摘要
目的研究富马酸酮替芬颗粒与富马酸酮替芬片(均为平喘药)的相对生物利用度,评价2者的生物等效性。方法采用双周期自身交叉试验设计,单剂量口服给药。24例健康男性受试者分别单剂量口服受试制剂和参比制剂,血浆样品采用高效液相色谱串联质谱法检测。结果受试制剂富马酸酮替芬颗粒及参比制剂富马酸酮替芬片的主要药代动力学参数:Cmax分别为(247.76±99.61),(229.24±96.44)ng.L-1;tmax分别为(2.38±0.97),(2.46±1.14)h;t1/2分别为(14.85±5.76),(14.69±7.91)h;AUC0-tn分别为(2641.07±1025.19),(2764.19±1231.50)ng.L-1.h;AUC0-∞分别为(3192.01±1272.20),(3431.11±1902.72)ng.L-1.h;受试制剂富马酸酮替芬颗粒的相对生物利用度F0-tn、F0-∞分别为(100.08±21.81)%,(102.75±30.33)%。结论受试制剂和参比制剂具有生物等效性。
Objective To study the bioequivalence of ketotifen fumar- ate granule and ketotifen fumarate tablets in healthy volunteers. Methods A single oral dose of ketotifen fumarate was given respectively to 24 healthy male volunteers in a two - way cross over test and plasma concen- trations were determined by HPLC - MS/MS. Results The main pharmaeokinetie parameters of the test preparation and reference preparation were as follows： Cmax were （247.76 ± 99.61 ）and （229.24± 96.44） ng·L-1 ; t were （2.38 ±0.97） and（2.46 ± 1.14） h; t1/z were（ 14. 85 ± 5.76） and（ 14. 69 ± 7.91 ） h ; AUC0-tn were （2641.07 ± 1025.19） and （2764.19 ± 1231.50） ng·L-1·h; AUC0-tn of were （3192.01 ± 1272.20）and（3431.11 ± 1902.72） ng·L-1·h; F0-tn, F0-∞ of test preparation were （ 100. 08 ± 21.81 ） % and（ 102. 75 ± 30.33 ） %. Con- clusion The test preparation was bioequivalent to the reference preparation.
出处
《中国临床药理学杂志》
CAS
CSCD
北大核心
2010年第10期757-760,共4页
The Chinese Journal of Clinical Pharmacology
