(12) United States Patent
`(10) Patent N0.:
`US 8,313,776 B2
`Burnside et a1.
`(45) Date of Patent:
`*Nov. 20, 2012
`
`USOO8313776B2
`
`536/74
`7/1987 Morimoto et al.
`
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`2/1988 Pope et 31.
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`
`6/1988 Reusser et al.
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`
`7/1988 Etienne et a1.
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`10/1988 McShanc ......
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`
`2/1989 Lu et al.
`........
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`3/1989 Haniashiina et a1.
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`Fujioka et all
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`. 514/29
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`Panoz et a1.
`£2£/468
`(Continued)
`
`FOREIGN PAT2N1 DOCUMgNTS
`2533358 A1
`/2005
`
`..
`
`
`
`
`
`.
`
`
`
`4,680,386 A
`4,710,565 A
`4,723,958 A
`4,728,512 A
`4.749.568 A
`4,755,385 A
`4,775,751 A
`4,794,001 A
`4,808,411 A
`4,812,561 A
`4,828,836 A
`4,831,025 A
`4,835,140 A
`4.842.866 A
`4,849,515 A
`4,879,135 A
`4,894,119 A
`4,895,934 A
`4,904,476 A
`4,915,953 A
`4,945,080 A
`4.945.405 A
`4,971,805 A
`4,990,602 A
`5,011,692 A
`5,045,533 A
`5,051,262 A
`
`(54)
`
`ANTIBIOTIC PRODUCT, USE AND
`FORMULATION THEREOF
`
`(75)
`
`Inventors: Beth A. Burnside, Bethesda, MD (US);
`Henry H. Flanner, Montgomery
`Village, MD (US); Colin Rowlings,
`Potomac, MD HIS)
`
`(73)
`
`Assignee: Shionogi Inc., l'lorham Park, NJ (US)
`
`(*)
`
`Notice:
`
`Subject to any disclaimer, the term of this
`patent is extended or adjusted under 35
`U.S.C. 154(b) by 1096 days.
`
`This patent is subject to a terminal dis-
`claimer.
`
`(21)
`
`(22)
`
`(65)
`
`(60)
`
`(51)
`
`(52)
`
`(58)
`
`(56)
`
`Appl. No.: 10/894,994
`
`Filed:
`
`Jul. 20. 2004
`
`Prior Publication Data
`
`US 2005/0019403 A]
`
`Jan. 27, 2005
`
`Related US. Application Data
`
`Provisional application No. 60/488,901, filed on Jul.
`21, 2003.
`
`CA
`
`Int. Cl.
`A61K 9/16
`US. Cl.
`
`(2006101)
`424/490; 424/457; 424/458; 424/468;
`424/469
`Field of Classification Search ........................ None
`See application file for complete search history.
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`(Continued)
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`OTHER PUBLICATIONS
`
`MedlinePlus. Merriam-Webster, definition "clinical”, http://Zmer—
`riam—webster.com/cgi-bin/mwmednlm. *
`MedlinePlus. Merriam-Webster, definition “in vitro”. http://2mer-
`riam-webster.com/cgi-bin/mwmednlm. *
`Adjei et al., Comparative Pharmacokinetic Study of Continuous
`Venous Infiision Flu orouracil and Oral Flu orouracil With Eniluraeil
`in Patients with Advanced Solid Tumors, Journal of C1inica1 Oncol—
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`inicrobials in the Therapy of Respiratory Tract Infections, Current
`Opinion in
`Infectious Diseases,
`14(2): 165-172, Apr. 2001.
`(Abstract).
`Auckenlhaler, Pharmacokinetics and Pharmacodynamics of Oral
`Beta-Lactam Antibiotics as 3 Two-Dimensional Approach to Their
`Efficacy, J Antimicrob Chemother, (2002) 50, 13-17.
`
`(Continued)
`
`Primary Examiner 7 Bethany Barham
`(74) Attorney, Agent, or FirmiMHZ Technology Law
`Group LLP
`
`ABSTRACT
`(57)
`An antibiotic product is comprised of at least three dosages
`forms, each of which has a different release profile, with the
`CW” for the antibiotic product being reached in less than
`about twelve hours. In one embodiment, there is an immedi-
`ate release dosage form, a delayed release dosage form, and a
`sustained release dosage form. with each ofthe dosage forms
`having a different release profile, wherein each reaches a
`mwe
`C
`at different times.
