(19) & (11) EP 2 316 468 A1 (12) EUROPEAN PATENT APPLICATION (43) Date of publication: (51) Int Cl.: 04.05.2011 Bulletin 2011/18 A61K 38/02 (2006.01) A61K 38/03 (2006.01) A61K 38/04 (2006.01) A61K 38/16 (2006.01) (21) Application number: 10183239.2 (22) Date of filing: 24.02.2003 (84) Designated Contracting States: • Kirk, Randal, J. AT BE BG CH CY CZ DE DK EE ES FI FR GB GR Radford, VA 24143-3526 (US) HU IE IT LI LU MC NL PT SE SI SK TR • Olon, Lawrence, P. Bristol, TN 37620-3034 (US) (30) Priority: 22.02.2002 US 358381 P 22.03.2002 US 366258 P (74) Representative: Harrison Goddard Foote 29.05.2002 US 156527 Belgrave Hall Belgrave Street (62) Document number(s) of the earlier application(s) in Leeds accordance with Art. 76 EPC: LS2 8DD (GB) 03713634.8 / 1 490 090 Remarks: (71) Applicant: Shire LLC •This application was filed on 30-09-2010 as a Florence, KY 41042 (US) divisional application to the application mentioned under INID code 62. (72) Inventors: •Claims filed after the date of receipt of the divisional • Piccariello, Thomas application (Rule 68(4) EPC). Blacksburg, VA 24060-2534 (US) (54) Delivery system and methods for protecting and administering dextroamphetamine (57) The present invention relates to active agent de- comprise amino acids, as single amino acids or peptides, livery systems and more specifically to compositions that covalently attached to active agents and methods for ad- ministering conjugated active agent compositions. EP 2 316 468 A1 Printed by Jouve, 75001 PARIS (FR) EP 2 316 468 A1 Description CROSS REFERENCE TO RELATED APPLICATIONS 5 [0001] This application is a continuation-in- part of U.S. Patent Application 10/156,527 filed May 29, 2002; U.S. Patent Application No. 09/986,426, filed November 8, 2001; U.S. Patent Application No. 09/411,238, filed October 4, 1999 now abandoned; U.S. Patent Application No. 09/265,415 now abandoned; U.S. Patent Application No. 09/642,820, filed August 22, 2000; U.S. Patent Application No. 09/987,458, filed November 14, 2001; U.S. Patent Application No. 09/988,071, filed November 16, 2001; U.S. Patent Application No. 09/988,034, filed November 16, 2001; U.S. Patent 10 Application No. 09/933,708, filed August 22, 2001; PCT Appln. No. PCT/US01/43089, filed November 14, 2001; PCT Appln. No. PCT/US01/43117, filed November 16, 2001; PCT Appln. No. PCT/US01/43115, filed November 16, 2001 and Provisional Appl. Nos. 60/366,258, filed 22/03/2002; 60/358,381, filed 22/02/2002; 60/274,622, filed 14/11/2001; 60/247,621, filed 14/11/2001; 60/247,620, filed 14/11/2001; 60/247,595, filed 14/11/2001; 60/247,594, filed 14/11/2001; 60/247,635, filed 14/11/2001; 60/247,634, filed 14/11/2001; 60/247,606, filed 14/11/2001; 60/247,607, filed 14/11/2001; 15 60/247,608, filed 14/11/2001; 60/247,609, filed 14/11/2001; 60/247,610, filed 14/11/2001; 60/247,611, filed 14/11/2001; 60/247,702, filed 14/11/2001; 60/247,701, filed 14/11/2001; 60/247,700, filed 14/11/2001; 60/247,699, filed 14/11/2001; 60/247,698, filed 14/11/2001; 60/247,807, filed 14/11/2001; 60/247,833, filed 14/11/2001; 60/247,832, filed 14/11/2001; 60/247,927, filed 14/11/2001; 60/247,926, filed 14/11/2001; 60/247,930, filed 14/11/2001; 