IR@PKUHSC  > 北京大学第一临床医学院  > 药剂科
学科主题药剂学
单次和多次口服氟伐他汀钠缓释片与速释胶囊在中国健康人体药代动力学研究
其他题名Study on pharmacokinetics of fluvastatin in healthy subjects after single and multiple doses of porolonged-extended release fluvastatin and immediate-release fluvastatin
赵楠1; 赵侠1; 许俊羽1; 赵蓉1; 崔一民1
关键词氟伐他汀钠缓释片 氟伐他汀钠速释胶囊 药代动力学 安全性 Extended Release Tablet Immediate Release Capsule Pharmacokinetic Safety
刊名中国临床药理学杂志
2014
DOI10.3969/j.issn.1001-6821.2014.08.011
8页:689-692
收录类别中国科技核心期刊 ; 中文核心期刊 ; CSCD
文章类型Journal Article
摘要目的:评价中国健康受试者单次和多次口服氟伐他汀钠缓释片与速释胶囊的药代动力学特征和相对生物利用度。方法开放性、随机、双周期、双治疗的交叉研究设计。24名受试者随机分成2组,给药周期1和周期2的第1~7天先后多次口服氟伐他汀钠缓释片(80 mg,qd)或速释胶囊(40 mg,bid)。用液相色谱-串联质谱法( LC-MS/MS)测定血清氟伐他汀血药浓度,用WinNonlin非房室模型计算药代动力学参数和相对生物利用度,用SPSS 18.0对药代动力学参数进行比较分析。结果受试者单次口服氟伐他汀钠缓释片(80 mg,qd)或速释胶囊(40 mg,bid)后主要药代动力学参数:Cmax分别为(79.00±36.83),(439.80±199.35) ng· mL-1;tmax分别为3.00,0.50 h;t1/2分别为(5.39±2.89),(1.88±0.50) h;AUC0-∞分别为(342.34±146.05),(792.32±294.33) ng· h· mL-1。受试者多次口服氟伐他汀钠缓释片(80 mg,qd)或速释胶囊(40 mg, bid)7 d 后主要药代动力学参数:Cmax,s 分别为(96.85±59.38),(526.54±228.08) ng· mL-1;Cav,s 分别为(18.04±8.29),(63.39±29.02) ng· mL-1;tmax,s分别为3.00,0.50 h;t1/2分别为(5.13±2.69),(1.74±0.26) h;AUCtau,ss分别为(435.46±213.14),(1190.11±582.51) ng· h· mL-1。以氟伐他汀钠速释胶囊40 mg为参照,氟伐他汀钠缓释片80 mg的相对生物利用度分别为43.94%(单次给药后)和38.67%(达稳态后)。试验中仅发生轻度药物不良反应。结论与速释胶囊相比较,氟伐他汀钠缓释片tmax显著滞后,Cmax显著降低;第7天的药代动力学特征与第1天相似,无明显蓄积现象。 Objective To evaluate the pharmacokinetic profiles and rel-ative bioavailability of fluvastatin in healthy Chinese subjects following o-ral administration of single and multiple doses of prolonged -extended re-lease ( XL) fluvastatin sodium tablets or immediate -release ( IR) cap-sules.Methods This was an open -label, randomized, two-period, two-treatment, crossover study.Twenty -four subjects were orally ad-ministered fluvastatin sodium XL tablet 80 mg qd or IR capsule 40 mg bid for 7 days.The serum concentrations of fluvastatin were determined by LC-MS/MS.The pharmacokinetic parameters and the relative bioavail-ability were calculated by non -compartmental analysis ( NCA ) using WinNonlin program.The statistical comparison of the pharmacokinetic parameters between these two formulations was conducted using SPSS 18.0.Results The pharmacokinetic parameters of fluvastatin after single oral dose of fluvastatin sodium XL tablet 80 mg qd and fluvastatin IR capsule 40 mg bid were as follows:Cmax were (79.00 ±36.83 ), (439.80 ±199.35 ) ng· mL-1;tmax were 3.00,0.50 h;t1/2 were (5.39 ± 2.89), (1.88 ±0.50) h;AUC0-24 h were (347.82 ±134.19 ), (815.25 ±326.30 ) ng· h· mL-1;AUC0-∞ were (342.34 ±146.05), (792.32 ±294.33) ng· h· mL -1, respectively.The pharmacokinetic parameters of fluvastatin after multiple oral doses of fluvastatin sodium XL tablet 80 mg qd and IR capsule 40 mg bid were as follows:Cmax,s were (96.85 ±59.38), (526.54 ±228.08) ng· mL-1;Cav,sswere (18.04 ±8.29), (63.39 ±29.02) ng· mL-1;tmax,ss were 3.00, 0.50 h;t1/2 were (5.13 ±2.69 ), (1.74 ±0.26 ) h; AUCtau,ss were (435.46 ±213.14 ), (1194.11 ± 582.51 ) ng· h· mL-1 , respectively.The relative bioavailabilities of fluvastatin sodium XL tablet 80 mg to IR capsule 40 mg were 43.94%and 38.67%on day 1 ( after single dose administration ) and day 7 ( after reaching steady state ) , respectively.Mild adverse events occurred in this trial.Conclusion Comparing with fluvastatin sodium IR capsues , Cmax of fluvastatin sodium XL tablet was reduced and tmax was prolonged.There was no significant accumulation for XL and IR formulations after multiple doses.
语种中文
原文出处查看原文
引用统计
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/43950
专题北京大学第一临床医学院_药剂科
作者单位1.北京大学 第一医院 药剂科,北京,100034
2.诺华 中国 生物医学研究有限公司,上海,201203
推荐引用方式
GB/T 7714
赵楠,赵侠,许俊羽,等. 单次和多次口服氟伐他汀钠缓释片与速释胶囊在中国健康人体药代动力学研究[J]. 中国临床药理学杂志,2014(8):689-692.
APA 赵楠,赵侠,许俊羽,赵蓉,&崔一民.(2014).单次和多次口服氟伐他汀钠缓释片与速释胶囊在中国健康人体药代动力学研究.中国临床药理学杂志(8),689-692.
MLA 赵楠,et al."单次和多次口服氟伐他汀钠缓释片与速释胶囊在中国健康人体药代动力学研究".中国临床药理学杂志 .8(2014):689-692.
条目包含的文件
条目无相关文件。
个性服务
推荐该条目
保存到收藏夹
查看访问统计
导出为Endnote文件
谷歌学术
谷歌学术中相似的文章
[赵楠]的文章
[赵侠]的文章
[许俊羽]的文章
百度学术
百度学术中相似的文章
[赵楠]的文章
[赵侠]的文章
[许俊羽]的文章
必应学术
必应学术中相似的文章
[赵楠]的文章
[赵侠]的文章
[许俊羽]的文章
相关权益政策
暂无数据
收藏/分享
所有评论 (0)
暂无评论
 

除非特别说明,本系统中所有内容都受版权保护,并保留所有权利。