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Cholinesterase inhibitors in liposomes and their production and use

A technology of cholinesterase and liposome, which is applied in the field of cholinesterase inhibitor in liposome and its preparation and application, and can solve the problems such as skin sensory dysfunction

Inactive Publication Date: 2007-04-11
SANOCHEMIA PHARMA AG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, the system is not suitable for the treatment of neuropathic pain or the loss of skin sensory function caused by neurodegeneration

Method used

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  • Cholinesterase inhibitors in liposomes and their production and use
  • Cholinesterase inhibitors in liposomes and their production and use
  • Cholinesterase inhibitors in liposomes and their production and use

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Embodiment Construction

[0017] Loading of liposomes with active substances can be divided into two main categories: loading of the membrane and loading of the aqueous phase within the liposome. Since galantamine-base is soluble in ethanol, first attempts were made to integrate the active substance molecules into liposome membranes, however without success. The more galantamine is not encapsulated in the membrane but is removed by filtration, the more galantamine will still be released again from the membrane. The fraction of membrane-bound and unbound galantamine was approximately equal. For this reason, subsequent attempts were made to load the aqueous phase of liposomes with galantamine. This process can be achieved in two ways: through active and passive loading. It has been shown from experiments with passively loaded liposomes with galantamine-HBr / base in PBS solution that stable galantamine-liposome-suspensions cannot thus be prepared. As already in the previous membrane tests, once the unen...

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Abstract

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.

Description

technical field [0001] The present invention relates to pharmaceutical compositions based on cholinesterase inhibitors in liposomes, to the preparation of such compositions, and to the possibility of their therapeutic use. Background of the invention [0002] Central cholinesterase inhibitors are used in the drug treatment of mild and moderately severe Alzheimer's disease to partially restore the cholinergic-stimulatory conduction system in the brain that is reduced by the disease in the context of this syndrome function. New research shows that many cholinesterase inhibitors not only block acetylcholinesterase and butyrylcholinesterase through different mechanisms, but also have direct effects on neuronal nicotinic acetylcholine receptors. These receptors, whose natural ligand is acetylcholine, are found not only on cholinergic nerves, but also in the serotonergic and glutamatergic nervous systems, where they control the release of each neurotransmitter. [0003] This eff...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K9/00
CPCA61K9/127A61P9/00A61P17/00A61P25/00A61P25/02A61P25/28A61P29/00A61P43/00
Inventor A·博登泰克J·伯克曼W·弗朗特西茨E·皮里克A·韦格纳K·沃劳尔-乌尔
Owner SANOCHEMIA PHARMA AG
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