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(12) United States Patent (10) Patent No.: US 8,829,005 B2 Abelson Et Al

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(12) United States Patent (10) Patent No.: US 8,829,005 B2 Abelson Et Al USOO8829005B2 (12) United States Patent (10) Patent No.: US 8,829,005 B2 Abelson et al. (45) Date of Patent: Sep. 9, 2014 (54) OPHTHALMC FORMULATIONS OF FOREIGN PATENT DOCUMENTS CETRIZINE AND METHODS OF USE EP O43376.6 A1 6, 1991 EP 0920315 B1 6, 1999 (71) Applicant: Aciex Therapeutics, Inc., Boston, MA RU 2220740 C1 1, 2004 (US) WO WO-9746243 A1 12, 1997 WO WO-9806394 A1 2, 1998 (72) Inventors: Mark Barry Abelson, Andover, MA WO WO-99.152O3 A1 4f1999 (US); Matthew J. Chapin, Amesbury, WO WO-O3O4977O A1 6, 2003 WO WO-2004O66960 A2 8, 2004 MA (US); Paul Gomes, Andover, MA WO WO-2004O69338 A1 8, 2004 (US); George Minno, Windham, NH WO WO-2005030331 A1 4/2005 (US); Jackie Nice, Medford, MA (US) WO WO-2005107711 A2 11/2005 WO WO-2006102494 A2 9, 2006 (73) Assignee: Aciex Therapeutics, Inc., Boston, MA WO WO-2007 117971 A2 10/2007 (US) OTHER PUBLICATIONS (*) Notice: Subject to any disclaimer, the term of this patent is extended or adjusted under 35 Berger et al., “Effects of adjuvant therapy with 0.1% olopatadine U.S.C. 154(b) by 0 days. hydrochloride ophthalmic solution on quality of life in patients with allergic rhinitis using systemic or nasal therapy'. Ann. Allergy (21) Appl. No.: 13/899,321 Asthma Immunol. 95(4):361-371 (2005). Lanier et al., Comparison of the Efficacy of Combined Fluticasone (22) Filed: May 21, 2013 Propionate and Olopatadine Versus Combined Fluticasone Propionate and Fexofenadine for the treatment of Allergic (65) Prior Publication Data Rhinoconjunctivitis Induced by Conjunctival Allergen Challenge, Clin. Ther. 24(7): 1161-1174 (2002). US 2013/O252971 A1 Sep. 26, 2013 Ousler et al., “An evaluation of the ocular drying effects of 2 systemic antihistamines: loratadine and cetirizine hydrochloride'. Ann. Allergy Asthma Immunol. 93(5):460-464 (2004). Related U.S. Application Data Spangler et al., “Randomized, Double-Masked Comparison of Olopatadine Ophthalmic Solution, Mometasone Furoate (62) Division of application No. 12/724,128, filed on Mar. Monohydrate Nasal Spray, and Fexofenadine Hydrochloride Tablets 15, 2010. Using the Conjunctival and Nasal Allergen Challenge Models”. Clin. (60) Provisional application No. 61/161,006, filed on Mar. Ther. 25(8):224.5-2267 (2003). 