CAJ | 학술논문

目的观察兔眼局部应用复方两性霉素B眼用凝胶的眼内通透性和药代动力学特征.方法将30只新西兰大白兔分为10组,每组3只(6只眼),分别于30只兔双眼点复方两性霉素B眼用凝胶50μl后,5、15、30、45、60、90、120、180、240和360 min时取泪液,并迅速处死后取角膜和房水,测定两性霉素B和利福平的含量,计算药代动力学参数.结果利福平有良好的眼内通透性,但房水中检测不到两性霉素B;两性霉素B和利福平在兔角膜中的达峰时间为20.96和7.57 min、达峰浓度为3.32和25.37μg/g、消除半衰期为45.34和31.69 min、浓度-时间曲线下面积为299.44和1368.91(min·mg)/g.结论复方两性霉素B眼用凝胶可用于治疗外眼真菌感染性疾病,但其能否用于内眼真菌感染,仍需进一步研究.
목적 관찰토안국부응용복방량성매소B안용응효적안내통투성화약대동역학특정.방법 장30지신서란대백토분위10조,매조3지(6지안),분별우30지토쌍안점복방량성매소B안용응효50μl후,5、15、30、45、60、90、120、180、240화360 min시취루액,병신속처사후취각막화방수,측정량성매소B화리복평적함량,계산약대동역학삼수.결과 리복평유량호적안내통투성,단방수중검측불도량성매소B;량성매소B화리복평재토각막중적체봉시간위20.96화7.57 min、체봉농도위3.32화25.37μg/g、소제반쇠기위45.34화31.69 min、농도-시간곡선하면적위299.44화1368.91(min·mg)/g.결론 복방량성매소B안용응효가용우치료외안진균감염성질병,단기능부용우내안진균감염,잉수진일보연구.
Objective To study the intraocular penetration and pharmacokinetics of amphotericin B and rifampicin following topically applying compound amphotericin B eye gel in rabbit eyes. Methods Thirty rabbits were randomly divided into 10 groups. The tears were collected at 5, 15, 30, 45, 60, 90, 120, 180, 240 and 360 minutes after compound amphotericin B eye gel was applied to the rabbit eyes. Then the rabbits were sacrificed and the cornea and aqueous humors were collected immediately. The concentrations of amphotericin B and rifampicin were detected by High-performance liquid chromatography (HPLC) and pharmacokinetic parameters were estimated.Results Rifampicin could rapidly penetrate into rabbit ocular tissues, but amphotericin B in aqueous humors could not be detected by HPLC. Amphotericin B could maintain high concentration in tears for 4 hours. The pharmacokinetic parameters of amphotericin B and rifampicin in rabbits cornea were as follows: Tpeak was 20.96 and 7.57 min,Cmax was 3.32 and 25.37 μg/g, t1/2 was 45.34 and 31.69 min and AUC was 299.44 and 1368.91 min ·μg/g.Conclusions The results may provide experimental data for treatment of extraocular fungal infectious disease with compound amphotericin B eye gel. However, the therapeutic effect of compound amphotericin B eye gel on intraocular fungal infection need to be furtherly studied.