`
`16 Claims, No Drawings
`
`KVK-TECH EXHIBIT 1017
`
`KVK-TECH EXHIBIT 1017
`
`

`

`US 8,313,776 B2
`
`Page2
`
`
`
`U.S. PATENT DOCUMENTS
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`
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`. 264/43
`5143661 A
`10/1992 Abramowitz etal.
`.
`424/458
`5,158,777 A
`424/438
`5 178 874 A
`“1993 K
`1
`
`“1993 TY)? et 331"
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`5,182,374 A
`5,204,055 A
`4993 $1113:le ~
`419,2
`
`5/1993 Bar-Shalom etal.
`424/473
`5,213,808 A
`
`424/451
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`
`. 536/7.4
`5,274,085 A
`12/1993 Amano etal.
`424,497
`5288 503 A
`2,1994 Woodetal
`
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`5,334,590 A
`8/1994 DiNinno er a1.
`5,340,656 A
`8/1994 Sachsetal.
`................... 428/546
`5358713 A
`10/1994 Shimamura
`424/729
`
`~~
`5,387,380 A
`2/1995 Cimaetal
`264/69
`..
`5,393,765 A
`2/1995 Infeld etal.
`514/365
`
`5395 626 A
`3/1995 Kotwal et al
`424/472
`'
`5,395,628 A
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`1
`424/490
`etz:.1...
`5,399,723 A
`”995 1.0
`549/403
`
`5,401,512 A
`”9% 131111113“ :1
`424/458
`~~~~~~~~~~~~~~~~
`5,407,686 A
`4/1995 P 01656;
`~
`5,413,777 A
`5/1995 $113112:31
`424/490
`514/535
`5,414,014 A
`5/1995 Schneider et al.
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`5422 343 A
`6/1995 Y
`1
`514/45
`~~ 514/14
`5,430,021 A
`7/1995 11:18:18,305”.
`
`.
`424/480
`5,445,829 A
`8/1995 Paradjssisetal.
`5457187 A
`10/1995 Gmeiner et al
`536/25 5
`5,462,747 A
`10/1995 Radebaugh etal.
`424/465
`.424/7837
`5,466,446 A
`11/1995 Stiefeletal.
`
`424/4 5 1
`5472 708 A
`”/1995 Ch
`”/1995 Y en ~~~~~~~~~~~~~~~~~~~~~~~~~ 514/254
`5,476,854 A
`
`2/1996 C(i)11111:get”81~~~~~~~~~~~~~~~~
`5,490,962 A
`264/22
`424/451
`5,508,040 A
`4/1996 Chen ........
`
`264/401
`5 518 680 A
`5/1996 C'
`1
`5,538,954 A
`7/1996 K212133211
`514/53
`
`8/1996 Waldstreicher .
`514/284
`5,543,417 A
`
`5 556 839 A
`9/1996 G
`1
`514/29
`"424/494
`5,567,441 A
`10/1996 Clrleene eta.
`
`5576022 A
`“/1996 YAEEAA~~~~~~
`424/472
`5,578,713 A
`11/1996 McGill, 111
`.................. 536/18.5
`5 599 557 A
`2/1997 Johnson et 31
`424/5 00
`
`5,607,685 A
`3/1997 Cimbollek et a1
`424/422
`5633 006 A
`5/1997 Ct
`.
`t
`1
`424/441
`
`9/1997 D? am.“ 31' ~
`{6725359 A
`424/463
`
`~~ 424/409
`5,688,516 A
`“/1997 Rigamieltm
`”/1997 MisuiaaAAA
`5,702,895 A
`43%
`
`'
`5705190 A
`1/1998 Broad etil
`”424/465
`~1
`5,707,646 A
`“1998 Y ..
`424/439
`~
`57195132 A
`2/1998 qumtlafta'
`514/50
`
`2/1998 ane 21.1~~~~~~
`5,719,272 A
`~536/74
`5,725,553 A
`“998 Mang 6th
`606/213
`
`5,733,886 A
`“998 Boemclllng ~~~1~
`514/24
`
`5/1998 Lam? 31/944
`5,756,473 A
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`7/1998 “1:9 ~~
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`5,789,584 A
`8/1998 Christensen etal.
