Composition for enhanced uptake of polar drugs from the colon

A - Human Necessities – 61 – K

Patent

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Details

A61K 47/38 (2006.01) A61K 31/70 (2006.01) A61K 38/18 (2006.01) A61K 38/21 (2006.01) A61K 38/22 (2006.01) A61K 47/12 (2006.01) A61K 47/14 (2006.01) A61K 47/34 (2006.01) A61K 48/00 (2006.01)

Patent

CA 2227764

The invention provides a drug delivery composition for colonic delivery comprising a polar drug, an absorption promoter which (a) comprises a mixture of a fatty acid having 6 to 16 carbon atoms or a salt thereof and a dispersing agent, or (b) comprises a mixture of mono/diglycerides of medium chain fatty acids and a dispersing agent, and means adapted to release the polar drug and absorption promoter in the colon following oral administration. A preferred fatty acid is capric acid or a salt thereof. Colon specific delivery can be achieved by providing the composition in a capsule, tablet or pellet which is coated with a material which dissolves in the small intestine or is degraded by the conditions in the colon.

L'invention concerne une composition d'apport colique de médicament, laquelle comprend un médicament polaire, un promoteur d'absorption constitué soit (a) d'un mélange d'un acide gras possédant 6 à 16 atomes de carbone, ou d'un sel de celui-ci, et d'un agent de dispersion, soit (b) d'un mélange de mono/diglycérides d'acides gras à chaînes moyennes et d'un agent de dispersion, ainsi que des moyens conçus pour libérer, dans le côlon, le médicament polaire et le promoteur d'absorption, après administration orale de la composition. Un acide gras préféré est l'acide caprique ou un sel de celui-ci. On obtient cet apport spécifique au niveau du côlon en plaçant la composition dans une gélule, dans un comprimé ou une pastille, lesquels sont revêtus d'un matériau qui se dissout dans l'intestin grêle ou est décomposé par le milieu ambiant du côlon.

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