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(19) United States (12) Patent Application Publication (10) Pub US 20140065203A1 (19) United States (12) Patent Application Publication (10) Pub. N6.: US 2014/0065203 A1 PeresWetoff-Morath et al. (43) Pub. Date: Mar. 6, 2014 (54) ANTIHISTAMINE- AND (60) Provisional application No. 60/712,822, ?led on Sep. CORTICOSTEROID-CONTAINING 1, 2005. LIPOSOME COMPOSITION AND ITS USE FOR THE MANUFACTURE OF A Publication Classi?cation MEDICAMENT FOR TREATING RHINITIS AND RELATED DISORDERS (51) Int. Cl. A61K 31/58 (2006.01) (71) Applicant: BiolipoX AB, Solna (SE) A61K 31/56 (2006.01) A61K 31/4545 (2006.01) (72) Inventors: Lena PeresWetoff-Morath, Solna (SE); A61K 31/4965 (2006.01) Anders Carlsson, Stockholm (SE); (52) U.s. c1. Torbjom Bjerke, Solna (SE) CPC ........... .. A61K 31/58 (2013.01); A61K 31/4965 (2013.01); A61K31/56 (2013.01); A61K (73) Assignee: BiolipoX AB, Solna (SE) 31/4545 (2013.01) (21) App1.No.: 13/954,694 USPC ......................................... .. 424/450; 514/171 (22) Filed: Jul. 30, 2013 (57) ABSTRACT Related US. Application Data There is provided homogeneous pharmaceutical composi tions for the treatment of, for example, rhinitis, asthma and/or (63) Continuation of application No. 11/991,091, ?led on chronic obstructive pulmonary disease comprising a corticos Apr. 10, 2009, ?led as application No. PCT/GB2006/ teroid and an antihistamine, a polar lipid liposome and a 003222 on Aug. 31, 2006. pharmaceutical-acceptable aqueous carrier. US 2014/0065203 A1 Mar. 6, 2014 ANTIHISTAMINE- AND onset of action and feWer side effects. At present, hoWever, CORTICOSTEROID-CONTAINING cetiriZine dihydrochloride is not an approved medicine for LIPOSOME COMPOSITION AND ITS USE local administration, although it has been administered in that FOR THE MANUFACTURE OF A manner in clinical trials. MEDICAMENT FOR TREATING RHINITIS [0010] In one trial (Francillon C, Pécoud A. E?‘ect of nasal AND RELATED DISORDERS spray ofcetirizine in a nasal provocation test with allergen. J. Allergy Clin. Immunol. 1993:91, Suppl. 2:258 (abstract)), FIELD OF THE INVENTION cetiriZine nasal spray Was found to reduce symptoms and [0001] This invention relates to compositions for use in increase nasal peak ?oW after an allergen challenge. Further, methods of treating certain in?ammatory disorders, such as in exercise-induced asthma, a good protective effect Was seen rhinitis, asthma and chronic obstructive pulmonary disease When cetiriZine mist Was administered to the lung With a (COPD), and to processes for the preparation of such com nebuliZer (Ghosh S K, De Vos C, Mcllroy l, Patel K R. E?‘ect positions. ofcetirizine on exercise induced asthma, Thorax 1991 April; 46(4), 242-4). BACKGROUND AND PRIOR ART [0011] Some effect Was seen on symptoms When cetiriZine (presumably as the di-hydrochloride) Was given as a nasal [0002] There are many diseases/disorders that are in?am spray in patients With perennial allergic rhinitis. Concentra matory in their nature. In?ammatory diseases that affect the tions of 0.625, 1.25, and 2.5 mg/mL of cetiriZine Were population include asthma, rhinitis, COPD, in?ammatory sprayed three times a day for tWo Weeks (Clement P, Roovers boWel disease, rheumatoid arthritis, osteoarthritis, conjunc M H, Francillon C, Dodion P. Dose-ranging, placebo-con tivitis and dermatitis. trolled study ofcetirizine nasal spray in adults with perennial [0003] Asthma is a disease of the airWays that contains allergic rhinitis, Allergy 1994 September; 49(8), 668-72). elements of both in?ammation and bronchoconstriction. The most common side effects Were related to nasal events, Treatment regimens for asthma are based on the severity of although no difference in incidence betWeen the placebo and the condition. Mild cases are either untreated or are only the cetiriZine-treated groups Was seen. HoWever, the authors treated With inhaled [3-agonists Which affect the bronchocon of this article speculated therein that local irritation had an striction element, Whereas patients With more severe asthma adverse effect on treatment e?icacy. are typically treated regularly With inhaled corticosteroids [0012] Indeed, due to the irritation of the nasal mucosa by Which to a large extent are antiin?ammatory in their nature. cetiriZine, it has been found to be necessary to decrease its [0004] Allergic and non-allergic rhinitis are common dis immediate exposure in nasal administration. In European orders affecting about 30% of the population. Rhinitis has a Patent No. EP 605 203 B 1, it has been reported that this can be considerable impact on quality of life. In fact, rhinitis is achieved by providing cetiriZine in form of a composition generally considered to affect the quality of life more so than, containing cyclodextrin. e.g., asthma. [0013] Liposomes (also knoWn as lipid vesicles) are