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`5 808017 A
`9/1998 Ch
`536/74
`5,817,321 A
`10/1998 A1531? ~~~~~-~~~~~1
`'424/400
`
`10/1998 M .OVetaA
`5,827,531 A
`424/450
`
`~
`~~ 424/459
`5,837,284 A
`“/1998 Moirtlsofit
`
`~
`5,837,829 A
`“/1998 Ke ‘13
`~
`536/7 4
`5840329 A
`11/1998 B21111
`~~~~~~~~~~~
`,424/458
`11/1998 Carraher, Jr. et al.
`......... 514/493
`5,840,760 A
`
`5,844,105 A
`12/1998 Liuetal.
`................
`53608.5
`..... 514/398
`5,849,776 A
`12/1998 Czernielewski etal.
`5 852180 A
`”/1998 P 11
`536/74
`5858986 A
`“1999 L2,”: 11""""""
`' 514/2'9
`5864023 A
`“1999 Kluet 31' "
`H536/72
`5869170 A
`2/1999 Cfigt~al~~
`”428/3044
`
`
`2/1999 Vermeulen et al
`...... 514/29
`5,872,104 A
`5872 229 A
`2/1999 Liu et al
`536““
`5877243 A
`3/1999 Sarnngafiernr82:32:22,. 524/139
`...... 514/25
`5:883:079 A
`3,1999 Zopfetal.
`
`..
`5,892,008 A
`4999 Kuetal.
`536/185
`5,910,322 A
`6/1999 Rivett etal.
`424/484
`7/1999 Knowlton ..................... 607/102
`5,919,219 A
`7/1999 Saleki-Gerhardtetal.
`5,919,489 A
`424/501
`5,919,916 A
`7/1999 Graceyetal.
`.................. 536/7.2
`
`
`
`
`
`5,929,219 A
`5’932’710 A
`5,945,124 A
`8883888 A
`’
`’
`5,980,942 A
`5,985,643 A
`5,998,194 A
`6’008’195 A
`6,010,718 A
`6,013,507 A
`6’020’002 A
`6,027,748 A
`8828888 A
`6051255 A
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`6,051,703 A
`2828888 A
`’
`’
`6,063,613 A
`6,063,917 A
`6,068,859 A
`6,110,925 A
`6,117,843 A
`6’120’803 A
`6,127,349 A
`6,132,768 A
`6’132’771 A
`6’136’587 A
`88282518: A
`’
`’
`6,162,925 A
`6,183,778 B1
`6,187,768 B1
`6’214’359 B1
`6,218,380 B1
`6,228,398 B1
`6’231’875 B1
`6,248,363 B1
`6,251,647 B1
`6,265,394 B1
`6’270’805 B1
`6,280,771 B1
`6’294’199 B1
`6,294,526 B1
`6,296,873 B1
`6,297,215 B1
`6,299,903 B1
`6’306’436 B1
`6,309,663 B1
`6,322,819 B1
`6,333,050 B2
`6,340,475 B2
`6,352,720 B1
`6,358,525 B1
`6,358,528 B1
`6’383’471 B1
`6,384,081 B2
`6,391,614 B1
`6,399,086 B1
`6,403,569 B1
`6,406,717 B2
`6,406,880 B1
`8228888 81
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`,
`,
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`6,514,518 B2
`6,515,010 Bl
`6,515,116 B2
`6,530,958 B1
`6,541,014 B2
`6,544,555 B2
`6,548,084 B2
`6,550,955 B2
`
`................................ 536/7.2
`7/1999 H_ill
`" 536/18'7
`8/1999 Llu etal'
`
`8/1999 Sachs et al.
`424/472
`18883; 8838mm etifl' """""""""43211783
`
`ajlmaeta' """""""""
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`11/1999 Tomasz etal.
`................ 435/243
`12/1999 Summers,Jr.etal.
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`" 514/14
`”/1999 seISted """"""
`
`.
`424/464
`1/2000 Al-Razzaketal.
