Cholinesterase inhibitors in liposomes and their preparation...

A - Human Necessities – 61 – K

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A61K 9/127 (2006.01)

Patent

CA 2563861

The invention relates to a pharmaceutical composition based on an active ingredient that is enclosed in liposomes for topical, transdermal application. The interior of said liposomes comprises an acidic, aqueous medium containing at least one cholinesterase inhibitor, preferably from the group containing donepezil, rivastigmine, galantamine, physostigmine, heptylphysostigmine, phenserine, tolserine, cymserine, thiatolserine, thiacymserine, neostigmine, huperzine, tacrine, metrifonate and dichlorvos, or an enantiomer or derivative of at least one of said compounds. In addition, the invention relates to a method for producing said composition, optionally in a sterile form and also to the use of the liposomes charged with the active ingredient in various galenic formulations for topical, transdermal application with a depot effect in the epidermis, for the prophylaxis and/or treatment of cutaneous neuropathic pain or the loss of cutaneous sensory function as a result of neuropathy.

L'invention concerne une composition pharmaceutique à base d'un principe actif inclus dans des liposomes destinés à une application topique, transdermique. Les liposomes présentent à l'intérieur un milieu aqueux acide et, dans ce dernier, au moins un inhibiteur de la cholinestérase, sélectionné de préférence dans le groupe comprenant les composés suivants: donepézil, rivastigmine, galantamine, physostigmine, heptylphysostigmine, phensérine, tolsérine, cymsérine, thiatolsérine, thiacymsérine, néostigmine, huperzine, tacrine, métrifonate et dichlorvos, ou un énantiomère ou dérivé d'au moins un de ces composés. L'invention concerne également un procédé de production de cette composition, éventuellement sous forme stérile, ainsi que l'utilisation des liposomes chargés de principe actif dans différentes formulations galéniques destinées à une application topique transdermique à libération prolongée dans l'épiderme, pour la prophylaxie et/ou la thérapie de la douleur neuropathique dermique ou de la perte de la fonction sensorielle dermique due à une neuropathie.

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