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纸质出版:2014
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钟萌,孙全,冯悦,万胜利,张景勍.不同粒径的阳离子阿奇霉素泡囊体内生物等效性研究[J].陆军军医大学学报(原第三军医大学学报),2014,36(12):1295-1298.
Zhong Meng,Sun Quan,Feng Yue,Wan Shengli,Zhang Jingqing.Bioequivalence of positive ion azithromycin niosomes in different particle sizes[J].J Amry Med Univ (J Third Mil Med Univ),2014,36(12):1295-1298.
目的 比较不同粒径的阳离子阿奇霉素囊泡及阿奇霉素(azithromycin,AM)原料药在大鼠体内的药代动力学参数,并计算其相对生物利用度。 方法 大鼠单剂量口服小粒径、大粒径阿奇霉素囊泡及阿奇霉素原料药后,采用HPLC法测定药物浓度,并用DAS2.1.1软件计算药代动力学参数并以统计矩参数C
max
、AUC
0-t
和t
max
,通过双向单侧 t 检验和非参数检验判断3种制剂的生物等效性。 结果 小粒径阿奇霉素泡囊(AMNSS)和大粒径阿奇霉素泡囊(AMNSL)以及原料药AM体内的C
max
分别为18.73、9.2 mg/L和10.31 mg/L;t
max
分别为6、4 h和2 h;AUC
0-t
分别为371.79、160.41 mg·h/L 和136.09 mg·h/L;AUC
0-∞
分别为454.92、263.16 mg·h/L和158.50 mg·h/L;小粒径阿奇霉素泡囊和大粒径阿奇霉素泡囊相对生物利用度为273.19%、117.87%;经方差分析、双向单侧 t 检验和非参数检验,小粒径阿奇霉素泡囊和阿奇霉素、小粒径阿奇霉素泡囊和大粒径阿奇霉素泡囊体内有统计学差异(
P
0.05)、而大粒径阿奇霉素泡囊和阿奇霉素体内无统计学差异(
P
0.05)。 结论 小粒径阿奇霉素泡囊和阿奇霉素、小粒径阿奇霉素泡囊和大粒径阿奇霉素泡囊体内生物不等效,而大粒径阿奇霉素泡囊和阿奇霉素体内生物等效。
Objective To compare the pharmacokinetic parameters and bioavailability of positive ion azithromycin niosomes and azithromycin solution in rats. Methods Drug concentrations in the plasma at different time points were determined by HPLC after single oral dose of small-particle-size azithromycin niosome (AMNSS)
large-particle-size azithromycin niosome (AMNSL) and azithromycin sol
ution (AM) in rats. The pharmacokinetic parameters were calculated by DAS 2.1.1. Statistical moment parameters were adopted to calculate the pharmacokinetic parameters including C
max
AUC
0-t
and t
max
. Analysis of nonparametric tests and two one-sided t-tests were used to evaluate the bioequivalence of the 3 formulations. Results The pharmacokinetic parameters of AMNSS
AMNSL and AM in plasma were: C
max
18.73
9.2 and 10.31 mg/L
respectively; t
max
6
4 and 2 h
respectively; AUC
0-t
371.79
160.41 and 136.09 mg·h/L
respectively; and AUC
0-∞
454.92
263.16 and 158.50 mg·h/L
respectively. AMNSS and AMNSL relative bioavailability F
0-t
was 273.19% and 117.87%
respectively. The main pharmacokinetic parameters analyzed by variance
two side t-test and Wilcoxon rank sum test showed significant differences between AMNSS and AM
as well as AMNSS and AMNSL in vivo (
P
0.05)
but no significant difference between AMNSL and AM (
P
0.05). Conclusion AMNSL and AM are bioequivalent
while AMNSS and AM are not
neither are AMNSS and AMNSL.
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