更新于：2024-12-11
Levamlodipine Besylate
苯磺酸左旋氨氯地平
更新于：2024-12-11
概要
基本信息
非在研机构 |
最高研发阶段批准上市 |
最高研发阶段(中国)批准上市 |
特殊审评- |
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结构
分子式C26H31ClN2O8S |
InChIKeyZPBWCRDSRKPIDG-LMOVPXPDSA-N |
CAS号150566-71-5 |
关联
59
项与 苯磺酸左旋氨氯地平 相关的临床试验健康受试者空腹和餐后状态下单次口服苯磺酸左氨氯地平片（2.5mg）单中心的随机、开放、两制剂、两周期、两序列、双交叉设计的生物等效性试验
苯磺酸左氨氯地平片在中国健康成年受试者中的一项单中心、随机、开放、空腹和餐后、单次给药、两制剂、两序列、两周期交叉的生物等效性研究
苯磺酸左氨氯地平片在中国健康受试者中单中心、随机、开放、单剂量、两制
剂、两周期、两序列、双交叉、空腹/餐后状态下生物等效性试验
100 项与 苯磺酸左旋氨氯地平 相关的临床结果
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100 项与 苯磺酸左旋氨氯地平 相关的转化医学
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100 项与 苯磺酸左旋氨氯地平 相关的专利（医药）
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12
项与 苯磺酸左旋氨氯地平 相关的文献（医药）2020-12-01BMC pharmacology & toxicology4区 · 医学
Bioequivalence of levamlodipine besylate tablets in healthy Chinese subjects: a single-dose and two-period crossover randomized study
4区 · 医学
ArticleOA
作者: Tao, Ye ; Liu, Yanping ; Liu, Shuqin ; Wang, Chenjing ; Ma, Yaping ; Cao, Yu ; Li, Xin ; Gao, Xiaomeng ; Li, Ting
Abstract:
Background:
Levamlodipine, a calcium channel blocker, has been show act as a cardiovascular drug. To compare the pharmacokinetic parameters between levamlodipine (test formulation) at a single dose of 5 mg and amlodipine (reference formulation) at a single dose of 10 mg, the bioequivalence study was carried out.
Methods:
A single-dose randomized, open-label, two-period crossover study was designed in healthy Chinese subjects. 48 subjects were divided into fasted and fed groups equally. The subjects randomly received the test or reference formulations at the rate of 1:1. Following a 21-day washout period, the alternative formulations were received. The blood samples were collected at 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 14, 24, 36, 48, 72, 96, 120, 144, 168 h later. Liquid chromatography-tandem mass spectrometry (LC-MS/MS) was applied to determine the plasma concentrations of levamlodipine. Adverse events were recorded.
Results:
The 90% confidence intervals (CIs) of the ratio of geometric means (GMRs) of Cmax, AUC0-t, and AUC0-∞ under both fasted and fed conditions were within the prespecified bioequivalence limits between 80 ~ 125%. Under fasted conditions, 24 subjects were enrolled and completed the study. The mean Cmax was (2.70 ± 0.49) ng/mL, AUC0-t was (141.32 ± 36.24) ng × h/mL and AUC0-∞ was (157.14 ± 45.65) ng × h/mL after a single dose of 5 mg levamlodipine. The mean Cmax was (2.83 ± 0.52) ng/mL, AUC0-t was (153.62 ± 33.96) ng × h/mL and AUC0-∞ was (173.05 ± 41.78) ng × h/mL after a single dose of 10 mg amlodipine. Under fed conditions, 24 subjects were enrolled and completed the study. The mean Cmax was (2.73 ± 0.55) ng/mL, AUC0-t was (166.93 ± 49.96) ng × h/mL and AUC0-∞ was (190.99 ± 70.89) ng × h/mL after a single dose of 5 mg levamlodipine. The mean Cmax was (2.87 ± 0.81) ng/mL AUC0-t was (165.46 ± 43.58) ng × h/mL and AUC0-∞ was (189.51 ± 64.70) ng × h/mL after a single dose of 10 mg amlodipine. Serious adverse event was not observed.
Conclusion:
The trial confirmed that levamlodipine at a single dose of 5 mg and amlodipine at a single dose of 10 mg were bioequivalent under both fasted condition and fed condition.
