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(12) Patent Application Publication (10) Pub. No.: US 2004/0023948A1 Green Et Al

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(12) Patent Application Publication (10) Pub. No.: US 2004/0023948A1 Green Et Al US 20040023948A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2004/0023948A1 Green et al. (43) Pub. Date: Feb. 5, 2004 (54) FAST-DISPERSING DOSAGE FORM continuation of application No. PCT/GB98/00885, CONTAINING 5-HT1AGONSTS filed on Mar. 24, 1998. (76) Inventors: Richard David Green, Canterbury (30) Foreign Application Priority Data (GB); Jonathan Lacy, Genthod (CH); Nicholas Mallard, Bristol (GB); Mar. 24, 1997 (GB)......................................... 97O6089.1 Edward Johnson, Berkshire (GB) Publication Classification Correspondence Address: Andrew G. Rozycki (51) Int. Cl." ........................ A61K 31/55; A61K 31/506 Cardinal Health, Inc. (52) U.S. Cl. ...................................... 514/216; 514/252.15 7000 Cardinal Place Dublin, OH 43017 (US) (57) ABSTRACT This invention relates to a pharmaceutical composition for (21) Appl. No.: 10/375,560 oral administration comprising a carrier and, as an active (22) Filed: Feb. 26, 2003 ingredient, a 5-HT agonist, characterized in that the com position is formulated to reduce pre-systemic metabolism of Related U.S. Application Data Said 5-HT agonist. A proceSS for preparing Such a compo Sition and the use of Such a composition for the treatment of (63) Continuation-in-part of application No. 09/408.595, anxiety, depression, attention deficit disorder and/or panic filed on Sep. 23, 1999, now abandoned, which is a disorders and/or as a memory enhancer are also provided. Patent Application Publication Feb. 5, 2004 Sheet 1 of 2 US 2004/0023948A1 o E So g) E CN O up - v- X o CN Cl h ( S. ( (w X s (up 6 u) guould sing eused Patent Application Publication Feb. 5, 2004 Sheet 2 of 2 US 2004/0023948A1 lo N as C i- n E EC O) g E. & 5 - a C. r -d i i u? O. wer v- 1. (s C E - ? C e (s C) SE ci O) - 9) l (\ CD l 3. is - O O 0. C C cad c o O C g ed O C d ab AA) r t cn w C (up 6 u) did eused US 2004/0023948 A1 Feb. 5, 2004 FAST-DSPERSING DOSAGE FORM CONTAINING lism, that is, metabolism in the gastrointestinal tract, in the 5-HT1AGONSTS membranes lining the gastrointestinal tract and also in the liver. However, it is clear that the clinical effectiveness of RELATED APPLICATION DATA buSpirone is compromised by the extensive pre-systemic 0001. This Application is a continuation-in-part of U.S. metabolism of this drug which occurs following conven patent application Ser. No. 09/408.595; filed Sep. 23, 1999 tional oral administration. which is a Continuation of International Application No. 0006 Buspirone is an example from a class of com PCT/GB98/00885, filed Mar. 24, 1998 (claiming priority pounds known as the azapirones which have been shown to from British Application No. 9706089.1, filed Mar. 24, be effective in the treatment of anxiety. Other azapirones 1997), now pending, which are hereby incorporated by include 4,4-dimethyl-1-4-4-(2-pyrimidinyl)-1-piperazinyl reference. butyl-2,6-piperidinedione (gepirone), 2-4-4-(2-pyrimidi