Nanoparticles comprising a non-ionizable cellulosic polymer and an amphiphilic non-ionizable block copolymer

摘要

A pharmaceutical composition comprises nanoparticles comprising a poorly water-soluble drug, a poorly aqueous soluble non-ionizable cellulosic polymer, and a poorly aqueous soluble polymeric amphiphilic non-ionizable block copolymer.

主权项

1. A pharmaceutical composition comprising nanoparticles, said nanoparticles consisting of:
(a) a drug having a solubility in water of less than 5 mg/mL over the pH range of 6.5 to 7.5 at 25° C., at least 90 wt % of said drug being non-crystalline; (b) a poorly aqueous soluble non-ionizable cellulosic polymer selected from the group consisting of ethylcellulose, cellulose acetate, cellulose propionate, cellulose butyrate, cellulose acetate butyrate, and mixtures thereof; and (c) a poorly aqueous soluble polymeric amphiphilic non-ionizable block copolymer, wherein the amphilphilic non-ionizable copolymer is poly(ethylene oxide-b-ε-caprolactone);wherein said nanoparticles have an average size of less than 500 nm; and comprise from 1 wt % to 80 wt % said drug, from 10 wt % to 75 wt % said non-ionizable cellulosic polymer, and from 5 wt % to 60 wt % said amphiphilic non-ionizable block copolymer.