期刊文献+

辛伐他汀口腔崩解片的人体生物等效性研究 被引量:6

Bioequiavailability of Simvastatin Orally Disintegrating Tablets in Healthy Volunteers
原文传递
导出
摘要 目的:比较2种辛伐他汀制剂的人体生物等效性。方法:18名健康男性志愿者随机交叉单剂量口服辛伐他汀口腔崩解片(受试制剂)与辛伐他汀片(参比制剂)40mg,用液-质联用法测定人血浆中药物浓度,并用3p97软件计算药动学参数和生物利用度。结果:2种辛伐他汀制剂在人体内药-时曲线符合一室模型,受试制剂与参比制剂的Cmax分别为(6.73±5.22)、(7.08±5.41)ng·mL-1,tmax分别为(2.11±0.74)、(1.89±0.85)h,AUC0~12分别为(19.83±19.09)、(19.98±18.20)ng·h·mL-1,AUC0~∞分别为(22.18±20.09)、(22.41±21.07)ng·h·mL-1。受试制剂相对于参比制剂的生物利用度为(99.25±13.11)%。结论:2种辛伐他汀制剂具有生物等效性。 OBJECTIVE:To compare the bioequiavailability of two simvastatin preparations in human bodies.METHODS: A total of 18 healthy male volunteers were enrolled in a randomized crossover study in which the subjects were randomly assigned to receive single dose of 40mg simvastatin orally disintegrating tablet(test) or simvastatin tablets(reference) .The plasma concentrations of simvastatin were determined by LC- MS, and the pharmacokinetic parameters and bioavailability were calculated with 3p97 program.RESULTS: The pharmacokinetics of simvastatin test and reference preparations were fitted the one - compartment model. The main pharmacokinetic parameters of the two preparations were as following: Cmax : (6.73 ± 5.22) vs. (7.08±5.41) ng·mL^-1、tmax (2.11±0.74)vs. (1.89 ±0.85)h, AUC0 -12: (19.83±19.09)vs. (19.98±18.20) ng · h · mL^-1, AUC0-∞: (22.18±20.09)vs. (22.41 ± 21.07)ng · h · mL^-1. The relative bioavailability of simvastatin orally disintegrating tablet as against simvastain tablet(reference) was (99.25±13.11)% .CONCLUSION: Simvastatin test and reference preparations were bioequivalent.
作者 石萍 陈相潘
出处 《中国药房》 CAS CSCD 北大核心 2007年第35期2757-2759,共3页 China Pharmacy
关键词 辛伐他汀口腔崩解片 液-质联用法 药动学 生物等效性 Simvastatin orally disintegrating tablet LC - MS Pharmacokinetics Bioequiavailability
  • 相关文献

参考文献3

二级参考文献13

  • 1曾天舒 陈璐璐 夏文芳.辛伐他汀促进成骨细胞增殖的实验研究[A]..中华医学会第一次全国骨质疏松学术会议论文汇编[C].北京:中华医学会,2001.121.
  • 2Mtmdy G, Garrett R, Harris S,et al. Stimulation of bone formation in vitro and in rodents by statins [ J]. Science,1999,286:1946-1949.
  • 3Sugiyama M, Kodama T, Konishi K, et al. Compaction and simvastatin, but not pravastatin, induce bone morphogenetic protein-2 in human osteosarcoma cells[J]. Biochem Biophys Res Commun, 2000,271:688-692.
  • 4Maeda T, Matsunuma A, Kawane T, et al. Simvastatin promotes osteoblast differentiation and mineralization in MC3T3E1 cells[J]. Biochem Biophys Res Commun, 2001,280:874-877.
  • 5Zerath E, Holy X, Noel B, et al. Effects of BMP-2 on osteoblastic cells and on skeletal growth and bone formation in unloaded rats[J]. Growth Horm IGF Res, 1998,8:141-149.
  • 6Fromigue O, Marie P J, Lomri A. Bone morphogenetic protein-2 and transforming growth factor-beta 2 interact to modulate human bone marrow stromal cell proliferation and differentiation[J]. J Cell Biochem, 1998,68:411-426.
  • 7Hay E, Hott M, Graulet A M, et al. Effects of bone morphogenetic protein-2 on human neonatal calvaria cell differentiation[J]. J Cell Biochem, 1999,72: 81-89.
  • 8Edwards C J, Hart D J, Spector T D. Oral statins and increased bone-mineral density in postmenopausal women[J] .Lancet, 2000,355: 2218-2219.
  • 9Chung Y S, Lee M D, Lee S K, et al. HMG-CoA reductase inhibitors increase BMD in type 2 diabetes mellitus patients [ J ]. J Clin Endocrinol Metab, 2000,85:1137-1142.
  • 10Meier C R, Schlienger R G, Kraenzlin M E, et al. HMGCoA reductase inhibitors and the risk of fractures [J]. JAMA,2000,283:3205-3210.

共引文献27

同被引文献67

引证文献6

二级引证文献8

相关作者

内容加载中请稍等...

相关机构

内容加载中请稍等...

相关主题

内容加载中请稍等...

浏览历史

内容加载中请稍等...
;
使用帮助 返回顶部