Preparation of pharmaceutical compositions
AssigneePhares Pharmaceutical Research N.V.
InventorsSteven Leigh, Mathew Louis Steven Leigh
Life of this patent
Estimating the term…
Abstract
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.
Claims46
A method for delivering a biologically active lipophilic compound to a living organism, which comprises administering orally to said organism a substantially homogeneous composition comprising said biologically active lipophilic compound, a blend of at least one diacyl phospholipid and at least onto monoacyl phospholipid which is derived from a partial enzyme digestion of diacyl phospholipids, said blend having a monoacyl phospholipid:diacyl phospholipid molar ratio of between 1:10 and 10:1, and said monoacyl phospholipid being a micelle-forming lipid,and not more than 10% by weight of water, the lipophilic compound being dissolved in or associated with said blend, wherein upon contact with aqueous fluid said composition spontaneously forms discrete lipid aggregates, which aggregates together with said associated biologically active lipophilic compound are sized to pass through a 200 nm pore size filter.
A substantially homogeneous composition for delivering a biologically active lipophilic compound orally to a living organism, said composition comprising
- a blend of at least one diacyl phospholipid and at least one monoacyl phospholipid said blend being derived from a partial enzyme digestion of diacyl phospholipids and having a monoacyl phospholipid:diacyl phospholipid molar ratio of between 1:10 and 10:1, and said monoacyl phospholipid being a micelle-forming lipid,
- not more than 10% by weight of water, and
- a biologically effective amount of said biologically active lipophilic compound being associated with said blend,
- wherein upon contact with aqueous fluid said composition spontaneously forming discrete lipid aggregates, which aggregates together with said associated biologically active lipophilic compound are sized to pass through a 200 nm pore size filter.
A composition for delivering a biologically active lipophilic compound orally to a living organism, said composition comprising
- a blend of at least one diacyl phospholipid and at least one monoacyl phospholipid said blend being derived from a partial enzyme digestion of diacyl phospholipids and having a monoacyl phospholipid:diacyl phospholipid molar ratio of between 1:10 and 10:1, and said monoacyl phospholipid being a micelle-forming lipid,
- not more than 10% by weight of water, and
- a biologically active lipophilic compound being associated with said blend, wherein upon contact with aqueous fluid said composition spontaneously forming discrete lipid aggregates, which aggregates together with said associated biologically active lipophilic compound are sized to pass through a 200 nm pore size filter.
Dependencies are inferred from the claim text.