Transnasal anticonvulsive pharmaceutical composition...

A - Human Necessities – 61 – K

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A61K 9/08 (2006.01) A61K 31/19 (2006.01) A61K 31/325 (2006.01) A61K 31/5513 (2006.01) A61P 25/08 (2006.01)

Patent

CA 2723649

There is provided a transnasal anticonvulsive pharmaceutical composition including a poorly soluble anticonvulsant. The anticonvulsive pharmaceutical composition comprising a poorly soluble anticonvulsant as an active component, which is transnasally spray- administered, comprises diethylene glycol monoethyl ether and fatty acid ester, wherein the fatty acid ester is selected from the group consisting of caprylocaproyl polyoxylglyceride, isopropyl palmitate, oleoyl polyoxylglyceride, sorbitan monolaurate 20, methyl laurate, ethyl laurate, and polysorbate 20. Also, the anticonvulsive pharmaceutical composition comprising a poorly soluble anticonvulsant as an active component, which is transnasally spray-administered, comprises diethylene glycol monoethyl ether, fatty acid ester, methylpyrrolidone, water and alcohol. Therefore, the transnasal anticonvulsive pharmaceutical composition may be useful to highly enhance the bioavailability of the poorly soluble anticonvulsant. Also, the transnasal anticonvulsive pharmaceutical composition may be useful to allow the poorly soluble anticonvulsant to show the improved viscosity and/ or enhanced solubility in order to effectively deliver the poorly soluble anticonvulsant at a therapeutic dose.

L'invention concerne une composition pharmaceutique anticonvulsive transnasale comprenant un anticonvulsivant faiblement soluble. La composition pharmaceutique anticonvulsive comprenant un anticonvulsivant faiblement soluble en tant que composant actif, qui est administré par pulvérisation transnasale, comprend du diéthylène glycol monoéthyl éther et de l'ester d'acides gras, l'ester d'acides gras étant sélectionné dans le groupe constitué de polyoxylglycéride de caprylocaproyle, de palmitate d'isopropyle, de polyoxylglycéride d'oléoyle, de monolaurate de sorbitan 20, de laurate de méthyle, de laurate d'éthyle et de polysorbate 20. La composition pharmaceutique anticonvulsive comprenant un anticonvulsivant faiblement soluble en tant que composant actif, qui est administrée par pulvérisation transnasale, comprend également du diéthylène glycol monoéthyl éther, de l'ester d'acides gras, de la méthylpyrrolidone, de l'eau et de l'alcool. Par conséquent, la composition pharmaceutique anticonvulsive transnasale peut être utile pour améliorer fortement la biodisponibilité de l'anticonvulsivant faiblement soluble. La composition pharmaceutique anticonvulsive transnasale peut en outre être utile pour permettre à l'anticonvulsivant faiblement soluble de présenter la viscosité améliorée et/ou la solubilité accrue afin d'administrer efficacement l'anticonvulsivant faiblement soluble à une dose thérapeutique.

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