FOOD INCREASES THE BIOAVAILABILITY OF ISOTRETINOIN
FOOD INCREASES THE BIOAVAILABILITY OF ISOTRETINOIN
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DOI：
10.1002/j.1552-4604.1983.tb01800.x
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发表时间：
1983-01-01
影响因子：
2.9
通讯作者：
HANIGAN, JJ
中科院分区：
文献类型：
--
作者：
COLBURN, WA;GIBSON, DM;HANIGAN, JJ
健康男性受试者 (20) 接受 80 毫克（2 × 40 毫克胶囊）口服异维A酸[一种皮肤科药物]，在开放随机交叉设计中间隔 2 周的冲洗期。异维A酸在完全禁食期间、标准早餐后1小时、标准早餐时或标准早餐前1小时施用。在 72 小时内的特定时间采集血样。异维A酸血液浓度通过特定的 HPL [高效液相色谱] 方法测定。餐前 1 小时、餐时或餐后 1 小时给药时，异维A酸的相对生物利用度（AUC [血浆浓度-时间曲线下面积]）比完全禁食期间给药时高 1.5-2 倍。此外，由于与食物一起给药时的Cmax[最大浓度]值比餐后1小时给药时的Cmax[最大浓度]值更低，因此异维A酸与食物同时给药可能是最好的给药方法。
Healthy male subjects (20) received 80 mg (2 .times. 40 mg capsules) oral isotretinoin [a dermatological drug] separated by 2 wk washout periods in an open randomized crossover design. Isotretinoin was administered during a complete fast, 1 h after a standard breakfast, with a standard breakfast, or 1 h before a standard breakfast. Blood samples were obtained at specific times over a 72 h period. Isotretinoin blood concentations were determined by a specific HPL [high performance liquid chromatography] method. The relative bioavailability (AUC [area under the plasma concentration-time curve]) of isotretinoin was 1.5-2 times greater when the dose was administered 1 h before, concomitantly with, or 1 h after a meal than when it was given during a complete fast. In addition, because the Cmax [maximum concentration] value is lower when the dose is administered with food rather than 1 h after a meal, coadministration of isotretinoin with food may be the best method of administration.