60/247,929, filed 14/11/2001; 60/247,928, filed 14/11/2001; 60/247,797, filed 14/11/2001; 60/247,805, filed 14/11/2001; 60/247,804, filed 14/11/2001; 20 60/247,803, filed 14/11/2001; 60/247,802, filed 14/11/2001; 60/247,801, filed 14/11/2001; 60/247,800, filed 14/11/2001; 60/247,799, filed 14/11/2001; 60/247,798, filed 14/11/2001; 60/247,561, filed 14/11/2001; 60/247,560, filed 14/11/2001; 60/247,559, filed 14/11/2001; 60/247,558, filed 14/11/2001; 60/247,556, filed 14/11/2001; 60/247,612, filed 14/11/2001; 60/247,613, filed 14/11/2001; 60/247,614, filed 14/11/2001; 60/247,615, filed 14/11/2001; 60/247,616, filed 14/11/2001; 60/247,617, filed 14/11/2001; 60/247,633, filed 14/11/2001; 60/247,632, filed 14/11/2001; 60/247,631, filed 14/11/2001; 25 60/247,630, filed 14/11/2001; 60/247,629, filed 14/11/2001; 60/247,628, filed 14/11/2001; 60/247,627, filed 14/11/2001; 60/247,626, filed 14/11/2001; 60/247,625, filed 14/11/2001; 60/247,624, filed 14/11/2001; 60/247,806, filed 14/11/2001; 60/247,695, filed 14/11/2001; 60/247,794, filed 14/11/2001; 60/247,793, filed 14/11/2001; 60/247,792, filed 14/11/2001; 60/247,791, filed 14/11/2001; 60/247,790, filed 14/11/2001; 60/247,789, filed 14/11/2001; 60/247,788, filed 14/11/2001; 60/247,787, filed 14/11/2001; 60/247,786, filed 14/11/2001; 60/247,785, filed 14/11/2001; 60/247,784, filed 14/11/2001; 30 60/247,783, filed 14/11/2001; 60/247,782, filed 14/11/2001; 60/247,781, filed 14/11/2001; 60/247,780, filed 14/11/2001; 60/247,779, filed 14/11/2001; 60/247,778, filed 14/11/2001; 60/247,777, filed 14/11/2001; 60/247,776, filed 14/11/2001; 60/247,775, filed 14/11/2001; 60/247,774, filed 14/11/2001; 60/247,773, filed 14/11/2001; 60/247,772, filed 14/11/2001; 60/247,771, filed 14/11/2001; 60/247,770, filed 14/11/2001; 60/247,769, filed 14/11/2001; 60/247,768, filed 14/11/2001; 60/247,767, filed 14/11/2001; 60/247,766, filed 14/11/2001; 60/247,871, filed 14/11/2001; 60/247,872, filed 14/11/2001; 35 60/247,873, filed 14/11/2001; 60/247,874, filed 14/11/2001; 60/247,875, filed 14/11/2001; 60/247,981, filed 14/11/2001; 60/247,982, filed 14/11/2001; 60/247,983, filed 14/11/2001; 60/247,984, filed 14/11/2001; 60/247,745, filed 14/11/2001; 60/247,744, filed 14/11/2001; 60/247,743, filed 14/11/2001; 60/247,742, filed 14/11/2001; 60/247,623, filed 14/11/2001; 60/247,985, filed 14/11/2001; 60/247,840, filed 14/11/2001; 60/247,839, filed 14/11/2001; 60/247,838, filed 14/11/2001; 60/247,837, filed 14/11/2001; 60/247,836, filed 14/11/2001; 60/247,889, filed 14/11/2001; 60/247,890, filed 14/11/2001; 40 60/247,891, filed 14/11/2001; 60/247,892, filed 14/11/2001; 60/247,893, filed 14/11/2001; 60/247,741, filed 14/11/2001; 60/247,740, filed 14/11/2001; 60/247,739, filed 14/11/2001; 60/247,738, filed 14/11/2001; 60/247,737, filed 14/11/2001; 60/247,736, filed 14/11/2001; 60/247,735, filed 14/11/2001; 60/247,734, filed 14/11/2001; 60/247,733, filed 14/11/2001; 60/247,732, filed 14/11/2001; 60/247,731, filed 14/11/2001; 60/247,730, filed 14/11/2001; 60/247,728, filed 14/11/2001; 60/247,729, filed 14/11/2001; 60/247,727, filed 14/11/2001; 60/247,726, filed 14/11/2001; 60/247,761, filed 14/11/2001; 45 60/247,760, filed 14/11/2001; 