Pharmacokinetic performance of the nitrendipine intravenous submicron emulsion in rats

被引:5
作者
Guan, Jibin [1 ]
Zhao, Nana [1 ]
Zhai, Yinglei [1 ]
Chu, Chunxia [1 ]
Chen, Hongming [1 ]
Zhang, Tianhong [1 ]
机构
[1] Shenyang Pharmaceut Univ, Sch Pharm, 103,Wenhua Rd, Shenyang 110016, Peoples R China
关键词
Nitrendipine; Submicron emulsion; Bioavailability; Method validation;
D O I
10.1016/j.ajps.2014.07.004
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
To compare pharmacokinetic behaviors of nitrendipine submicron emulsion with nitrendipine solution following intravenous administration in rats. The plasma concentrations were analyzed by ultra-performance liquid chromatography coupled with tandem mass spectrometry detection (UPLCeMS/MS) through a new validated method. The pharmacokinetic parameters of the nitrendipine submicron emulsion and nitrendipine solution were as follows: AUC(0) (t) 900.76 +/- 186.59 versus 687.08 +/- 66.24 ng h/ml, C-max 854.54 +/- 159.48 versus 610.59 +/- 235.99 ng/ml, t(1/2) 2.37 +/- 1.99 versus 2.80 +/- 2.69 h. The relative bioavailability of nitrendipine submicron emulsion to nitrendipine solution was 131.4 +/- 11.3%. The developed methods could meet the requirements of bioanalysis. Compared to the solution injection, intravenous submicron emulsion presents higher systematic exposure which can help to improve the therapeutic efficacy. (C) 2014 Shenyang Pharmaceutical University. Production and hosting by Elsevier B.V. All rights reserved.
引用
收藏
页码:330 / 335
页数:6
相关论文
共 20 条
[11]   Determination of nimodipine in human plasma by ultra performance liquid chromatography-tandem mass spectrometry and pharmacokinetic application [J].
Qin, Feng ;
Ma, Yuanyuan ;
Wang, Yiqi ;
Chen, Lingyun ;
Wang, Dong ;
Li, Famei .
JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS, 2008, 46 (03) :557-562
[12]   A novel surface modified nitrendipine nanocrystals with enhancement of bioavailability and stability [J].
Quan, Peng ;
Shi, Kai ;
Piao, Hongze ;
Piao, Hongyu ;
Liang, Na ;
Xia, Dengning ;
Cui, Fude .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2012, 430 (1-2) :366-371
[13]  
SINGH M, 1986, Journal of Parenteral Science and Technology, V40, P34
[14]   Preparation and evaluation of solid dispersion for nitrendipine-carbopol and nitrendipine-HPMCP systems using a twin screw extruder [J].
Wang, LA ;
Cui, FD ;
Hayase, T ;
Sunada, H .
CHEMICAL & PHARMACEUTICAL BULLETIN, 2005, 53 (10) :1240-1245
[15]   Improvement of the dissolution rate of nitrendipine using a new pulse combustion drying method [J].
Wang, Liang ;
Cui, Fu-De ;
Sunada, Hisakazu .
CHEMICAL & PHARMACEUTICAL BULLETIN, 2007, 55 (08) :1119-1125
[16]   Solid self-emulsifying nitrendipine pellets: Preparation and in vitro/in vivo evaluation [J].
Wang, Zhiyuan ;
Sun, Jin ;
Wang, Yongjun ;
Liu, Xiaohong ;
Liu, Yanhua ;
Fu, Qiang ;
Meng, Ping ;
He, Zhonggui .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2010, 383 (1-2) :1-6
[17]   Effect of Crystal Size on the In Vitro Dissolution and Oral Absorption of Nitrendipine in Rats [J].
Xia, Dengning ;
Cui, Fude ;
Piao, Hongze ;
Cun, Dongmei ;
Piao, Hongyu ;
Jiang, Yanbo ;
Ouyang, Mei ;
Quan, Peng .
PHARMACEUTICAL RESEARCH, 2010, 27 (09) :1965-1976
[18]   Preparation of stable nitrendipine nanosuspensions using the precipitation-ultrasonication method for enhancement of dissolution and oral bioavailability [J].
Xia, Dengning ;
Quan, Peng ;
Piao, Hongze ;
Piao, Hongyu ;
Sun, Shaoping ;
Yin, Yongmei ;
Cui, Fude .
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES, 2010, 40 (04) :325-334
[19]   In vivo evaluation of two novel controlled-release nitrendipine formulations [J].
Yang, MS ;
Cui, FD ;
You, BG ;
Yang, MH ;
Tao, AJ ;
Cun, DM ;
Kawashima, Y .
DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY, 2005, 31 (07) :589-595
[20]  
Zhao N., 2011, ASIAN J PHARM SCI, V6, P151