Fantes F E, Parrish R K, Heuer D K, Sossi N
Ophthalmic Surg. 1987 May;18(5):375-8.
Aqueous, corneal, and tear film 14C 5-fluorouracil (5-FU) levels were measured in rabbit eyes to better understand the mechanisms of intraocular penetration after subconjunctival injection. Significantly higher aqueous and tear 5-FU levels were achieved one hour after administration when the subconjunctival injection was given transconjunctivally rather than percutaneously through the upper lid [aqueous = 65.7 +/- 9.1 micrograms/ml vs 21.3 +/- 5.1 micrograms/ml (mean +/- SE; p = 0.02, 2-tailed t-test); and tears = 5408.8 +/- 357.3 micrograms/ml vs 228.0 +/- 46.4 micrograms/ml (mean +/- SE; p = 0.004, 2-tailed t-test)]. The aqueous 5-FU levels four hours after transconjunctival injection were significantly greater in anesthetized rabbits without blink reflexes than in those with intact reflexes [32.0 +/- 3.2 micrograms/ml vs 13.4 +/- 0.5 micrograms/ml (mean +/- SE; p = 0.026, 2-tailed t-test)]. The corneal 5-FU levels four hours after transconjunctival injection were greatest nearest the injection site. Direct corneal penetration appears to account for the majority of the aqueous 5-FU concentration after subconjunctival injection; however, there may also be diffusion through the limbus.
为了更好地理解结膜下注射后眼内渗透的机制，对兔眼的房水、角膜和泪膜中的14C 5-氟尿嘧啶（5-FU）水平进行了测量。结膜下注射经结膜给药而非经上睑经皮给药时，给药1小时后房水和泪液中的5-FU水平显著更高[房水=65.7±9.1微克/毫升对21.3±5.1微克/毫升（平均值±标准误；p=0.02，双侧t检验）；泪液=5408.8±357.3微克/毫升对228.0±46.4微克/毫升（平均值±标准误；p=0.004，双侧t检验）]。结膜下注射4小时后，无瞬目反射的麻醉兔的房水5-FU水平显著高于有完整反射的兔[32.0±3.2微克/毫升对13.4±0.5微克/毫升（平均值±标准误；p=0.026，双侧t检验）]。结膜下注射4小时后，角膜5-FU水平在最靠近注射部位处最高。结膜下注射后房水5-FU浓度的大部分似乎是由角膜直接渗透所致；然而，也可能存在通过角膜缘的扩散。
