THE PHARMACOKINETICS OF BETA-CYCLODEXTRIN AND HYDROXYPROPYL-BETA-CYCLODEXTRIN IN THE RAT

被引:99
作者
FRIJLINK, HW [1 ]
VISSER, J [1 ]
HEFTING, NR [1 ]
OOSTING, R [1 ]
MEIJER, DKF [1 ]
LERK, CF [1 ]
机构
[1] UNIV GRONINGEN,DEPT PHARMACOL & THERAPEUT,9713 AW GRONINGEN,NETHERLANDS
关键词
absorption; hydroxypropyl-β-cyclodextrin; intravenous administration; oral administration; pharmacokinetics; β-cyclodextrin;
D O I
10.1023/A:1015929720063
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
Hydroxypropyl-β-cyclodextrin was analyzed by HPLC using postcolumn complexation with phenolphthalein and negative colorimetric detection, with a detection limit of 20 µg/ml. The pharmacokinetics of β-cyclodextrin and of hydroxypropyl-β-cyclodextrin were studied after intravenous administration to permanently cannulated rats. The pharmacokinetic behavior of both cyclodextrins was similar to that of inulin, showing rapid distribution over extracellular fluids. Elimination occurred through glomerular filtration. When a dose of 200 mg/kg β-cyclodextrin was administered the elimination rate was decreased, probably as a result of nephrotoxicity of β-cyclodextrin. Within 24 hr after administration most of the cyclodextrin dose was recovered unchanged in urine. After oral administration, only insignificant amounts of intact β-cyclodextrin were absorbed from the gastrointestinal tract. © 1990, Plenum Publishing Corporation. All rights reserved.
引用
收藏
页码:1248 / 1252
页数:5
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