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滴眼剂的局部滴注是一种方便而有用的治疗手段,但药物的利用度差,作用时间短,不适于亲脂性药物。近来,提出利用脂质体作为眼用。本文用地塞米松(DM)及其缬草酸酯(DV)、棕榈酸酯(DP)为模型药物用于兔眼,试验脂质体作为难溶性药物眼用给药系统的效用。制备氚标记的甾类脂质体和水混悬液,滴至雄性新西兰白兔角膜,进行示踪实验。杀死动物,收集眼房水,取出眼球,分离角膜、虹膜和晶状体,处理后在液体闪烁计数器上计数。眼房水中各制剂的达峰时均在1～2h,然后以一级过程消除。滴注DV或DM混悬液后,甾类的浓度几乎相同,DP混悬液的浓度明显低于前二者。滴注DV脂质体后,浓度最高,在各眼组织中的利用度也最高。脂质体改变峰浓度,但并不改变达峰时或消除速率,其主要
Eye drops of local drip is a convenient and useful treatment, but poor drug utilization, short duration of action, not suitable for lipophilic drugs. Recently, the use of liposomes for ophthalmic use has been proposed. In this paper, dexamethasone (DM) and its Valerian acid ester (DV), palmitate (DP) as a model drug for the rabbit eye, liposomes as a trial of the efficacy of poorly soluble drug ophthalmic delivery system. Preparation of tritiated steroid liposomes and water suspension, drops to male New Zealand white rabbit corneas, tracer experiments. Animals were sacrificed, aqueous humor was collected, eyes removed, corneal, iris and lens removed, counted on a liquid scintillation counter after treatment. All preparations in the aqueous humor in the peak of 1 ~ 2h, and then to eliminate a process. After instillation of DV or DM instillation, the concentrations of steroids were almost the same, and the concentration of DP suspension was significantly lower than the former two. Instillation of DV liposomes resulted in the highest concentration and the highest availability in each ocular tissue. Liposomes change the peak concentration, but do not change the peak or elimination rate, which is mainly