine. Finally,with regard to outcome studies of cardiovascular(CV) morbidity and mortality,there is definitive outcome evidence for nifedipine GITS but there is no evidence that treatment with lercanidipine leads to reductions in CV morbidity and mortality.CONCLUSION: There is no evidence in terms of longterm BP control and CV protection to justify the contention that lercanidipine is therapeutically equivalent to nifedipine GITS.展开更多
Background Combination therapy is an effective method to reduce the blood pressure (BP) for patients with hypertension.This study was performed to evaluate the efficacy and safety of benazepril/lercanidipine compare...Background Combination therapy is an effective method to reduce the blood pressure (BP) for patients with hypertension.This study was performed to evaluate the efficacy and safety of benazepril/lercanidipine compared with benazepril alone in patients with mild-to-moderate hypertension.Methods One hundred and eighty-one patients with mild-to-moderate primary hypertension were assigned in this randomized,single-blind,parallel-group study and were randomly divided into group A (benazepril 10 mg/lercanidipine 10 mg) and group B (benazepril 10 mg) for 8 weeks.At 4 weeks,the dosage of Benazepril was titrated up to 20 mg if the diastolic blood pressure (DBP) remained ≥90 mmHg.BP control and side effects were evaluated at the end of 1,4 and 8 weeks.Results The baseline characteristics of the two groups were similar.The BP in both groups decreased from the baseline (P 〈0.05).At the end of 4 and 8 weeks,Benazepril/Lercanidipine produced greater BP reduction than Benazepril alone (P 〈0.05).The comparison of the rate of BP control for the benazepril/lercanidipine and benazepril groups at the end of 1,4,and 8 weeks were 41.2% vs.37.6% (P 〉0.05),67.1% vs.44.7% (P 〈0.05),and 71.8% vs.45.9% (P 〈0.05).There was no significant difference of side effects between the two groups.Conclusion The benazepril/lercanidipine combination is more effective in reducing BP than benazepril alone,while it does not increase the incidence of side effects.展开更多
基金UGC-BSR (F 4-1/2009 (BSR)/7-74/2007)New Delhi, for research fellowship, F 4-1/2009 (BSR)/7-74/2007Department of Chemistry, Gujarat University, for supporting this work
文摘An improved and reliable ultra-performance liquid chromatography/tandem mass spectrometry (UPLC- MS/MS) method has been developed and validated for the determination of lercanidipine in human plasma. Plasma samples with lercanidipine-d3 as an internal standard (IS) were prepared by solid phase extraction on Phenomenex Strata-X cartridges using 100 μL of human plasma. Chromatographic analysis was performed on UPLC BEH C18 (50 mm × 2.1 mm, 1.7 μm) column under isocratic conditions. Linear calibration curves were obtained over a wide dynamic concentration range of 0.010-20.0 ng/mL. Matrix effect was assessed by post-column infusion, post-extraction spiking and standard-line slope methods. The mean extraction recovery was 〉 94% for the analyte and IS. Inter-batch and intra-hatch precision (% CV) across five quality controls was 〈 5.8%. Bioequivalence study was performed with 36 healthy sub- jects after oral administration of 10 mg of lercanidipine and the assay reproducibility was evaluated by reanalysis of 133 incurred samples.
文摘AIM: To undertake a review of the evidence that nifedipine GITS and lercanidipine are therapeutically equivalent in the management of essential hypertension.METHODS: A systematic review of the published literature was prompted by the findings of two meta-analyses which indicated that there was a lower incidence of peripheral(ankle) oedema with lercanidipine. However,neither meta-analysis gave detailed attention to comparative antihypertensive efficacy or cardiovascular protection. Accordingly,a systematic,detailed and critical review was undertaken of individual published papers. The review started with those studies incorporated into the 2 meta-analyses and then all other salient and directly relevant papers identified through the following search criteria: all randomized controlled trials in which the therapeutic profile and antihypertensive effects of lercanidipine were directly compared with those of nifedipine GITS(in hypertensive patients). The searchstrategy was focused on the reports of clinical trials of lercanidipine vs nifedipine GITS,which were identified through a systematic search of PubMed(from 1966 to October 2012),Embase(from 1980 to October 2012) and the Cochrane library(from 1 October 2008 to end October 2013). The search combined terms related to lercanidipine vs nifedipine GITS(including MeSH search using calcium antagonists,calcium channel blockers and dihydropyridines).RESULTS: With regard to blood pressure(BP) control and the consistency of BP control throughout 24-h,there is limited published evidence. However,two studies using 24 h ambulatory blood pressure monitoring clearly identified the dose-dependency of BP lowering with lercanidipine and its variably sustained 24-h efficacy. In contrast,there is evidence of a consistent antihypertensive effect throughout 24 h with nifedipine GITS. The incidence of the most common "side effect",i.e.,peripheral(ankle) oedema can be estimated as follows. For every 100 patients treated with lercanidipine,2.5 will report oedema compared to 6 patients treated with nifedipine GITS. However,98 or 99 patients will continue treatment with nifedipine GITS,compared with 99.5 patients on lercanidipine. Finally,with regard to outcome studies of cardiovascular(CV) morbidity and mortality,there is definitive outcome evidence for nifedipine GITS but there is no evidence that treatment with lercanidipine leads to reductions in CV morbidity and mortality.CONCLUSION: There is no evidence in terms of longterm BP control and CV protection to justify the contention that lercanidipine is therapeutically equivalent to nifedipine GITS.
文摘Background Combination therapy is an effective method to reduce the blood pressure (BP) for patients with hypertension.This study was performed to evaluate the efficacy and safety of benazepril/lercanidipine compared with benazepril alone in patients with mild-to-moderate hypertension.Methods One hundred and eighty-one patients with mild-to-moderate primary hypertension were assigned in this randomized,single-blind,parallel-group study and were randomly divided into group A (benazepril 10 mg/lercanidipine 10 mg) and group B (benazepril 10 mg) for 8 weeks.At 4 weeks,the dosage of Benazepril was titrated up to 20 mg if the diastolic blood pressure (DBP) remained ≥90 mmHg.BP control and side effects were evaluated at the end of 1,4 and 8 weeks.Results The baseline characteristics of the two groups were similar.The BP in both groups decreased from the baseline (P 〈0.05).At the end of 4 and 8 weeks,Benazepril/Lercanidipine produced greater BP reduction than Benazepril alone (P 〈0.05).The comparison of the rate of BP control for the benazepril/lercanidipine and benazepril groups at the end of 1,4,and 8 weeks were 41.2% vs.37.6% (P 〉0.05),67.1% vs.44.7% (P 〈0.05),and 71.8% vs.45.9% (P 〈0.05).There was no significant difference of side effects between the two groups.Conclusion The benazepril/lercanidipine combination is more effective in reducing BP than benazepril alone,while it does not increase the incidence of side effects.