colloi [0005] Hay fever and perennial allergic rhinitis are charac dal particles that are prepared from polar lipid molecules terised by sneeZing, rhinorrhea, nasal congestion, pruritus, derived either from natural sources or chemical synthesis. conjunctivitis and pharyngitis. ln perennial rhinitis, chronic Such spherical, closed structures composed of curved lipid nasal obstruction is often prominent and may extend to eus bilayers, are typically used to entrap drugs, Which are often tachian tube obstruction. cytotoxic, in order to reduce toxicity and/ or increase ef?cacy. [0006] Oral or local antihistamines are ?rst line treatments, Liposome-entrapped drug preparations are often provided in and nasal steroids second line treatments for rhinitis. For most a dry (e.g. freeZe-dried) form, Which is subsequently recon patients, topical corticosteroids and long acting antihistamine stituted With an aqueous solution immediately prior to admin agents provide signi?cant relief of symptoms.Antihistamines istration. This is done in order to minimise the possibility of may also affect non-immunologically (non-lgE) mediated leakage of eg cytotoxic drug into aqueous solution and hypersensitivity reactions such as non-allergic rhinitis, exer thereby reducing the entrapping effect of the liposome. cise induced asthma, cold urticaria, and non-speci?c bron [0014] Liposomes have also been employed to encapsulate chial hyperreactivity. various drug compounds for delivery via the nasal route, in [0007] CetiriZine, [2-{4-[(4-chlorophenyl)phenylmethyl] order to improve bioavailability or as an adjuvant. Drugs that 1-piperaZinyl}ethoxy]acetic acid, is an orally and locally may be mentioned include tetanus toxoid vaccine, insulin, active, potent, long acting peripheral histamine H1 receptor desmopressin and diphenhydramine hydrochloride (see antagonist. CetiriZine (in the form of the dihydrochloride salt) Turker et al, Review Article: Nasal Route and Drug Delivery is one of the most Widely used second generation antihista Systems, Pharm. World Sci., 2004; 26, 137-142 and the ref mines for the treatment of rhino-conjunctivitis and urticaria. erences cited therein), as Well as cipro?oxacin, CM3 and It is effective, Well tolerated and safe When used orally in a salbutamol (see Desai et al, A Facile Method of Delivery of dose of 10 mg daily. Sedation and dry mouth do hoWever Liposomes by Nebulization, J. Control. Release, 2002; 84, occur as side effects in orally treated patients. CetiriZine is 69-78). also approved in children for the treatment of rhinitis. [0015] Examples of formulations comprising inter alia [0008] The main clinical effects of antihistamines include liposome-encapsulated active ingredients are discussed in reduced sneeZing and rhinorrhea. HoWever, nasal blockage US. Pat. No. 4,427,649, US. Pat. No. 4,839,175, US. Pat. appears to be less responsive. Local administration of anti No. 5,569,464, EP 249 561, WO 00/38681, WO 88/01862, histamines (such as aZelastine and levocabastine) has advan WO 98/58629, WO 98/00111, WO 03/105805, US. Pat. No. tages, including rapid onset of action and feWer side effects. 5,049,388, US. Pat. No. 5,141,674, US. Pat. No. 5,498,420, [0009] Local administration of antihistamines (such as US. Pat. No. 5,422,120, WO 87/01586, WO 2005/039533, aZelastine and levocabastine) has advantages, including rapid US 2005/0112199 and US. Pat. No. 6,228,393. US 2014/0065203 A1 Mar. 6, 2014 [0016] Combination therapies comprising co-administra is intended to encompass formulations that include only com tion of antihistamines and corticosteroids are described in ponents that are regarded in the art as suitable for admini stra WO 97/01337, WO 97/46243, WO 98/48839 and WO tion to mammalian, and especially human, patients. In the 03/049770. context of the present invention, the teen may also mean that [0017] Liposome-entrapped cetiriZine has been adminis the compositions of the invention are in a form of a liquid that tered topically to evaluate peripheral antihistaminic activity is ready-to-use, directly from the shelf, and not a formulation and systemic absorption in a rabbit model (ElZainy et al, in Which drugs are encapsulated inside liposomes requiring Cetirizine from Topical Phosphatidylcholine-Hydrogenated reconstitution shortly prior to administration in order to avoid Liposomes, The AAPS Journal, 2004; 6, 1-7, see also Drug leakage of drugs from liposomes into an aqueous carrier. Development and Industrial Pharmacy, 2005; 31, 281-291). [0025] By “homogeneous” We include not only that the [0018] The lipophilic behaviour of the cationic (Wherein compositions of the invention comprise liposomes dispersed the anion is chloride), ZWitterionic, and anionic forms of evenly throughout the aqueous carrier, but further that active cetiriZine
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