`............. 435/2523
`1/2000 Tomasz etal.
`”000 Myersetal'
`................... 424/458
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`2218888 88%: 21:1 """"""""""" 2388:;
`
`424/482
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`1
`on eye”
`
`.....
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`28888 31111009114111.
`'
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`
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`5/2000 De Lencastre et a1
`435/252.3
`
`.......
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`540/217
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`.
`424/490
`
`.
`8/2000 Williams et al.
`514/272
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`.
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`
`”000 wong etal.
`424/473
`
`..... 514/77
`10/2000 Chasalow .
`.. 424/458
`10/2000 Sachs etal.
`
`"
`10/2000 Depul et 31'
`424/468
`
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`
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`
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`..........
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`............... 514/192
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`424/465
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`..... 514/12
`10/2001 Rivett e131.
`......
`424/464
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`424/464
`10/2001 Patel etal.
`.......
`424/450
`11/2001 Burnsideetal
`424/494
`
`12/2001 Wong etal.
`424/473
`.................... 424/469
`1/2002 Shell et a1.
`3/2002 Martin et a1.
`................. 424/464
`3/2002 Guo et a1.
`........
`424/464
`
`3/2002 Grimmett etal.
`424/474
`
`""" 424/45
`”002 Chen etal'
`5/2002 Berman
`514/621
`
`5/2002 Tomasz etal.
`......
`435/2532
`
`6/2002 Katzhendleretal.
`424/405
`6/2002 Achterrath ............ 514/50
`
`6/2002 Cherukuri
`.
`424/484
`
`6/2002 Thornton ................. 435/32
`
` 8,8888 Exitifigerem'
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`' """""
`'
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`51476
`
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`11/2002 Wolff .....
`. 514/252.17
`
`12/2002 Pena et a1.
`.. 424/433
`
`...........
`12/2002 Royer
`424/468
`1/2003 Bekkaouietal.
`................. 435/6
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`,,,,,,,,,,,,,,,, 536/7'2
`2/2003 Monkhouse etal.
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`2/2003 Suhetal.
`..
`536/7.2
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`623/2351
`
`
`4/2003 Rudnic etal~ ~
`424/400
`4/2003 Rudnic et31~ ~~~~~~~~~~~~~~~~~ 424/468
`4/2003 Leonard etal.
`............... 424/482
`4/2003 D’Silva ......................... 366/130
`
`
`
`
`
`
`
`.
`
`

`

`US 8,313,776 B2
`
`Page 3
`
`6,551,584 B2
`
`6,551,616 B1
`6,558,699 B2
`6,565,873 B1
`6,565,882 B2
`6,569,463 B2
`6,585,997 B2
`6,599,884 B2
`6,605,069 B1
`6,605,300 B1
`6,605,609 B2
`6,605,751 B1
`6,610,323 B1
`6,610,328 B2
`6,617,436 B2
`6,623,757 B2
`6,623,758 B2
`6,624,292 B2
`6,627,222 B2
`6,627,743 B1
`6,630,498 B2
`6,632,453 B2
`6,635,280 B2
`6,638,532 B2
`6,642,276 B2
`6,663,890 B2
`6,663,891 B2
`6,667,042 B2
`6,667,057 B2
`6,669,948 B2
`6,669,955 B2
`6,673,369 B2
`6,682,759 B2
`6,696,426 B2
`6,702,803 B2
`6,706,273 B1
`6,723,340 B2
`6,723,341 B2
`6,730,320 B2
`6,730,325 B2
`6,735,470 B2
`6,740,664 B2
`6,746,692 B2
`6,756,057 B2
`6,767,899 B1
`6,777,420 B2
`6,783,773 B1
`6,818,407 B2
`6,824,792 B2
`6,872,407 B2
`6,878,387 B1
`6,906,035 B2
`6,929,804 B2
`6,946,458 B2
`6984401 B2
`6,991,807 132
`7,008,633 B2
`2001/0046984 A1
`2001/0048944 A1
`2002/0004070 A1
`2002/0004499 A1
`2002/0015728 A1
`2002/0028920 A1
`2002/0042394 A1
`2002/0068078 A1
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`FOREIGN PATENT DOCUMENTS
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`4/2001
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