ABSORPTION OF POLYETHYLENE GLYCOL-600 THROUGH POLYETHYLENE GLYCOL-2000 - THE MOLECULAR-WEIGHT DEPENDENCE OF GASTROINTESTINAL AND NASAL ABSORPTION

被引:147
作者
DONOVAN, MD [1 ]
FLYNN, GL [1 ]
AMIDON, GL [1 ]
机构
[1] UNIV MICHIGAN,COLL PHARM,ANN ARBOR,MI 48109
关键词
gastrointestinal absorption; molecular weight cutoff; molecular weight-dependent absorption; nasal absorption; permeability; polyethylene glycol;
D O I
10.1023/A:1015921101465
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
Polyethylene glycols (PEGs) 600,1000, and 2000 were used to study the molecular weight permeability dependence in the rat nasal and gastrointestinal mucosa. Absorption of the PEGs was measured by following their urinary excretion over a 6-hr collection period. HPLC methods were used to separate and quantitate the individual oligomeric species present in the PEG samples. The permeabilities of both the gastrointestinal and the nasal mucosae exhibited similar molecular weight dependencies. The steepest absorption dependence for both mucosae occurs with the oligomers of PEG 600, where the extent of absorption decreases from approximately 60% to near 30% over a molecular weight range of less than 300 daltons. Differences in the absorption characteristics between the two sites appear in the molecular weight range spanned by PEG 1000. For these oligomers, the mean absorption from the nasal cavity is approximately 14%, while that from the gastrointestinal tract is only 9%. For PEG 2000, mean absorption decreases to 4% following intranasal application and below 2% following gastrointestinal administration. Within the PEG 1000 and 2000 samples, however, very little molecular weight dependency is seen among the oligomers. In the range studied, a distinct molecular weight cutoff was not apparent at either site. © 1990, Plenum Publishing Corporation. All rights reserved.
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页码:863 / 868
页数:6
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