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Hovey Et Al. (45) Date of Patent: *May 26, 2015 USOO9040O88B2 (12) United States Patent (10) Patent No.: US 9,040,088 B2 Hovey et al. (45) Date of Patent: *May 26, 2015 (54) NANOPARTICULATE MEGESTROL (2013.01); A61 K9/10 (2013.01); A61K 9/145 FORMULATIONS (2013.01); A61 K9/146 (2013.01); A61 K3I/57 (2013.01); A61K 45/06 (2013.01); A61K47/20 (71) Applicant: Alkermes Pharma Ireland Limited, (2013.01); A61 K47/32 (2013.01); A61K47/38 Dublin 4 (IE) (2013.01); A61 K9/08 (2013.01); A61 K3I/573 (2013.01); A61 K47/26 (2013.01); A61K47/34 (72) Inventors: Douglas Hovey, Trooper, PA (US); John (2013.01); A61 K47/42 (2013.01) Pruitt, Suwanee; GA (US); Tuula Ryde (58) Field of Classification search Malvern, PA (US) CPC ........................................................ A61 K9/14 See application file for complete search history. (73) Assignee: ALKERMES PHARMA IRELAND LIMITED, Dublin (IE) (56) References Cited (*) Notice: Subject to any disclaimer, the term of this U.S. PATENT DOCUMENTS patent is extended or adjusted under 35 M U.S.C. 154(b) by 0 days. 4,783,484. A 1 1/1988 Violante et al. This patent is Subject to a terminal dis- 4,826,689 A 5, 1989 Violanto et al. claimer. (Continued) (21) Appl. No.: 14/536,517 FOREIGN PATENT DOCUMENTS 1-1. EP O 338 404 10, 1989 (22) Filed: Nov. 7, 2014 EP 338404 A1 * 10, 1989 (65) Prior Publication Data (Continued) US 2015/OO56286 A1 Feb. 26, 2015 OTHER PUBLICATIONS Related U.S. Application Data Office Action dated Sep. 18, 2008, for related U.S. Appl. No. 10/878,623, 16 pgs. (60) Division of application No. 10/878,623, filed on Jun. pg (Continued) 29, 2004, which is a continuation-in-part of application No. 10/412,669, filed on Apr. 14, 2003, now Pat. No. 7,101,576. Primary Examiner — Carlos Azpuru (60) Provisional application No. 60/371,680, filed on Apr. Assistant Examiner — Casey Hagopian 12, 2002, provisional application No. 60/430,348, (74) Attorney, Agent, or Firm — Foley & Lardner LLP filed on Dec. 3, 2002. (57) ABSTRACT (51) Eiki/4 2006.O1 The present invention is directed to nanoparticulate compo A6 IK9/00 30 6. 8: sitions comprising megestrol. The megestrol particles of the compositionp have an effective averagege pparticle size of less (Continued) than about 2000 nm. (52) U.S. Cl. CPC ................. A61 K9/14 (2013.01); A61 K9/0095 29 Claims, 5 Drawing Sheets 1, 5.0 s 4.0 - - 5 3.0 - uo > - 2.0 -8 -- O 10 - - -e- D O. O co- - O 2O 40 60 8O 1 OO Concentration of Active (mg/ml) US 9,040,088 B2 Page 2 (51) Int. C. 6,045,829 A 4/2000 Liversidge et al. A6 IK 9/10 6,068,858 A 5/2000 Liversidge et al. (2006.01) 6,153,225 A 11/2000 Lee et al. A 6LX3/57 (2006.01) 6,165,504 A 12, 2000 Bell A6 IK 45/06 (2006.01) 6,165,506 A 12/2000 Jain et al. A6 IK 47/20 (2006.01) 6,221,400 B1 4/2001 Liversidge et al. 6,264,922 B1 7/2001 Wood et al. A6 IK 47/32 (2006.01) 6,267,989 B1 7/2001 Liversidge et al. A6 IK 47/38 (2006.01) 6,268,356 B1 7/2001 Ragunathan et al. A6 IK9/08 (2006.01) 6,270.806 B1 8/2001 Liversidge et al. A 6LX3/573 6,316,029 B1 1 1/2001 Jain et al. (2006.01) 6,375,986 B1 4/2002 Ryde et al. A6 IK 47/26 (2006.01) 6,428,814 B1 8, 2002 Bosch A6 IK 47/34 (2006.01) 6,431,478 B1 8, 2002 Reed et al. A6 IK 47/42 (2006.01) 6.432,381 B2 8/2002 Liversidge et al. 6,593,318 B2 7/2003 Ragunathan References Cited 6,593,320 B2 7/2003 Ragunathan (56) 6,656,505 B2 12/2003 Kundu et al. 6,833,373 B1 12/2004 McKearn et al. 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