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纸质出版:2013
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郭惠玲,杜改萍,胡莲娜,王大江,王丽强,黄一飞.新型免疫抑制剂J2纳米混悬液结膜下注射后在兔外周血及眼内的分布[J].陆军军医大学学报(原第三军医大学学报),2013,35(12):1225-1228.
Guo Huiling,Du Gaiping,Hu Lianna,Wang Dajiang,Wang Liqiang,Huang Yifei.Distribution of a novel immunosuppressant J2 nano-suspension in peripheral blood and eyes in rabbits after subconjunctival injection[J].J Amry Med Univ (J Third Mil Med Univ),2013,35(12):1225-1228.
郭惠玲,杜改萍,胡莲娜,王大江,王丽强,黄一飞.新型免疫抑制剂J2纳米混悬液结膜下注射后在兔外周血及眼内的分布[J].陆军军医大学学报(原第三军医大学学报),2013,35(12):1225-1228. DOI:
Guo Huiling,Du Gaiping,Hu Lianna,Wang Dajiang,Wang Liqiang,Huang Yifei.Distribution of a novel immunosuppressant J2 nano-suspension in peripheral blood and eyes in rabbits after subconjunctival injection[J].J Amry Med Univ (J Third Mil Med Univ),2013,35(12):1225-1228. DOI:
目的 观察新型免疫抑制剂J2-NS兔结膜下注射后在外周血及眼内组织的分布。 方法 8~12周龄健康成年新西兰白兔18只(36眼),结膜下注射J2-NS,分别于注药后1、3 d,1、2、3、4周后取角膜、房水、虹膜以及外周血,HPLC法检测组织内的药物浓度(n=6),并使用WinNonlin药代动力学软件计算主要的药代动力学参数。 结果 J2-NS兔结膜下注射后,观察期内在组织中均可检测到药物浓度。1 d到4周内血清药物浓度为(11.19±0.33)~(13.23±0.84)ng/mL;眼部组织中角膜的药物浓度最高,而在房水和虹膜内的药物浓度较低。在角膜内,1 d到4周内药物浓度为(5.72±1.67)~(11.86±4.35)ng/mg,峰浓度(Cmax)为11.861 3 ng/mg,达峰时间(Tmax)为1 d,曲线下面积(AUC)为201.561 5 ng/(mg·d),半衰期(T
1/2
)达45 d。 结论 新型免疫抑制剂J2-NS在结膜下单次注射后药物主要分布于外周血及角膜内,且在长时间能够维持有效药物浓度。
Objective To investigate the distribution of a novel immunosuppressant
J2 nano-suspension (NS)
in the peripheral blood and intraocular tissues in rabbits after subconjunctival injection. Methods Totally 18 healthy New Zealand white rabbits (36 eyes)
8- to 12-week-old
were given an subconjunctival injection of 0.2 ml 1% J2-NS. Drug concentration in the cornea
aqueous humor
and iris (6 eyes in each time point) and peripheral blood was detected by high-performance liquid chromatography (HPLC) on the days 1 and 3
and the
weeks of 1
2
3 and 4 respectively after injection. The main pharmacokinetic parameters were calculated by pharmacokinetic software
WinNonlin. Results J2-NS at different concentrations was found in all detected organs during the observation period after injection. The serum concentration of J2-NS was 11.19±0.33 to 13.23±0.84 ng/mL from the day 1 to week 4 after injection. The cornea had the highest dose in all the eye tissues
but it was at lower dose in the aqueous humor and iris. The concentration was 5.72±1.67 to 11.86±4.35 ng/mg in the cornea from the day 1 to week 4 after injection
with Cmax of 11.861 3 ng/mg
Tmax of 1 d
and area under curve (AUC) of 201.561 5 ng/(mg·d)and T
1/2
of 45 d. Conclusion Single subconjunctival injection of J2-NS leads the drug mainly being distributed in the peripheral blood and cornea
and being maintained at the effective drug concentration for a long time.
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