公开(公告)号：WO1996040192A1

公开(公告)日：1996-12-19

申请号：PCT/US1996009607

申请日：1996-06-07

Applicant: AVMAX, INC. ,  BENET, Leslie, Z. ,  WACHER, Vincent, J. ,  BENET, Reed, M.

Inventor： AVMAX, INC.

IPC: A61K38/00

CPC classification number: A61K47/44 ,  A61K9/0014 ,  A61K31/337 ,  A61K36/13 ,  A61K36/14 ,  A61K36/15 ,  A61K36/185 ,  A61K36/23 ,  A61K36/235 ,  A61K36/25 ,  A61K36/28 ,  A61K36/282 ,  A61K36/324 ,  A61K36/328 ,  A61K36/45 ,  A61K36/48 ,  A61K36/53 ,  A61K36/532 ,  A61K36/534 ,  A61K36/537 ,  A61K36/54 ,  A61K36/57 ,  A61K36/61 ,  A61K36/63 ,  A61K36/67 ,  A61K36/738 ,  A61K36/752 ,  A61K36/80 ,  A61K36/8962 ,  A61K36/898 ,  A61K36/899 ,  A61K36/9064 ,  A61K36/9068 ,  A61K38/13 ,  A61K47/10 ,  A61K2300/00

Abstract: A method for increasing bioavailability of an orally administered hydrophobic pharmaceutical compound, which comprises orally administering the pharmaceutical compound to a mammal in need of treatment with the compound concurrently with an essential oil or essential oil component in an amount sufficient to provide bioavailability of the compound in the presence of the essential oil or essential oil component greater than bioavailability of the compound in the absence of the essential oil or essential oil component, wherein the essential oil or essential oil component has an activity of at least 10% inhibition at a concentration 0.01 wt.% or less in an assay that measures reduced conversion of cyclosporine to hydroxylated products using an assay system containing 250 mu g rat liver microsomes, 1 mu M cyclosporine and 1 mM reduced nicotinamide adenine dinucleotide phosphate (NADPH) in 1 ml of 0.1 M sodium phosphate buffer, pH 7.4.

Abstract translation: 一种用于提高口服给药的疏水性药物化合物的生物利用度的方法，其包括将药物化合物口服给需要用精油与精油成分同时处理的哺乳动物，其量足以提供化合物的生物利用度 在不存在精油或精油成分的情况下，精油或精油成分的存在大于化合物的生物利用度，其中精油或精油成分在0.01重量％的浓度下具有至少10％的抑制活性 在使用含有250μg大鼠肝微粒体，1μM环孢菌素和1mM还原型烟酰胺腺嘌呤二核苷酸磷酸（NADPH）的测定系统测量环孢菌素转化为羟基化产物的测定中，％或更少，在1ml 0.1M钠 磷酸盐缓冲液，pH 7.4。