60/247,759, filed 14/11/2001; 60/247,758, filed 14/11/2001; 60/247,757, filed 14/11/2001; 60/247,756, filed 14/11/2001; 60/247,765, filed 14/11/2001; 60/247,764, filed 14/11/2001; 60/247,763, filed 14/11/2001; 60/247,762, filed 14/11/2001; 60/247,755, filed 14/11/2001; 60/247,746, filed 14/11/2001; 60/247,725, filed 14/11/2001; 60/247,724, filed 14/11/2001; 60/247,723, filed 14/11/2001; 60/247,722, filed 14/11/2001; 60/247,721, filed 14/11/2001; 60/247,720, filed 14/11/2001; 60/247,719, filed 14/11/2001; 60/247,718, filed 14/11/2001; 60/247,717, filed 14/11/2001; 50 60/247,716, filed 14/11/2001; 60/247,754, filed 14/11/2001; 60/247,753, filed 14/11/2001; 60/247,752, filed 14/11/2001; 60/247,751, filed 14/11/2001; 60/247,750, filed 14/11/2001; 60/247,749, filed 14/11/2001; 60/247,748, filed 14/11/2001; 60/247,747, filed 14/11/2001; 60/247,796, filed 14/11/2001; 60/247,815, filed 14/11/2001; 60/247,814, filed 14/11/2001; 60/247,813, filed 14/11/2001; 60/247,812, filed 14/11/2001; 60/247,811, filed 14/11/2001; 60/247,810 filed 14/11/2001; 60/247,809 filed 14/11/2001; 60/247,808 filed 14/11/2001; 60/247,885 filed 14/11/2001; 60/247,884 filed 14/11/2001; 55 60/247,883 filed 14/11/2001; 60/247,882 filed 14/11/2001; 60/247,881 filed 14/11/2001; 60/247,880 filed 14/11/2001; 60/247,879 filed 14/11/2001; 60/247,878 filed 14/11/2001; 60/247,826 filed 14/11/2001; 60/247,835 filed 14/11/2001; 60/247,834 filed 14/11/2001; 60/247,897 filed 14/11/2001; 60/247,896 filed 14/11/2001; 60/247,895 filed 14/11/2001; 60/247,894 filed 14/11/2001; 60/247,901 filed 14/11/2001; 60/247,900 filed 14/11/2001; 60/247,899 filed 14/11/2001; 2 EP 2 316 468 A1 60/247,898 filed 14/11/2001; 60/247,903 filed 14/11/2001; 60/247,902 filed 14/11/2001; 60/247,919 filed 14/11/2001; 60/247,918 filed 14/11/2001; 60/247,917 filed 14/11/2001; 60/247,916 filed 14/11/2001;60/247,915 filed 14/11/2001; 60/247,914 filed 14/11/2001; 60/247,913 filed 14/11/2001; 60/247,912 filed 14/11/2001; 60/247,911 filed 14/11/2001; 60/247,910 filed 14/11/2001; 60/247,877 filed 14/11/2001; 60/247,876 filed 14/11/2001; 60/247,707 filed 14/11/2001; 5 60/247,706 filed 14/11/2001; 60/247,705 filed 14/11/2001; 60/247,704 filed 14/11/2001; 60/247,703 filed 14/11/2001; 60/247,692 filed 14/11/2001; 60/247,691 filed 14/11/2001; 60/247,690 filed 14/11/2001; 60/247,689 filed 14/11/2001; 60/247,688 filed 14/11/2001; 60/247,687 filed 14/11/2001; 60/247,686 filed 14/11/2001; 60/247,685 filed 14/11/2001; 60/247,684 filed 14/11/2001; 60/247,683 filed 14/11/2001; 60/247,694 filed 14/11/2001; 60/247,693 filed 14/11/2001; 60/247,712 filed 14/11/2001; 60/247,711 filed 14/11/2001; 60/247,710 field 14/11/2001; 60/247,709 filed 14/11/2001; 10 60/247,708 filed 14/11/2001; 60/247,697 filed 14/11/2001; 60/247,696 filed 14/11/2001; 60/247,695 filed 14/11/2001; 60/247,565 filed 14/11/2001; 60/247,564 filed 14/11/2001; 60/247,545 filed 14/11/2001; 60/247,546 filed 14/11/2001; 60/247,547 filed 14/11/2001; 60/247,548 filed 14/11/2001; 60/247,568 filed 14/11/2001; 60/247,570 filed 14/11/2001; 60/247,580 filed 14/11/2001; 60/247,555 filed 14/11/2001; 60/247,554 filed 14/11/2001; 60/247,553 filed 14/11/2001; 60/247,552 filed 14/11/2001: 60/247,551