US Patent No. 9,872,848


Patent No. 9,872,848
Issue Date January 23, 2018
Title Stable Formulations For Lyophilizing Therapeutic Particles
Inventorship Greg Troiano, Pembroke, MA (US)
Young-ho Song, Natick, MA (US)
Stephen E. Zale, Hopkinton, MA (US)
James Wright, Lexington, MA (US)
Christina Van Geen Hoven, Cambridge, MA (US)
Assignee Pfizer Inc., New York, NY (US)

Claim of US Patent No. 9,872,848

1. A lyophilized pharmaceutical composition comprising:
polymeric nanoparticles that comprises a poly(lactic) acid-block-poly(ethylene)glycol copolymer or poly(lactic)-co-poly(glycolic)
acid-block-poly(ethylene)glycol copolymer, and a therapeutic agent, wherein the polymeric nanoparticles have a diameter of
about 60 nm to about 140 nm;

a sugar; and
hydroxypropyl ?-cyclodextrin,
wherein upon reconstitution of the lyophilized pharmaceutical composition in an aqueous medium, the reconstituted composition
comprises 10-100 mg/mL concentration of the nanoparticles; 4 to 6 weight percent of the sugar; and 7 to 12 weight percent
of the hydroxypropyl ?-cyclodextrin, and wherein 100 mL of the reconstituted composition comprises less than 6000 microparticles
of greater than or equal to 10 microns; and less than 600 microparticles of greater than or equal to 25 microns.