nyl)-1-piperazinylbutyl-1,2-benzisothiazol-3(2H)-one 1,1- FIELD OF THE INVENTION dioxide (ipsapirone), (3ao,4C,4C.f3, 6C.f3, 7C,7ao)-3a,4,4a, 6a,7,7a-hexahydro-2-4-4-(2-pyrimidinyl)-1-piperazinyl 0002 This invention relates to a pharmaceutical compo butyl-4,7-etheno-1H-cyclobut fisoindole-1,3(2H)-dione Sition, a process for preparing Such a composition and the (Zalospirone), 3-butyl-7-4-4-(2-methoxyphenyl)-1-piper use of Such a composition for the treatment of anxiety, azinylbutyl-9,9-dimethyl-3,7-diazabicyclo3.3.1 nonane depression, attention deficit disorder and/or panic disorders, 2,4,6,8-tetrone(umeSpirone), (S)-8-4-(3,4-dihydro-5- Sleep apnea and/or related respiratory disorders and/or Sub methoxy-2H-1-benzopyran-3-yl)propylaminobutyl-8- stance addition, especially alcohol abuse, the treatment azaspiro4.5decane-7,9-dione (alnespirone), 6-(3- and/or prophylaxis of incontinence disorders, inducing chlorophenoxy)-2-methyl-1-Oxa-4-azaspiro4.5decan-3- immunosuppression and/or treating immune disorders, the one (eniloSpirone), octahydro-3-4-4-(2-pyrimidinyl)-1- alleviation of extrapyramidal motor disorders and/or as a piperazinylbutyl-1,5-methano-6,7,9-metheno-1H memory enhancer. pentaleno1,2-diazepine-2,4(3H,5H)-dione (WY-48723),4- 4-4-(2-pyrimidinyl)-1-piperazinylbutyl-1,4- BACKGROUND OF THE INVENTION benzoxazepine-3.5 (2H4H)-dione (SUN-8399), (3ao,4B, 0003 Buspirone (8-4-4-(2-pyrimidinyl)-1-piperazinyl 7B,7ao)-hexahydro-2-4-4-(2-pyrimidinyl)-1-piperazinyl butyl-8-azaspiro4.5decane-7,9-dione) has been shown to butyl-4,7-methano-1H-isoindole-1,3(2H)-dione be effective in the treatment of anxiety. The mechanism of 2-hydroxy-1,2,3-propanetricarboxylate (1:1) (tandospirone) action of buspirone has not been fully elucidated. However, and Salts thereof. All these compounds act as agonists at it is known that buspirone is a 5-HT agonist and, in 5-HT, receptors, particularly 5-HT1A receptors, and, like particular, a potent 5-HTA agonist and it is thought that it is buSpirone, are Subject to extensive pre-Systemic metabo the action at these receptors which may account for its lism. Other compounds which interact with 5-HT, receptors anxiolytic activity. (5-HT, agonists) include (+)-N-2-4-2,3-dihydro-2-(hy droxymethyl)-1,4-benzodioxin-5-yl)-1-piperazinylethyl 0004 Buspirone is currently administered orally in the 4-fluoro-benzamide (flesinoxan), 2-4-4-(4-chloro-1H form of a conventional tablet which is Scored in a manner pyrazol-1-yl)butyl-1-piperazinylpyrimidine (lesopitron) which provide for it to be broken into halves or thirds along (R)-3,4-dihydro-N-(1-methylethyl)-3-((1-methylethyl)pro breaklines, thus allowing for Some titration of the dose. pylamino)-2H-1-benzopyran-5-carboxamide (ebalZotan), However, each tablet or portion thereof is designed to be N-2-4-(2-pyrimidinyl)-1-piperazinyladamantane-1-car Swallowed whole. Doses range from 15 to 60 mg per day and boxamide (adatanserin), (R)-4-(dipropylamino)-1,3,4,5-tet may be delivered as 2 or 3 divided doses. When adminis rahydro-benz(cd)indole-6-carboxamide (LY-228729), tered in this way, buSpirone is absorbed from the gastrointes F-8910-RS, (-)-cis-3-propyl-2,3,3a(R),4,5,9b-hexahydro tinal tract, that is, the Stomach, the Small