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(11)    Patent No :    AP 2255   
(21)    Application No :    AP/P/2006/003837   
(22)    Filing Date :    31.05.2005   
(24)    Date of Grant &    21.07.2011   
(45)    Publication :

(30)  Priority Data           
(33) Country    (31)    Number    (32) Date
JP    2004    -163742    01.06.2004

(84)    Designated State

KE   UG   ZW 

(73) Applicant(s)

KABUSHIKI KAISHA YAKULT HONSHA, 1-19, Higashi Shinbashi 1-chome, Minato- ku, Tokyo 1058660, Japan

(72) Inventors

YOSHINO Keisuke, Japan

NOZAWA Shigenori, Japan

ISOZAKI Masashi, Japan

et al

(74) Representative

(51)  International  Classification   A61K 9/127 (2006.01)    A61K 31/4745 (2006.01)
A61K 47/04 (2006.01)   

(54)    Title

Irinotecan preparation.

(58)    Abstract

Provided is an irinotecan formulation capable of supporting irinotecan and/or a salt thereof in a closed vesicle carrier at a high concentration and existing in blood for a long period of time by dramatically improved retentivity in blood compared to a conventionally known irinotecan liposome formulation. That is, an irinotecan formulation including a closed vesicle formed by a lipid membrane, in which irinotecan and/or a salt thereof is encapsulated at a concentration of at least 0.07 mol/mol (drug mol/membrane total lipid mol). There is an ion gradient between an inner aqueous phase and an outer aqueous phase, in the irinotecan formulation. The closed vesicle is preferably liposome, in which only the outer surface of the liposome is preferably modified with a surface-modifying agent containing a hydrophilic polymer.

(56)    Documents Cited :    WO 2003-041681    JP 2002-527466    JP 2001-064158    WO 2004-087104


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