Oral formulation for delivery of poorly absorbed drugs

A - Human Necessities – 61 – K

Patent

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A61K 9/20 (2006.01)

Patent

CA 2595116

A composition for oral delivery of a poorly absorbed drug is disclosed. The composition includes the drug, an enhancer for increasing absorption of the drug through the intestinal mucosa, a promoter, which alone does not increase absorption of the drug through the intestinal mucosa, but which further increases the absorption of the drug in the presence of the enhancer, and optionally a protector for protecting the drug from physical or chemical decomposition or inactivation in the gastrointestinal tract. Illustrative enhancers include sucrose fatty acid esters, and illustrative promoters include aminosugars and amino acid derivatives, such as poly(amino acids). Illustrative protectors include methylcellulose, poly(vinyl alcohol), and poly(vinyl pyrrolidone).

La présente invention concerne une composition permettant l'administration orale d'un médicament faiblement absorbé. Cette composition contient ledit médicament, un agent améliorant permettant d'accroître l'absorption du médicament à travers la muqueuse intestinale, un agent promoteur qui à lui seul n'accroît pas l'absorption du médicament à travers la muqueuse intestinale mais qui favorise l'accroissement de cette absorption du médicament en présence de l'agent améliorant, et éventuellement un agent protecteur conçu pour protéger le médicament d'une décomposition ou inactivation physique ou chimique dans le tractus gastro-intestinal. Les agents améliorants proposés incluent des esters d'acide gras et les agents promoteurs proposés incluent des aminosucres et des dérivés d'acides aminés, du type poly(acides aminés). Les agents protecteurs proposés incluent la méthylcellulose, un poly(alcool de vinyle) et une poly(pyrrolidone de vinyle).

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