BUCCAL DELIVERY OF PROGESTATIONAL STEROIDS .1. CHARACTERIZATION OF BARRIER PROPERTIES AND EFFECT OF PENETRANT HYDROPHILICITY

被引:17
作者
NAIR, M [1 ]
CHIEN, YW [1 ]
机构
[1] RUTGERS STATE UNIV,COLL PHARM,CONTROLLED DRUG DELIVERY RES CTR,PISCATAWAY,NJ 08855
关键词
BUCCAL DELIVERY; MUCOSAL PERMEABILITY; BARRIER CHARACTERIZATION; HYDROPHILICITY EFFECT; PROGESTATIONAL STEROID;
D O I
10.1016/0378-5173(93)90306-Z
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
In an attempt to characterize the barrier functions of buccal mucosa, a series of systematic studies were performed, using the rabbit as the animal model. The model penetrants used in these studies were progesterone, a lipophilic compound, and the hydroxy derivatives of progesterone, which have approximately similar molecular weights but differ in their hydrophilicity, to study the effect of a systematic variation in lipophilicity on the kinetics and rate of permeation across the rabbit buccal mucosa. The results indicated that transbuccal permeation occurs via both a lipoidal pathway and an aqueous-pore pathway. The mucosal permeability and partition coefficient are both governed by the degree of hydrophilicity, and are increased with removal of the lipid domain from the mucosal membrane.
引用
收藏
页码:41 / 49
页数:9
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