Compositions and methods for improved delivery of ionizable...

A - Human Necessities – 61 – K

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A61K 47/02 (2006.01) A61K 9/14 (2006.01) A61K 9/48 (2006.01)

Patent

CA 2366702

The present invention is directed to a pharmaceutical composition including a hydrophobic therapeutic agent having at least one ionizable functional group, and a carrier. The carrier includes an ionizing agent capable of ionizing the functional group, a surfactant, and optionally solubilizers, triglycerides, and neutralizing agents. The invention further relates to a method of preparing such compositions by providing a composition of an ionizable hydrophobic therapeutic agent, an ionizing agent, and a surfactant, and neutralizing a portion of the ionizing agent with a neutralizing agent. The compositions of the invention are particularly suitable for use in oral dosage forms.

L'invention concerne une composition pharmaceutique comprenant un agent thérapeutique hydrophobe possédant au moins un groupe fonctionnel ionisable, et un porteur. Ce dernier comporte un agent ionisant capable d'ioniser le groupe fonctionnel, un agent de surface, et facultativement des agents solubilisants, des triglycérides, et des neutralisants. L'invention concerne, en outre, un procédé de préparation de ces compositions en produisant une composition d'un agent thérapeutique hydrophobe ionisable, un agent ionisant, et un agent de surface, et en neutralisant une partie de l'agent ionisant avec un neutralisant. Les compositions de cette invention sont particulièrement appropriées à des formes galéniques buccales.

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