Phares Pharmaceutical Research, N.v.

Phares Technology Bv

Steven Leigh

Mathew Louis Steven Leigh

Peter J Ayres

Caroline Mary Thompson

Mathew L S Leigh

Mathew Louis Leigh

A composition in the form of a dry powder and which comprises: a) at least one membrane lipid, and b) at least one biologically active compound comprising a xanthine and/or a carboxylic acid, and which forms structured lipid assemblies when dispersed/dissolved in an aqueous medium. A method of preparing such a composition is also provided, together with a dispersion of structured lipid assemblies suspended in a solution of at least one biologically active compound and a method of preparing the same. The compositions and dispersions are suitable for use in creams and lotions for skin care.

Membrane lipid compositions

The invention provides a composition for delivering at least one biologically active compound to a living organism, said composition comprising at least one micelle-forming membrane lipid

Pharmaceutical compositions and their use

A substantially homogeneous composition for human administration comprises a biologically active lipophilic compound dissolved in or associated with at least one micelle-forming lipid. For example, cyclosporin A is dissolved or dispersed in the mixture of PC and MAPC. The composition may be made by dissolving the lipid material in ethanol, adding the lipophilic compound to the ethanol and removing the ethanol, after which the composition may be formulated for human oral administration.

Preparation of pharmaceutical compositions

Compositions that are sprayable or that are in the form of discrete particles and that contain a lipid and a biologically active compound in the form of a micronized powder combine a high initial entrapment of the active compound in the membrane lipid with sustained release at the site of application as indicated by in-vitro and in-vivo tests. In a first form pro-liposomes are prepared by spraying under pressure through a nozzle a single composition comprising at least one volatile liquid propellant, at least one membrane lipid that is at least partly dissolved or dispersed in the propellant and at least one biologically active compound that is present in dispersion in the propellant and/or the lipid, the composition being free from other solvent for the lipid. In a second form the membrane lipid and the biologically active compound are minor components of micronized solid particles whose major component is a physiologically acceptable solid carrier.

Methods of preparing pro-liposome dispersions and aerosols

Pro-liposome compositions comprise membrane lipids such as lecithin or distearyl dimethylammonium chloride, water-miscible solvents such as ethanol, optionally a minor proportion of water, and optionally fatty acid esters and drugs. On addition to excess water they spontaneously form dispersions of liposomes having high void volumes and high drug entrapment ratios. Aerosol compositions are presented in a volatile liquid propellant. On being sprayed they form an aerosol of droplets which, on contact with aqueous media, spontaneously form liposome dispersions.

Pro-liposome compositions

Pharmaceutical compositions for application topically or by suppository comprise:

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London, United Kingdom

Steven Leigh