GB2497728A — Statin formulations for transmucosal delivery

USPTO Abstract

A pharmaceutical composition for the transmucosal delivery of a stain comprises a statin and a carrier in which the statin is soluble or forms a suspension or emulsion. The statin may be lipophilic, preferably selected from simvastatin, atorvastatin, lovastatin, pitavastatin or a salt thereof, and the carrier may be an oil that comprises a glyceride wherein the statin is solubilised in the carrier. Alternatively, the lipophilic statin may be combined with an aqueous carrier where the statin is suspended or emulsified in the carrier. The statin may also be hydrophilic, preferably selected from fluvastatin, pravastatin, rosuvastatin or a salt thereof and the carrier may be an aqueous solution where the statin is solubilised in the carrier provided that if the statin is pravastatin then the composition has a pH of at least 8 and is substantially free of ethanol. Alternatively, the hydrophilic statin may be combined with an oil carrier comprising a glyceride, wherein the statin is suspended or emulsified in the carrier, provided that if the statin is pravastatin then the composition is substantially free of ethanol. Preferably, the oil carrier is medium chain triglyceride or a macrogolglyceride, in particular, caprylocaproyl macrogolglyceride. Preferably, the formulation is delivered buccally or sublingually. A pharmaceutical composition comprising a statin for use in inhibiting cholesterol synthesis in vivo, wherein the composition is delivered via the transmucosal route is also outlined.