中国临床药理学杂志2024，Vol.40Issue(9)：1321-1326,6.DOI:10.13699/j.cnki.1001-6821.2024.09.017
复方利多卡因乳膏在中国健康受试者体内的生物等效性研究
Bioequivalence study of compound lidocaine cream in healthy Chinese subjects
摘要
Abstract
Objective To study the pharmacokinetic characteristics of the test formulation of compound lidocaine cream and reference formulation of lidocaine and prilocaine cream in Chinese healthy subjects and to evaluate whether there is bioequivalence between the two formulations.Methods A single-center,single-dose,randomized,open-label,two-period,two-sequence,crossover design was used.This study included 40 healthy subjects,and in each period,test formulation or reference formulation 60 g was applied to the skin in front of both thighs(200 cm2 each side,a total of 400 cm2)under fasting conditions,and the drug was left on for at least 5 h after application.The concentrations of lidocaine and prilocaine in plasma were determined using liquid chromatography-tandem mass spectrometry(LC-MS/MS)method.Pharmacokinetic parameters were calculated using WinNonlin 8.0 software to evaluate the bioequivalence of the two formulations.Results After the application of the test formulation compound lidocaine cream and the reference formulation lidocaine and prilocaine cream on both thighs of the subjects,the pharmacokinetic parameters of lidocaine in plasma were as follows:Cmax were(167.27±91.33)and(156.13±66.86)ng·mL-1,AUC0-t were(1 651.78±685.09)and(1 636.69±617.23)ng·mL-1·h,AUC0-∞ were(1 669.85±684.65)and(1 654.37±618.30)ng·mL-1·h,the adjusted geometric mean ratios were 104.49％,101.88％and 101.89％,respectively,with 90％confidence intervals of 98.18％-111.20％,97.80％-106.13％and 97.87％-106.07％,all within the range of 80.00％-125.00％.The pharmacokinetic parameters of prilocaine in plasma were as follows:Cmax were(95.66±48.84)and(87.52±39.16)ng·mL-1,AUC0-t were(790.86±263.99)and(774.14±256.42)ng·mL-1·h,AUC0_m were(807.27±264.67)and(792.84±254.06)ng·mL-1 h,the adjusted geometric mean ratios were 107.34％,103.55％and 102.98％,respectively with 90％confidence intervals of 101.69％-113.31％,99.94％-107.30％and 99.65％-106.43％,all within the range of 80.00％-125.00％.Conclusion The test formulation compound lidocaine cream and the reference formulation lidocaine and prilocaine cream are bioequivalent.关键词
复方利多卡因乳膏/健康受试者/生物等效性/药代动力学/液相色谱-串联质谱Key words
compound lidocaine cream/healthy subject/bioequivalence/pharmacokinetics/liquid chromatography-tandem mass spectrometry(LC-MS/MS)分类
医药卫生引用本文复制引用
常梦琦,孙宇琦,徐秋瑾,钱希曦,赵迎春,曹艳,王柳,张程,于栋梁..复方利多卡因乳膏在中国健康受试者体内的生物等效性研究[J].中国临床药理学杂志,2024,40(9):1321-1326,6.基金项目
江苏省新药研究与临床药学重点实验室开放研究课题基金资助项目(KFKT-2110) （KFKT-2110）
