Topical compositions for prostaglandin e1 delivery

A - Human Necessities – 61 – K

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A61K 47/00 (2006.01) A61K 9/00 (2006.01) A61K 31/5575 (2006.01) A61K 47/14 (2006.01) A61K 47/18 (2006.01) A61K 47/36 (2006.01)

Patent

CA 2373821

A composition of a semi-solid consistency is provided for use in the manufacture of a topical medicament for the transdermal application of prostaglandin E1. The composition comprises prostaglandin E1, a penetration enhancer, a polysaccharide gum, a lipophilic compound, and an acidic buffer system. The penetration enhancer is an alkyl-2-(N,N-disubstituted amino)- alkanoate ester, an (N,N-disubstituted amino)-alkanol alkanoate, or a mixture of these. The lipophilic compound may be an aliphatic C1 to C8 alcohol, an aliphatic C8 to C30 ester, or a mixture of these. The composition includes a buffer system capable of providing a buffered pH value for said composition in the range of about 3 to about 7.4. The composition is useful for the manufacture of medicaments for the treatment of erectile dysfunction, female sexual dysfunction and peripheral vascular disease.

L'invention concerne une composition de consistence semi-solide utilisée pour fabriquer un médicament topique permettant une application transdermique de prostaglandine E¿1?. Cette composition renferme de la prostaglandine E¿1?, un agent favorisant la pénétration, une gomme polysaccharidique, un composé lipophile, et un système tampon acide. L'agent favorisant la pénétration est un ester d'alkyl-2-(N,N-amino disubstitué)-alcanoate, un alcanoate de (N,N-amino disubstitué)-alcanole, ou un mélange de ceux-ci. Le composé lipophile peut être un alcool aliphatique C¿1? à C¿8?, un ester aliphatique C¿8? à C¿30?, ou un mélange de ceux-ci. De plus, le système tampon de cette composition est capable de conférer à celle-ci une valeur de pH tamponné qui varie approximativement entre 3 et 7,4. Cette composition peut être utilisée pour fabriquer des médicaments destinés à traiter les troubles de l'érection, les dysfonctionnements sexuels chez la femme, et les maladies péripheriques vasculaires.

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