Sublingual drug formulations having combined rapid onset of...

A - Human Necessities – 61 – K

Patent

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A61K 45/08 (2006.01) A61K 31/135 (2006.01) A61K 47/12 (2006.01) A61K 47/26 (2006.01) A61K 47/36 (2006.01)

Patent

CA 2243983

The invention relates to sublingual drug formulations containing active ingredients in dosages equal to or near standard oral dosages. A portion of sublingual form is sublingually absorbed and the remaining portion of the same is absorbed mainly by the enteral route. These formulations have a more rapid onset of action than and a termination of action similar to that of oral forms. As a result, the pharmacological effect is prolonged (almost doubled). Overall total bioavailability is the same as for oral forms. Formulations useful in the treatment of allergy and asthma are disclosed. They comprise at least one of the following: a .beta.2-mimetic, a corticosteroid, an anti-H1 histamine, an anti-cholinergic, a xanthine derivative, a non-steroid anti-inflammatory agent, an anti-leukotriene and a mast cell stabilizer.

L'invention a trait à des formulations pharmaceutiques sublinguales contenant des ingrédients actifs à des doses égales ou presque égales aux doses orales standard. Une partie de la forme sublinguale est absorbée sous la langue et le reste est absorbée surtout par la voie intestinale. Ces formulations ont un délai d'action plus rapide et une durée d'action comparable à celle des formes orales. Il en résulte donc que l'effet pharmacologique est prolongé (presque double). La biodisponibilité totale est essentiellement la même que dans le cas des formes orales. Des formulations pouvant être utilisées dans le traitement de l'allergie et de l'asthme sont divulguées. Elles comprennent au moins une des substances suivantes : un bêta.2mimétique, un corticostéroïde, un anti-H1 histamine, un anticholinergique, un dérivé de la xanthine, un anti-inflammatoire non stéroïdien, un anti-leucotriène et un stabilisateur de mastocytes.

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