Ahlawat Preeti, Srinivas Nuggehally R
Global Drug Development, ClinTec (India) International Pvt Ltd, Bangalore 560 078, India.
Eur J Drug Metab Pharmacokinet. 2008 Jul-Sep;33(3):187-90. doi: 10.1007/BF03191117.
Compounds that belong to the class known as dual (alpha,gamma) peroxisome proliferator-activated receptors (PPARs) show interesting pharmacological properties--regulation of blood glucose, fatty acids, and lipid parameters. Using the recently published preclinical data of naveglitazar, an allometric method was used to predict the human pharmacokinetic parameters (CL/F and Vss/F). The predicted parameters were compared to observed/predicted values of other important dual (a,y) PPAR compounds. The allometry data suggested that naviglitazar (CL/F) was at least 4 times faster than that of ragaglitazar, while the Vss was either equal to or 40% lower as compared to that of ragaglitazar.
属于双（α，γ）过氧化物酶体增殖物激活受体（PPAR）类的化合物具有有趣的药理学特性——调节血糖、脂肪酸和脂质参数。利用最近公布的那格列净的临床前数据，采用异速生长法预测人体药代动力学参数（CL/F和Vss/F）。将预测参数与其他重要的双（α，γ）PPAR化合物的观察/预测值进行比较。异速生长数据表明，那格列净的CL/F至少比拉格列净快4倍，而其Vss与拉格列净相当或低40%。
