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W O 2010/004256 Al (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization IN International Bureau (10) International Publication Number (43) International Publication Date 14 January 2010 (14.01.2010) PCT W O 2010/004256 Al (51) International Patent Classification: Block B, Holland Park, Holland Drive, Newcastle Upon A61K 31/05 (2006.01) A61K31/29 (2006.01) Tyne Tyne & Wear NE2 4LZ (GB). A61K 31/055 (2006.01 ) A61K 31/343 (2006.01 ) A61K 31/06 (2006.01) A61K 31/415 (2006.01) (74) Agent: GILHOLM, Stephen, Philip; Pheons Intellec A61K31/135 (2006.01) A61K 31/485 (2006.01) tual Property, Buzzard Office, The Hawk Creative Busi A 61K 31/1357(2006.0l1) A 61K 31/45 (2006.0 1) ness Park, Easingwold, A61K31/137 (2006.01 ) A61K 31/5415 (2006.01 ) York YO61 3FF (GB). A61K31/167(2006.01) A61K 31/616 (2006.01) (81) Designated States (unless otherwise indicated, for every A61K 31/194 (2006.01) A61P 25/24 (2006.01) kind of nationalprotection available>: AE, AG, AL, AM, (21) International Application Number:AT, AU, AZ, BA, BB, BG, , BR, BW, BY, BZ, CN, CO, CR, CU, CZ, DF, DK, DM, DO, PCT/GB2009/001515PCT/B209/00515 DZ,CA, CH,FC, FE,CL, EG, ES, Fl, GB, GD, GE, GH, GM, GT, (22) International Filing Date: HN, HR, HU, 11, IL, IN, IS, JP, KE, KG, KM, KN, KP, 17 June 2009 (17.06.2009) KR, KZ, LA, LC, LK, LR, LS, LT, LU, LY, MA, MD, ME, MG, MK, MN, MW, MN, MY, MZ, NA, NG, NI, (25) Filing Language: English NO, NZ, OM, PE, PG, PH, PL, PT, RO, RS, RU, SC, SD, (26) Publication Language: English SE, SG, SK, SL, SM, ST, SV, SY, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. (30) Priority Data: 0811024.9 17 June 2008 (17.06.2008) GB (84) Designated States (unless otherwise indicated, for every 61/084,665 30 July 2008 (30.07.2008) GB kind of regionalprotection available>: ARIPO (BW, GH, GM, KE, LS, MW, MZ, NA, SD, SL, SZ, TZ, UG, ZM, (71) Applicant (for all designated States except US): E- ZW), Eurasian (AM, AZ, BY, KG, KZ, MD, RU, TJ, THERAPEUTICS PLC [GB/GB]; Block B, Holland TM), European (AT, BE, BG, CH, CY, CZ, DE, DK, EE, Park, Holland Drive, Newcastle Upon Tyne, Tyne & ES, Fl, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, Wear NE2 4LZ (GB). MC, MK, MT, NL, NO, PL, PT, RO, SE, SI, SK, TR), (72)(7)Ivnos-n Inventors; and OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, ML, (75) Inventors/Applicants (for US only): YOUNG, Malcolm, MR, NE, SN, TD, TG). Philip [GB/GB]; e-Therapeutics plc, Block B, Holland Published: Park, Holland Drive, Newcastle Upon Tyne Tyne & Wear NE2 4LZ (GB). IDOWU, Olusola, Clement [GB/GB]; e Therapeutics plc, Block B, Holland Park, Holland Drive, before the expiration of the time limit for amending the Newcastle Upon Tyne Tyne & Wear NE2 4LZ (GB). claims and to be republished in the event of receipt of MCKEOWN, Philip [GB/GB]; e-Therapeutics pSc, amendments (Rule 48.2(hIl o(54) Title: CONTROLLED RELEASE TREATMENT OF DEPRESSION (57) Abstract: There is described a pharmaceutical composition for controlled release of an active compound wherein the active compound is selected from the group comprising tramadol, resveratrol, acetaminophen, xorphanol, cinfenoac, fircloprofen, bis fA mouth subsalicylate, enofelast, triflusal, ketorfanol, indriline, furofenac, cizoliTine, dacemazine, demelverine, and fenethazine, and derivatives and/or combinations thereof for the treatment or alleviation of depression. More particularly, there is described an Abuse resistant pharmaceutical composition for the treatment of, inter alia, depression and controlled release pharmaceutical com positions of related thereto. WO 2010/004256 PCT/GB2009/001515 1 CONTROLLED RELEASE TREATMENT OF DEPRESSION FIELD OF THE INVENTION The present invention provides a novel once daily oral pharmaceutical composition 5 for controlled release of a medicament for the treatment of depression and methods related thereto. More particularly, the present invention relates to abuse resistant pharmaceutical compositions and abuse resistant compositions for the treatment of depression and 10 controlled release pharmaceutical compositions related thereto. BACKGROUND OF THE INVENTION Tramadol hydrochloride is suitable as a long-term treatment for chronic pain. Tramadol is a centrally acting analgesic that has been shown to be effective in a 15 variety of acute and chronic pain states in conjunction with non-steroidal anti inflammatory drugs (NSAIDs) for the reduction of pain attributed to osteoarthritis. After oral administration, tramadol hydrochloride is rapidly and almost completely absorbed, and it is extensively metabolised. Immediate release formulations of 20 tramadol hydrochloride are well known in the art. Such formulations, however, require frequent dosing in order to provide effective pain relief. Lack of compliance with