17, 2009, provisional application No. 61/174,850, Abelson et al., “A Randomized, Double-Blind, Parallel-Group Com parison of Olopatadine 0.1% Ophthalmic Solution Versus Placebo filed on May 1, 2009. for Controlling the Signs and Symptoms of Seasonal Allergic Int. C. Conjuctivitis and Rhinoconjunctivitis', Clinical Therapeutics, (51) 25(3):931-947 (2003). A6 IK3I/495 (2006.01) Crampton et al., “A Comparison of the Relative Clinical Efficacy of (52) U.S. C. a Single Dose of Ketotifen Fumarate 0/025% Ophthalmic Solution USPC ..................................................... S14/255.04 Versus Placebo in Inhibiting the Signs and Symptoms of Allergic (58) Field of Classification Search Rhinoconjunctivitis as Induced by the Conjunctival Allergen Chal USPC ..................................................... 514/255.04 lenge Model”, Clinical Therapeutics, 24(11): 1800-1808 (2002). See application file for complete search history. Goodman and Gilman's The Pharmacological Basis of Therapeutics (Tenth Edition) (2001), McGraw Hill, Chapter 1, pp. 3-29. (56) References Cited United States Pharmacopeia (http://en.wikipedia.org/wiki/United States Pharmacopeiai Product quality.E2.80.93 standards and U.S. PATENT DOCUMENTS verification) assessed from the internet on Oct. 22, 2012. 4,407,791 A 10, 1983 Stark 4,525,358 A 6, 1985 Baltes Primary Examiner — Zohreh Fay 5,188,826 A 2, 1993 Chandrasekaran et al. 5,419,898 A 5/1995 Ikejiri et al. (74) Attorney, Agent, or Firm — Cooley LLP 5,698,558 A 12/1997 Gray 6,103,735 A 8/2000 Aslanian et al. 6,436,924 B2 8/2002 Poppe et al. (57) ABSTRACT 6,649,602 B1 1 1/2003 Yanni 6,827,946 B2 12/2004 Hirsh The present invention provides stable topical formulations of 2002fOO37297 A1 3/2002 Crespo et al. 2004/0198743 A1 10/2004 Hey et al. cetirizine that provide a comfortable formulation when 2004/O198828 A1 10, 2004 Abelson et al. instilled in the eye and is effective in the treatment of allergic 2005/02397.45 A1 10, 2005 Abelson et al. conjunctivitis and/or allergic conjunctivitis. The invention 2006.0025391 A1 2/2006 Lulla et al. further provides methods of treating allergic conjunctivitis 2006,0183698 A1 8, 2006 Abelson and/or allergic rhinoconjunctivitis in a Subject in need of such 2006/0216353 A1 9/2006 Liversidge et al. 2006/0228.306 A1 10, 2006 Lane treatment by topical application of the cetirizine formulations 2007/0020330 A1 1/2007 Dang et al. of the invention directly to the eye. 2007/0275974 A1 11, 2007 Fanara et al. 2008/0085922 A1 4/2008 Raja et al. 2008/0254029 A1 10, 2008 Yanni et al. 8 Claims, 31 Drawing Sheets U.S. Patent Sep. 9, 2014 Sheet 1 of 31 US 8,829,005 B2 OVO?sod(u?uu)au]] N O l.9£0 V- La 9°), O (eleos v-O) seloos fuuo Jeno OueeN U.S. Patent Sep. 9, 2014 Sheet 2 of 31 US 8,829,005 B2 S?JOOSSS3up3}}|e^??oun?uoo:g]eun61-I pVO-?sod(u?uu)?uu?L (eleos 7-0) euopS SSeupe lemounuoo ueeW U.S. Patent Sep. 9, 2014 Sheet 4 of 31 US 8,829,005 B2 6u?uÐ?JOS:u6?s?GÁpn?S:\/9?un61-I ??s?A(OAeq)WZ\ISIA!