Topical carbonic anhydrase inhibitors IV: Relationship between excised corneal permeability and pharmacokinetic factors.
Topical carbonic anhydrase inhibitors IV: Relationship between excised corneal permeability and pharmacokinetic factors.
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局部碳酸酐酶抑制剂 IV：离体角膜通透性与药代动力学因素之间的关系。
DOI：
10.1002/jps.2600740506
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发表时间：
1985
影响因子：
3.8
通讯作者：
Barfknecht,CF
中科院分区：
文献类型：
--
作者：
Eller,MG;Schoenwald,RD;Dixson,JA;Segarra,T;Barfknecht,CF
乙氧唑胺(1)和两个代表苯环(2和3)6位上的羟乙氧基和氢取代的类似物，通过局部输注方法被应用于兔眼，以提供恒定的房水速率。统计矩理论被应用于局部输液数据，以描述每种化合物在兔眼内的分布。对于每个类似物，可以比较角膜吸收速率常数(Ka)、房水清除速率常数(K10)、处置平均停留时间(MRTd)、表观稳态分布体积(Vdss)和总眼球清除(QE)。活体眼球下降值与体外测定的最大角膜穿透率有关。特别是，与1和3相比，2有更长的停留时间和更慢的清除速度，这可能是由于它在兔眼局部给药时能够降低眼压，而1和3没有表现出任何活动。
Ethoxzolamide (1) and two analogues, representing a hydroxyethoxy and a hydrogen substitution on the 6-position of the benzene ring (2and3), were applied to rabbit eyes using a topical infusion method designed to provide a constant rate into aqueous humor. Statistical-moment theory was applied to the topical infusion data to describe disposition of each compound within the rabbit eye. For each analogue, it was possible to compare the corneal absorption rate constant (ka), aqueous humor elimination rate constant (k10), disposition mean residence time (MRTd), apparent steady-state volume of distribution (Vdss), and total ocular clearance (Qe). In vivo ocularkavalues were related to maximum in vitro corneal penetration rates determined across excised rabbit corneas. In particular,2had a much longer residence time and a slower clearance than1and3, which may be responsible for its ability to lower intraocular pressure when dosed topically to the rabbit eye, whereas1and3show no activity.