Trial registration:
Cinicaltrials, NCT04411875. Registered 3 June 2020 - Retrospectively registered
2017-10-01International journal of clinical pharmacology and therapeutics4区 · 医学
Randomized, two-way crossover bioequivalence study of levamlodipine besylate tablets in healthy Chinese subjects
4区 · 医学
Article
作者: Wang, Yu-Lu ; Li, Dan ; Xu, Ping-Sheng ; Li, Xiao-Min ; Li, Dai ; Xu, Su-Mei
OBJECTIVE:
The present bioequivalence study was designed to compare the newly-developed levamlodipine besylate 2.5-mg tablet (test) with that of its 2.5-mg marketed counterpart (reference) in healthy Chinese adult male volunteers.
METHODS:
A single-dose, randomized, open-label, two-period, and two-treatment self-crossover study was conducted in healthy Chinese volunteers after informed consent was obtained. In each part of the study, the subjects were randomly assigned to receive the test or reference product (5 mg levamlodipine) in a 1 : 1 ratio, and then received the alternative product, following a 14-day washout period. Plasma levamlodipine concentrations were analyzed by liquid chromatography-tandem mass spectrometry. Pharmacokinetic parameters (noncompartmental model) were assessed with WinNonlin software. Analysis of variance (ANOVA) and FDA (USA) bioequivalence statistical criterion of 90% CI for 80 - 125% range (set at p ≤ 0.05) of geometric means ratios of test : reference product for Cmax, AUC0-t, and AUC0-∞ were determined. Tolerability was assessed during the entire study period.
RESULTS:
ANOVA indicated that the period, sequence, and formulation had no significant effect on the PK parameters (p ≥ 0.05), although there was a statistically-significant difference between formulations in AUC0-t (p ≤ 0.05). The test formulation was bioequivalent to the marketed formulation as the 90% CI for the ratio of geometric means of Cmax (84.52 - 103.00%), AUC0-t (87.49 - 98.23%), and AUC0-∞ (84.30 - 103.25%) were within equivalence limits (80 - 125%) under fasting condition. No serious adverse events were found among the subjects.
CONCLUSION:
This study confirmed that test and reference levamlodipine besylate tablets were bioequivalent under fasting condition.
.
2016-05-01Hypertension research : official journal of the Japanese Society of Hypertension3区 · 医学
Effects of antihypertensive drugs losartan and levamlodipine besylate on insulin resistance in patients with essential hypertension combined with isolated impaired fasting glucose
3区 · 医学
Article
作者: Wei, Ping ; Liu, Ling ; Jiang, Xue-Shu ; Tan, Ming-Hong ; Xiao, Wei-Yin ; Yi, Dong ; Zhou, Liang ; Ning, Ning
The objective of this study was to observe the antihypertensive effect of losartan and levamlodipine besylate on insulin resistance in patients with essential hypertension (EH) combined with isolated impaired fasting glucose (i-IFG). Patients (n=244) were randomly assigned to losartan potassium tablets (50-100 mg per day) or levamlodipine besylate tablets (2.5-5.0 mg per day) for intensive antihypertensive treatment with no lifestyle interventions for 3 years. The changes in fasting plasma glucose, fasting insulin (FINS) and insulin sensitivity index (ISI) from before to after treatment were observed. Blood pressure (BP) in each group was significantly reduced by treatment (P<0.05). After 12 months of treatment, the FINS level in the losartan potassium group was significantly decreased and ISI was significantly increased compared with before treatment (P<0.05) and compared with the levamlodipine besylate group (P<0.05). After 24 and 36 months of treatment, FINS was significantly decreased and ISI was significantly improved in both groups compared with baseline (P<0.05), and there was no difference between the groups (P>0.05). The incidence of new-onset diabetes mellitus was not significantly different between two groups. The antihypertensive effect of losartan and levamlodipine besylate could amoliorate insulin resistance in patients with EH combined with i-IFG. The improvement of insulin resistance by losartan potassium at 12 months might be better than that by levamlodipine besylate; however, after 24 and 36 months of follow-up, both agents significantly alleviated insulin resistance. These results suggest that the effects of these two drugs on insulin resistance are not significantly different.
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 心绞痛 | 韩国 | 2006-01-01 | |
| 高血压 | 韩国 | 2006-01-01 |
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