(T-I?SIA(OAeq)az U.S. Patent Sep. 9, 2014 Sheet 5 of 31 US 8,829,005 B2 U.S. Patent US 8,829,005 B2 - W ad U.S. Patent US 8,829,005 B2 v La -------------7 ele OS (7-O) SS 8 up 9 |e All 0 unu O Oueo 0 W U.S. Patent Sep. 9, 2014 Sheet 8 of 31 US 8,829,005 B2 ) t on led r- l cN8 e 9 s (O) fullre- 8 MS pil Ueees W U.S. Patent Sep. 9, 2014 Sheet 9 of 31 US 8,829,005 B2 (&#7||SI/\)uo?s?6uOO[eseN:Áueu]])':/eun61 ele OS (7-0) U OS 8 fu O 9 |ese Nu e 8 W U.S. Patent Sep. 9, 2014 Sheet 10 of 31 US 8,829,005 B2 I N. I Sue a NS U.S. Patent Sep. 9, 2014 Sheet 11 of 31 US 8,829,005 B2 |- || | | OZ (Ey??SI/\)Sseup?>Kue|O:ÁJepuoO3S:6eun61-I Ya r a 23 s (7-0) ssa up a y i. eIO Uee W U.S. Patent Sep. 9, 2014 Sheet 12 of 31 US 8,829,005 B2 (g?7??SIA)Sseupe,Ieue|Os|dE:ÁJepu000SIOL?un61-I r ele OS (7-0) SSaupe eje) S due 0 W U.S. Patent Sep. 9, 2014 Sheet 13 of 31 US 8,829,005 B2 (&#7||SIA)SISOUue?O:ÁuepuoO3S:L??In6|- La Y Widele OS (to) SIS O we 40 ue aw U.S. Patent Sep. 9, 2014 Sheet 14 of 31 US 8,829,005 B2 (giz??SI/\)SÐÁEÁJe?eN\:ÁJepuoo?S:z],eun61-I L Y ele OS (-0) Se A Aua e M u e a w U.S. Patent Sep. 9, 2014 Sheet 15 of 31 US 8,829,005 B2 U.S. Patent US 8,829,005 B2 ele OS (7 O) ee J. Ouy Lee N U.S. Patent Sep. 9, 2014 Sheet 17 of 31 US 8,829,005 B2 (87||S!/\)S??unude?e|edJoJeE:G|?Jnfil ele OS (O) Sdn. d 8 eled J O Jeue 0 W U.S. Patent Sep. 9, 2014 Sheet 18 of 31 US 8,829,005 B2 (gº?ISIA)SI??unudleseN:9)?Ln6|- _º2*SEONBHBHAIGINVOLJINOISATIVOINITO lo s w ele3S (v-o) S} n es e N 20 w U.S. Patent Sep. 9, 2014 Sheet 19 of 31 US 8,829,005 B2 | N ) infil[eseNIe?oL:/Le?JOOS||SI/\)(G# | c do co r on Cd St SN ver ele OS (9-0) 8 JSO duu O Olese Nel O. ue 0 W U.S. Patent Sep. 9, 2014 Sheet 20 of 31 US 8,829,005 B2 tolence g I is is N S ..I O O 3 Z E CC do É D S s O S Li H. I U.S. Patent Sep. 9, 2014 Sheet 21 of 31 US 8,829,005 B2 Mean 96 of Baseline PNF %96 %06 %98 %0,1 |----- || 0960 U.S. Patent Sep. 9, 2014 Sheet 22 of 31 US 8,829,005 B2 ?JOOS?JO?uuOOdOJCIZ??SI/\:OZ?un61– co --- d r se (ele O S OO) 8 O 3 S J 0. woo tie aw d U.S. Patent Sep. 9, 2014 Sheet 23 of 31 US 8,829,005 B2 ?un61-I??SI/\:LZ?JOOS?JO?uuOOdouC]© (eleos 0-0) aloo Suoguoo ueeN U.S. Patent Sep. 9, 2014 Sheet 24 of 31 US 8,829,005 B2 SILNE/\EESHE/\CIV-ÅLEHVSIZZ?un61– U.S. Patent Sep. 9, 2014 Sheet 25 Of 31 US 8,829,005 B2 | | | | | s F-----r i s o N- d v cy N v- C s e r w- wa va was t- re (6Huu) dOl U.S. Patent Sep. 9, 2014 Sheet 26 of 31 US 8,829,005 B2 SqSouleupE ein61vz (eleoS 7-0) alooseous U.S. Patent Sep. 9, 2014 Sheet 27 Of 31 US 8,829,005 B2 GZ?un61– (eleost-0) euooSeoulio eaeue NW U.S. Patent Sep. 9, 2014 Sheet 28 of 31 US 8,829,005 B2 9Z?un61– n (eleos 7-0) eluooSeoulo eaeue NW U.S.
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