Patent SG-11201901294Q-A (SG)
Title: Sustained-release buprenorphine formulations background of invention
Inventor: LIN TONG-HO
IPC: A61P25/36
Filed: 2017-09-12
Abstract: INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property 111111101111 0 1110101011111 011101 0 011111111111111111111011111111111110111111 Organization International Bureau (10) International Publication Number (43) International Publication Date ......0\" WO 2018/050043 Al 22 March 2018 (22.03.2018) WIP0 I PCT (51) International Patent Classification: TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, A61K 31/485 (2006.01) A61K 47/22 (2006.01) KM, ML, MR, NE, SN, TD, TG). A61K 9/08 (2006.01) A61P 25/36 (2006.01) A61K 47/10 (2006.01) A61P 25/04 (2006.01) Published: (21) International Application Number: — with international search report (Art. 21(3)) PCT/CN2017/101327 (22) International Filing Date: 12 September 2017 (12.09.2017) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 62/394,168 13 September 2016 (13.09.2016) US (71) Applicant: ALAR PHARMACEUTICALS INC. [CN/CN]; No. 3, Aly. 27, Ln. 30, Sec. 4, Xinyi Rd., Da'an Dist., Taipei City, Taiwan 106 (CN). (72) Inventors: LIN, Tong-Ho; No. 3, Aly. 27, Ln. 30, Sec. 4, Xinyi Rd., Da'an Dist., Taipei City, Taiwan 106 (CN). WEN, Yung-Shun; No. 3, Aly. 27, Ln. 30, Sec. 4, Xinyi Rd., Da'an Dist., Taipei City, Taiwan 106 (CN). LIANG, Jui-Wei; No. 3, Aly. 27, Ln. 30, Sec. 4, Xinyi Rd., Da'an Dist., Taipei City, Taiwan 106 (CN). Agent: SHANGHAI PATENT & TRADEMARK LAW = (74) OFFICE, LLC; 435 Guiping Road, Shanghai 200233 (CN). Designated States (unless otherwise indicated, for every kind of national protection available): AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JO, JP, KE, KG, KH, KN, KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. (81) Designated States (unless otherwise indicated, for every kind of regional protection available): ARIPO (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, (84) 1-1 M 71- (54) Title: SUSTAINED-RELEASE BUPRENORPHINE FORMULATIONS BACKGROUND OF INVENTION 0 0 (57) : An injectable pharmaceutical composition includes a solution of 3-acyl-buprenorphine, or a pharmaceutically acceptable It In salt thereof, in a biocompatible organic solvent, wherein the injectable pharmaceutical composition exhibits a steady release profile last- = ing over one week when injected into a patient. The acyl group is an alkylcarbonyl group, and an alkyl portion of the alkylcarbonyl group ww is a straight-chain, branched-chain, having 1-20 carbon atoms. The biocompatible organic solvent is N-methyl-2-pyrrolidone, ethyl 1-1 © acetate, ethanol, butanol, 2-butanol, isobutanol, ispropanol, glycerin, benzyl benzoate, dimethyl sulfoxide, N, N-dimethylacetamide, f'1 propylene glycol, dimethyl glycol, benzyl alcohol, or a combination of two or more thereof. C