Pharmacokinetics of different nitrendipine tablets in rats

Abstract

Abstract: AIM: To study the pharmacokinetics of different nitrendipine tablets in rats. METHODS: An LC-MS method was established for the detection of nitrendipine in plasma after a single oral dose of 50 mg/kg nitrendipine tablets. Pharmacokinetics parameters were calculated by DAS 3.0 data-processing system. RESULTS: Determination results of the three bulk drug manufactures indicated that nitrendipine form Ⅳ had a higher absorption and bioavailability than nitrendipine form Ⅰ which was commonly used. Pharmacokinetic parameters of the 16 products selected randomly from different industries were different after a single dose of 50 mg/kg. Maximum differences of C_max,t_max,t_1/2, AUC_(0-t) came up to 2.5, 24.4, 4.5 and 1.6 times. CONCLUSION: There are differences among the pharmacokinetics of different nitrendipine tablets in rats. Crystal form is a principal element leading to the discrepancies

Key words: Nitrendipine, LC-MS, Crystal form, Pharmacokinetics, Bioavailability

CLC Number:

R969.1

SUN Jia-lin, SONG Jun-ke, XING Cheng, LV Yang, DU Guan-hua. Pharmacokinetics of different nitrendipine tablets in rats[J]. Chinese Journal of Clinical Pharmacology and Therapeutics, 2012, 17(7): 755-760.

References

[1] Kumar VV,Chandrasekar D,Ramakrishna S,et al.Development and evaluation of nitrendipine loaded solid lipid nanoparticles:influence of wax and glyceride lipids on plasma pharmacokinetics[J].Int J Pharm,2007,335(1/2):167-175.
[2] Han P,Chu ZX,Shen FM,et al.Synergism of hydrochlorothiazide and nitrendipine on reduction of blood pressure and blood pressure variability in spontaneously hypertensive rats[J].ActaPharmacol Sin,2006,27(12):1575-1579.
[3] 李妍,邹梅娟,王悦,等.不同厂家尼群地平片溶出度考察[J].中国药剂学杂志,2008,6(3):96-101.
[4] Palem CR,Gannu R,Yamsani SK,et al.Development of a high-performance liquid chromatography method for simultaneous determination of pioglitazone and felodipine in pig serum:application to pharmacokinetic study[J].Biomed Chromatogr,2011,25(8):952-958.
[5] 袁恒杰,陈大为,刘艳丽,等.尼莫地平多晶型家免体内药动学研究[J].中国药学杂志,2005,40 (8):609-612.
[6] Venishetty VK,Durairaj C,Sistla R,et al.Development and validation of a reversed-phase HPLC method for determination of nitrendipine in rat plasma:application to pharmacokinetic studies[J].Biomed Chromatoqr,2007,21(4):363-368.
[7] Palem CR,Gannu R,Yamsani SK,et al.Development of a high-performance liquid chromatography method for simultaneous determination of pioglitazone and felodipine in pig serum:application to pharmacokinetic study[J].Biomed Chromatogr,2011,25(8):952-958.
[8] Wang D,Jiang K,Yang S,et al.Determination of nifedipine in human plasma by ultra performance liquid chromatography-tandem mass spectrometry and its application in a pharmacokinetic study[J].J Chromatogr B Analyt Technol Biomed Life Sci,2011,879(20):1827-1832.
[9] Liu Y,Jia J,Liu G,et al.Pharmacokinetics and bioequivalence evaluation of two formulations of 10-mg amlodipine besylate:an open-label,single-dose,randomized,two-way crossover study in healthy Chinese male volunteers[J].ClinTher,2009,31(4):777-783.
[10] Wang D,Jiang K,Yang S,et al.Determination of nifedipine in human plasma by ultra performance liquid chromatography-tandem mass spectrometry and its application in a pharmacokinetic study[J].J Chromatogr B AnalytTechnol Biomed Life Sci,2011,879(20):1827-1832.
[11] 吕扬,杜冠华.晶型药物[M].北京:人民卫生出版社,2009:35-36.
[12] Xia D,Quan P,Piao H,et al.Preparation of stable nitrendipinenanosuspensions using the precipitation-ultrasonication method for enhancement of dissolution and oral bioavailability [J].Eur J Pharm Sci,2010,40(4):325-334.

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