活性剤を送達するための二ナトリウム塩、一水和物、およびエタノール溶媒和物

Japanese Patent JP4588221

B2

The inventors have discovered that the disodium salt of certain delivery agents has surprisingly greater efficacy for delivering active agents than the corresponding monosodium salt. Furthermore, the inventors have discovered that the disodium salts of these delivery agents form solvates with ethanol and hydrates with water. Preferred delivery agents include, but are not limited to, N-(5-chlorosalicyloyl)-8-aminocaprylic acid (5-CNAC), N-(10-[2-hydroxybenzoyl]amino)decanoic acid (SNAD), and sodium N-(8-[2-hydroxybenzoyl]amino)caprylate (SNAC). The invention also provides methods of preparing the disodium salt, ethanol solvate, and hydrate and compositions containing the disodium salt, ethanol solvate, and/or hydrate.

William E. Bay
Rajesh Kay Agarwal
Kiran Choudary
Singai Majuru
Michael M. Goldberg
Joanne Pie Russo

JP2000609376A

November 24, 2010

April 05, 2000

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Emisfair Technologies Inc.

A61K47/16; A61K9/08; C07C235/60; A61K9/20; A61K9/48; A61K31/726; A61K38/22; A61K47/12; A61K47/18; A61P3/14; A61P7/02; C07C231/00; C07C231/12; C07D265/26; C07C235/58

JP10152441A
JP10507762A
JP2001513080A
JP2002506418A
JP2001524109A

ES369853A1

BAUGHMAN,R.A. et al,Oral delivery of anticoagulant doses of heparin. A randomized, double-blind, controlled study in humans,Circulation,1998年,Vol.98, No.16,p.1610-1615
GONZE,M.D. et al,Orally administered heparin with a carrier agent is therapeutic for deep venous thrombosis treatment,Surgical Forum,1998年,Vol.49,p.335-337

Masatake Shiga
Tadashi Takahashi
Takashi Watanabe
Masakazu Aoyama
Suzuki Mitsuyoshi
Kazuya Nishi
Yasuhiko Murayama
Shinya Mitsuhiro

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