intestine and the 14-benzelindole-9-carboxamide (U-93385), 4-2-4-(naph proximal large intestine (colon), into the hepatic portal thalen-1-yl)piperazin-1-yl)ethylquinolin-2(1H)one (SL System and is presented to the liver before reaching the 87.0765), 2-4-44-bis(4-fluorophenyl)butyl-1- Systemic circulation. The liver is known to be the principal piperazinyl-3-pyridinecarboxylic acid methyl ester (FG Site for conversion of active buSpirone into metabolites and, 5893), 4-fluoro-N-2-4-7-methoxy-1-naphthylpiperazin indeed, buSpirone is rapidly metabolized by the liver into a 1-yl)ethylbenzamide (S-14506), 5-methoxy-3-4-(4-(4- large number of metabolites. In a radio-label Study in man, methoxyphenyl)-1-piperazinyl)butylindole (EMD-56551), twelve metabolites of buspirone were isolated from urine (-)-N-2-(8-methyl-1,4-benzodioxan-2- (see H. K. Jajoo et al., Drug Metabolism and Disposition, ylmethylamino)ethyladamantane-1-carboxamide (HT (1989), 17, 634-640). However, only one of these metabo 90B), F-92502-CN, 2-4-4-(4-nitropyrazol-1-yl)butyll lites, 1-pyrimidinylpiperazine (1-PP), has been reported to piperazin-1-ylpyrimidine (E-4414), 5-3-(2S)-1,4- possess any potential therapeutic activity and this compound benzodioxan-2-ylmethyl-aminopropoxy]-1,3- is said to possess, at most, only 20% of the activity of benzodioxolane (MKC-242), 4-methyl-2-4-(4-(pyrimidin unchanged buspirone as determined by the Vogel conflict 2-yl)-piperazino)butyl-2H4H-1,2,4-triazin-3,5-dione test in rats (see R. E. Gammans et al., Am. J. Med., (1986), (F-12439), 1-(2-(4-(3-trifluoromethylphenyl)piperazin-1-yl 80 (suppl.3B), 41-51). )ethyl)benzimidazol-1H-2-one (BIMT-17), LY-39, 0005 The mean systemic availability of unchanged bus SL-88.0338, 1,2,3,6-tetrahydro-1-2-(2-naphthalenyl pirone is thought to be about 4% after conventional oral )ethyl-4-3-(trifluromethyl)phenylpyridine (SR-57746A), administration and the plasma levels of this drug are Said to 1-(9H-fluoren-2-yl)-2-(1H-imidazol-1-yl)ethanone (LY exhibit great variability. This latter effect has been attributed 175644), (+/-)trans-2-(4-(3a,4,4a,6a,7,7a-hexahydro-4,7- to differences between individuals in pre-systemic metabo etheno-1H-cyclobut fisoindol-1,3-dionyl)butyl-9-meth US 2004/0023948 A1 Feb. 5, 2004 oxy-2,3,3a,4,5,9b-hexahydro-1H-benzeisoindol that the composition of the invention is formulated to (A-74283), 1,3,4,5-tetrahydo-6-methoxy-N,N-dipropylbenz promote pre-gastric absorption of the 5-HT agonist. cdlindol-4-amine (Bay-r-1531), 4-(4-methyl-1-piperazi nyl)-7-(trifluoromethyl)-pyrrolo1,2-aquinoxaline (Z)-2- DETAILED DESCRIPTION OF THE butendioate (1:2) (CGS-12066B), trans-1,3,4,4a,5,10b INVENTION hexahydro-10-methoxy-4-propyl-2H-1 benzopyrano3,4- bipyridine (CGP-50281), N-propyl-N-2-(4- 0010. The term “pre-gastric absorption” is used to refer to fluorobenzamido)ethylamino-5,6,7,8-tetrahydroquinoline absorption of the active ingredient from that part of the (WAY-100012), 3a,4,4a,6a,7,7a-hexahydro-2-4-4-(2-pyri alimentary canal prior to the Stomach and includes buccal, midinyl)-1-piperazinylbutyl-4,7-ethenocyclobutaf-1,2- Sublingual, oropharyngeal and esophageal absorption.
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