复方两性霉素B滴眼液局部应用的兔眼通透性

Intraocular penetration of compound amphotericin B eye drops after topical administration in rabbit eyes

目的考察眼局部应用复方两性霉素B滴眼液的眼通透性。方法将复方两性霉素B滴眼液50μL滴入兔结膜囊内后,分别于30和60min取泪液、角膜和房水作为测试样本,并用高效液相色谱法测定其药物浓度。结果复方两性霉素B滴眼液滴眼后30和60min,利福平在角膜中的浓度分别为(9.9±s1.0)μg·g-1和(5.8±0.9)μg·g-1,在泪液中的浓度为(96±10)μg·g-1和(5.2±0.8)μg·g-1,在房水中的浓度为(0.42±0.11)mg·L-1和(0.73±0.17)mg·L-1;两性霉素B在角膜中的浓度分别为(1.9±0.4)μg·g-1和(1.31±0.25)μg·g-1,在泪液中的浓度为(430±70)μg·g-1和(191±23)μg·g-1。结论利福平有良好的眼通透性,复方两性霉素B在角膜中可获得高于多数真菌的最低抑菌浓度,复方两性霉素B滴眼液可用于真菌性角膜炎的治疗。

AIM To investigate the intraocular penetration of compound amphotericin B eye drops. METHODS The tear, cornea and aqueous humor of the experimental rabbits were collected at 30 min and 60 min after topical application of 50 μL compound amphotericin B eye drops, and then the concentrations of amphotericin B and rifampicin were detected by HPLC. RESULTS The concentration of amphotericin B in cornea and tears at 30 min and 60 min after administration of 50 p.L compound amphotericin B eye drops were （1.9 ± s 0.4）ixg＇g-1 vs. （1.31 ± 0.25）μg·g^-1 and （430 ± 70）μg·g^-1 vs. （191 ± 23）μg·g^-1 , respectively. The concentrations ofrifampicin in cornea and tears were （9.9 ± 1.0） μg·g^-1vs. （5.8± 0.9） μg·g^-1 and （96 ± 10）μg·g^-1 vs. （5.2 ± 0.8）μg·g^-1, respectively, with （0.42 ± 0.11）mg·L^-1 vs. （0.73 ± 0.17）mg·L^-1 in aqueous humor. CONCLUSION Rifampicin has the good intraocular penetration, and the concentrations of amphotericin B in tear and cornea are higher than minimum inhibitory concentration for treatingmost fungi, so compound amphotericin B eye drops can be used to treat fungal keratitis.