Title:
経口用ペプチド薬剤
Document Type and Number:
Japanese Patent JP3549542
Kind Code:
B2
Abstract:
A pharmaceutical compositions for oral delivery of physiologically active peptide agents comprises: (a) active peptide; (b) pH-lowering agent(s), present in a quantity that, if added to 0.1 M aqueous sodium bicarbonate solution (10 ml), would be sufficient to lower the pH of the to solution to \~ 5.5.; (c) absorption enhancer(s) effective in promoting bioavailability of the agent, and (d) acid-resistant protective vehicle effective to transport the composition through the stomach of the patient while preventing contact between the active peptide and stomach proteases. (c) is a surfactant, which is preferably absorbable or biodegradable, especially an acylcarnitine, phospholipid or bile acid, and the composition preferably further contains (e) a sucrose ester. (c) is a surfactant chosen from an anionic agent that is a cholesterol derivative, a mixture of a negative charge neutraliser and an anionic surfactant, a non-ionic surfactant or a cationic surfactant. The composition includes \- 2 (c), one of which is a cationic surfactant and another of which is an anionic surfactant that is a cholesterol derivative, e.g. a water-soluble bile acid. The composition is a solid dosage form with a wt. ratio of (b) to (c) being 5:1-10:1. (b) is chosen from citric acid, tartaric acid and an acid salt of an amino acid. (b) is present in an amount \~ 300 (preferably 400) mg. (a) is vasopressin, salmon calcitonin or insulin. (d) is viscous protective syrup.
Inventors:
Stern, william
Jilligan, James Pee
Jilligan, James Pee
Application Number:
JP53285997A
Publication Date:
August 04, 2004
Filing Date:
March 14, 1997
Export Citation:
Assignee:
Unigene Laboratories, Inc.
International Classes:
A61F2/00; A61K9/16; A61K9/28; A61K9/30; A61K9/36; A61K9/00; A61K9/48; A61K9/50; A61K9/52; A61K9/62; A61K38/00; A61K38/095; A61K38/23; A61K38/28; A61K47/18; A61K47/24; A61K47/28; A61P19/08; A61P19/10; (IPC1-7): A61K38/23; A61K9/00; A61K38/11; A61K38/28; A61K47/24
Domestic Patent References:
| JP2040320A | ||||
| JP2022222A | ||||
| JP60239427A | ||||
| JP63096138A | ||||
| JP5148154A |
Foreign References:
| WO1995025534A1 |
Other References:
Advanced Drug Delivery Review,Vol.8,No.1(1992年)P.3
Attorney, Agent or Firm:
Aoyama Aoi
Kazuaki Kojima
Kazuaki Kojima