high frequency dosing regimens can result in inconsistent plasma drug concentrations and accordingly less consistent analgesia. Twice daily formulations are available and are desirable over immediate release formulations as they provide 25 longer periods of analgesia after administration and require less frequent dosing. A WO 2010/004256 PCT/GB2009/001515 2 once daily formulation is even more desirable for increased effectiveness, safety and convenience. European Patent Application No. 1 576 986 describes a solid dosage pharmaceutical 5 formulation containing tramadol hydrochloride comprising a physical mixture of polyvinyl acetate, polyvinylpyrrolidone and tramadol hydrochloride. The known once daily oral pharmaceutical composition when ingested orally provides a clinical effect over 24 hours. 10 Our co-pending International Patent application No. WO 2009/001040 describes certain compounds which are useful for the treatment or alleviation of depression contributed to or caused by pain. More particularly, the aforementioned co-pending application describes a compound selected from the group comprising tramadol, resveratrol, acetaminophen, xorphanol, cinfenoac, furcloprofen, bismuth 15 subsalicylate, enofelast, triflusal, ketorfanol, indriline, furofenac, cizolirtine, dacemazine, demelverine, and fenethazine, and derivatives and/or combinations thereof, as being useful for the treatment or alleviation of depression; and especially depression contributed to or caused by pain. 20 A once daily pharmaceutical composition of, for example, tramadol, which, when ingested orally, provides a clinical effect over 24 hours is known. However, an extended or controlled release analgesic anti-depressant composition is novel per se. Generally, such extended or controlled release pharmaceutical 25 compositions will tend to contain a high dosage of the pharmaceutical so the relief WO 2010/004256 PCT/GB2009/001515 3 provided is adequate for the extended period. However, such controlled release compositions are often subject to abuse because they carry such a high dosages of the medicament. Thus, for example, a patient may crush or chew a controlled release tablet or capsule providing an immediate high dosage release of the medicament. 5 Such abuse of antidepressants may have catastrophic results, such as death or suicide. Therefore, there is a need for a novel controlled release pharmaceutical composition of a pharmaceutical, such as tramadol, (and/or the related compounds hereinafter described) provide continuous relief of pain and/or depression or depression caused 10 by pain, without the risk of abuse by the patient. We have now found a novel pharmaceutical composition which has extended release characteristics and which is resistant to or minimises abuse by the patient. 15 SUMMARY OF THE INVENTION The novel controlled or controlled release pharmaceutical composition pharmaceutical composition comprises one of the aforementioned compounds, namely, a compound selected from the group comprising tramadol, resveratrol, acetaminophen, xorphanol, cinfenoac, furcloprofen, bismuth subsalicylate, enofelast, 20 triflusal, ketorfanol, indriline, furofenac, cizolirtine, dacemazine, demelverine, and fenethazine, and derivatives and/or combinations thereof. The use of the compounds as hereinbefore described in the once daily dosage treatment or alleviation of depression; and especially depression contributed to or 15 caused by pain, is novel per se. WO 2010/004256 PCT/GB2009/001515 4 Therefore, according to a first aspect of the invention we provide a pharmaceutical composition for controlled release of an active compound wherein the active compound is selected from the group comprising tramadol, resveratrol, 5 acetaminophen, xorphanol, cinfenoac, furcloprofen, bismuth subsalicylate, enofelast, triflusal, ketorfanol, indriline, furofenac, cizolirtine, dacemazine, demelverine, and fenethazine, and derivatives and/or combinations thereof for the treatment or alleviation of depression 10 The invention particularly provides a pharmaceutical composition wherein the antidepressive effect is in connection with depression contributed to or caused by pain. Thus, the medicament may be suitable for the treatment or alleviation of pain and depression separately, simultaneously or sequentially. 15 More particularly the present invention provides a once daily oral pharmaceutical composition for controlled release of an active compound as hereinbefore described, in which the composition, upon initial administration, provides an onset of antidepressive effect within 2 hours, which antidepressive effect continues for at least 24 hours after administration. We especially provide a once daily oral pharmaceutical 20 composition as hereinbefore
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