A dermatological topical preparation such as a cream, a lotion, an emulsion, a paste, an ointment and the likes where a lipo-dissolving emulsifier such as a biliary compound is transdermally delivered through the superficial layers of the skin into the subcutaneous adipose tissue with the use of skin permeability enhancers. Some of these skin permeability enhancers are cyclodextrins, while others are substances which have the peculiar property of enhancing delivery of the lipo-dissolving substance locally into the adipose subcutaneous tissue maximizing subcutaneous uptake while minimizing systemic absorption in order to achieve maximization of local effect.
Dissolution of arterial cholesterol plaques by pharmacological preparation
申请人:Zadini P. Filiberto
公开号:US20070116754A1
公开(公告)日:2007-05-24
A pharmacological substance namely a biliary salt or acid or precursor or derivative with emulsifying properties administered into the systemic circulation of a patient via a variety of routes of administration including topical-mucous membrane such as sublingual, topical-dermatological such as via a skin patch, intravenous, subcutaneous, rectal, intramuscular, intradermal, inhalatory in form of inhaled microcrystals, intrarterial, systemic, or via specialized catheter for in loco delivery of the substance, said substance being capable of crossing the fibrous cap of the atherosclerotic plaque to reach and dissolving with its emulsifying properties the cholesterol aggregates and in general the lipidic core within the plaque. The solubilized cholesterol exits the plaque and enters finely dissolved into the systemic circulation leaving behind a plaque emptied of its lipid content: the plague appears as a virtual cavity roofed by the fibrous cap. As a result of this pharmacological action upon the atherosclerotic plaque by the compound, the plaque is no longer vulnerable to rupture and arterial flow is restituted to physiological pre-plaque formation values. This effect on the lipid core of the plaque is expected to reduce and/or eliminate altogether preexisting atherosclerotic lesions and significantly reduce chances of acute and chronic ischemic events.
DISSOLUTION OF ARTERIAL PLAQUE
申请人:ZADINI Filiberto
公开号:US20080187569A1
公开(公告)日:2008-08-07
Embodiments of methods of treating atherosclerosis are described. In some embodiments an emulsifier is provided to achieve levels in the systemic circulation that are effective to solubilize atherosclerotic plaque, resulting in plaque regression. In some embodiments, levels of greater than 50 μM are achieved; in some embodiments levels ranging from about 100 μM to about 600 μM are achieved; in some embodiments, levels ranging from about 100 μM to about 300 μM are achieved. Emulsifiers can include bile salts, saponins, and ionic, nonionic, and zwitterionic detergents, or salts, conjugates, hydrates, solvates, or polymorphs thereof. In some embodiments, a statin can be administered simultaneously or sequentially with an emulsifier.
Dissolution of Arterial Cholesterol Plaques by Pharmacologically Induced Elevation of Endogenous Bile Salts
申请人:Zadini Filiberto P.
公开号:US20080287429A1
公开(公告)日:2008-11-20
A group of pharmaceutical substances induce elevation of endogenous bile salts and acids via different mechanisms. The elevated circulating bile salts exert a beneficial effect in atherosclerosis by acting both as atherolytic and antiatherogenic agents. The result of the elevated circulating endogenous bile salt is the dissolution of cholesterol/lipidic aggregates of the atherosclerotic plaques.