A - Human Necessities – 61 – K
Patent
A - Human Necessities
61
K
A61K 35/50 (2006.01) A61K 31/165 (2006.01) A61K 31/522 (2006.01) A61K 31/575 (2006.01) A61K 31/58 (2006.01) A61K 39/395 (2006.01) A61K 39/40 (2006.01) A61K 39/42 (2006.01) A61K 39/44 (2006.01) A61P 9/04 (2006.01) A61P 31/12 (2006.01) A61P 43/00 (2006.01) C07J 41/00 (2006.01) A61K 47/48 (2006.01)
Patent
CA 2405151
Many compounds have poor bioavailability or variable bioavailability because of poor absorption of the compound in the small intestine. Conjugation of the compound with bile acid to form a prodrug will increase the bioavailibility of the compound and/or reduce the bioavailability variability of the compound because of the active transport of the prodrug by the intestinal bile acid transporter and because of increased lipophilic nature of the prodrug. A linker group can be used between the bile acid and the compound. One example of a bile acid containing prodrug is acyclovir valylchenodeoxycholate, where valine is the linker group. Another example of this prodrug is atenolol cholic acid amide.
De nombreux composés présentent une biodisponibilité médiocre ou variable du fait de la difficulté d'absorption du composé dans l'intestin grêle. La conjugaison du composé avec l'acide biliaire pour obtenir un promédicament augmente la biodisponibilité du composé et/ou réduit la variabilité de la biodisponibilité du composé du fait du transport actif du promédicament par le transporteur de l'acide biliaire dans l'intestin et du fait du caractère lipophile accru du composé. Un exemple de promédicament contenant l'acide biliaire est l'acyclovir valylchénodésoxycholate, la valine étant le groupe de liaison. Un autre exemple de ce type de promédicament est l'amide d'acide cholique aténolol.
Coop Andrew
Lentz Kimberley A.
Maeda Dean Y.
Polli James E.
Coop Andrew
Gowling Lafleur Henderson Llp
Lentz Kimberley A.
Maeda Dean Y.
Polli James E.
LandOfFree
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