Liquid filled formulations of pde5 inhibitors
AssigneeMW Encap Limited
InventorsPeter John Scammells, Christopher John Hamilton Porter, Hassan Benameur, Hywel David Williams, Leigh Ford
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Abstract
The instant disclosure provides a composition comprising a capsule and a fill formulation for lipophilic salts of PDE5 inhibitors. Embodiments of the fill formulation contain a liquid, lipid vehicle in which the active ingredient is dissolved and present at relatively high amounts.
Claims18
A composition comprising a capsule and a fill formulation, wherein the fill formulation comprises:
- a. an active ingredient selected from sildenafil, vardenafil, avanafil, udenafil, mirodenafil and lodenafil;
- b. a lipophilic counterion to the active ingredient, the lipophilic counterion being present in an amount of at least 90 mol % of the active ingredient so as to be capable of forming a lipophilic salt of the active ingredient;
- and
- c. a lipid vehicle that is liquid or predominantly liquid at 25° C.;
- wherein the active ingredient is completely dissolved in the lipid vehicle in an amount of at least 1.0 wt % at 25° C. (expressed as free base equivalents) of the fill formulation.
The composition of claim 16 wherein the cosurfactant is selected from the group consisting of:
- propylene glycol mono- and di-esters of C8-C22 fatty acids;
- and sorbitan fatty acid esters.
The composition of claim 17 wherein the oil comprises a C8-C18 fatty acid ester of glycerol.
The composition of claim 17 wherein the amount of surfactant present in the fill formulation is from 10 to 96 wt %, the amount of cosurfactant present in the fill formulation is from 5 to 50 wt %, and the amount of oil present in the fill formulation is from 5 to 50 wt % (where the amount of fill formulation includes the mass of the active ingredient, lipophilic counterion, the lipid vehicle and any other optional excipients).
A composition comprising an active ingredient selected from sildenafil docusate, sildenafil lauryl sulfate, sildenafil decyl sulfate and sildenafil dodecanoate.
Dependencies are inferred from the claim text.