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(12) United States Patent (10) Patent No.: US 8,088,414 B2 Siepmann Et Al

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(12) United States Patent (10) Patent No.: US 8,088,414 B2 Siepmann Et Al US008.088414B2 (12) United States Patent (10) Patent No.: US 8,088,414 B2 Siepmann et al. (45) Date of Patent: Jan. 3, 2012 (54) LATEXORPSEUDOLATEX COMPOSITIONS, FOREIGN PATENT DOCUMENTS COATINGS AND COATING PROCESSES EP O315414 A1 5, 1989 EP O425O23 A2 5, 1991 (75) Inventors: Juergen Siepmann, Lille (FR); EP 143O889. A 6, 2004 JP 1997-194347 7/1997 Florence Siepmann, Lille (FR); Brian WO WO-O 132152 A1 5, 2001 A. C. Carlin, Pittsgrove, NJ (US); WO WO-02085.335 A1 10/2002 Jian-Xin Li, North Brunswick, NJ (US) OTHER PUBLICATIONS (73) Assignee: FMC Corporation, Philadelphia, PA BASF Press Release, “BASF Extends Kollicoat IR Range.” Dec. 13, (US) 2004. Lange, Ronald F.M. et al., “The Development of an Instant Release (*) Notice: Subject to any disclaimer, the term of this Tablet Coating.” International Pharmaceutical Excipients Council Europe News, May 2004. patent is extended or adjusted under 35 Rohera, Ghagwan D. and Parikh, Nilesh H., “Influence of Type and U.S.C. 154(b) by 0 days. Level of Water-Soluble Additives on Drug Release and Surface and Mechnical Properties of Surelease(R) Films.” Pharmaceutical Devel (21) Appl. No.: 11/669,630 opment and Technology, 2002, pp. 421-432, vol. 7, No. 4. Kollicoat(R) IR. Technical Information Bulletin, Jul. 2006. Kollicoat(R) SR 30 D, Technical Information Bulletin, Aug. 2005. (22) Filed: Jan. 31, 2007 Mies, S. et al., “Correlation of Drug Permeation Through Isolated Films and Coated Dosage Forms Based on Kollicoat(R) SR30D/IR.” (65) Prior Publication Data AAPS Annual Meeting and Exposition, Nov. 7-11, 2004, Baltimore, Maryland. US 2007/O1841 O2 A1 Aug. 9, 2007 Kolter, K. and Ruchatz, F. “Kollicoat(R) SR 30 D-A New Sus tained Release Excipient.” The 26th International Symposium on Related U.S. Application Data Controlled Release of Bioactive Materials, Jun. 20-25, 1999, Boston, MA. (60) Provisional application No. 60/870,012, filed on Dec. Bordaweker, M., Zia, H., and Quadir, A., “Release Characteristics of 14, 2006, provisional application No. 60/790,418, Selected Drugs with a Newly Developed PolyvinylAcetate Disper filed on Apr. 7, 2006, provisional application No. sion.”31st International Symposium on Controlled Release of Bioac tive Material, Jun. 12-16, 2004, Honolulu, Hawaii. 60/771,199, filed on Feb. 7, 2006. Meyer, K. and Kolter, K., “Reliability of Drug Release from an Innovative Single Unit Kollicoat(R) Drug Delivery System.” 31st (51) Int. Cl. International Symposium on Controlled Release of Bioactive Mate A 6LX 9/50 (2006.01) rials, Jun. 12-16, 2004, Honolulu, Hawaii. (52) U.S. Cl. ....................................................... 424/495 Postel, M. et al., Innovative Tilidine-Naloxone Sustained Release (58) Field of Classification Search ........................ None Drug Delivery Systems based on Kollicoat(R) Polymers, Poster, May See application file for complete search history. 21, 2004. * cited by examiner (56) References Cited Primary Examiner — Michael G. Hartley U.S. PATENT DOCUMENTS Assistant Examiner — Paul Dickinson 4,330,338 A 5, 1982 Banker 4,975,284. A * 12/1990 Stead et al. ................... 424/497 (57) ABSTRACT 5,370,880 A 12/1994 Jones et al. 6,129,933 A 10, 2000 Oshlack et al. A composition comprising: (i) at least one latex or pseudola 6,274,173 B1* 8/2001 Sachs et al. ................... 424/480 tex water insoluble film former, (ii) at least one permeation 2002/0155156 A1 10/2002 Mulye enhancing agent and, optionally, (iii) one or more plasticizers. 2002/0192285 A1 12/2002 Mulye The present invention is also directed to substrates coated 2003. O107149 A1 6/2003 Yang et al. 2003/0175342 A1* 9, 2003 Kolter et al. .................. 424/468 with the composition of the invention, films made from the 2005, 0196444 A1* 9, 2005 Kolter et al. ... 424/472 composition and methods for making and using Such compo 2005/0220878 A1* 10/2005 Fegely et al. ................. 424/473 sitions, coated Substrates and films. 2006/0269605 A1 11/2006 Lizio et al. 2007. O1841.98 A1 8, 2007 Li et al. 36 Claims, 45 Drawing Sheets U.S. Patent Jan. 3, 2012 Sheet 1 of 45 US 8,088,414 B2 (q)I9.InáI 91 O 92 % 'sseu uy Mup (e)I9.InãIJI O N CN %ueu Ooueenw U.S. Patent Jan. 3, 2012 Sheet 2 of 45 US 8,088,414 B2 100 5 0 O 0.00005 0.0001 0.00015 0.0002 time/thickness, hlum? Figure 2 U.S. Patent Jan. 3, 2012 Sheet 3 of 45 US 8,088,414 B2 O G/. N % 'SSeu Luy Wup O G/ N 9, ueuoo JeeM U.S. Patent Jan. 3, 2012 Sheet 4 of 45 US 8,088,414 B2 100 57 O5 2 5 O 0.00005 0.0001 0.00015 0.0002 timethickness, hlum? Figure 4 U.S. Patent Jan. 3, 2012 Sheet 5 of 45 US 8,088,414 B2 (q)S9.InáH L C N L CN 9, 'sseu u Aup O 00|| 91 L CN %ueuoso JeeM U.S. Patent Jan. 3, 2012 Sheet 6 of 45 US 8,088,414 B2 100 75 5 O 2 5 O 0.00005 0.0001 0.00015 O.0002 time/thickness, hlum Figure 6 U.S. Patent Jan. 3, 2012 Sheet 7 of 45 US 8,088,414 B2 C Vf ds aa S S. N g d 3. 2. CN O O C O O N GN vm % “SSeu up. Aup C CO o SS S SS SS SS S C C. V N. O. Y v aa } Es sN d e e CX CN C OX s&SESS o O C d O N N vals %ueuoso JeeM U.S. Patent Jan. 3, 2012 Sheet 8 of 45 US 8,088,414 B2 100 5 O 2 5 O 0.00005 O.0001 O.OOO15 0.0002 time?thickness?, hlum? Figure 8 U.S. Patent Jan. 3, 2012 Sheet 9 of 45 US 8,088,414 B2 f O 00|| N CN % 'SSeu u Aup (e)63.ináI L O N L CN %ueuOpeeM U.S. Patent Jan. 3, 2012 Sheet 10 of 45 US 8,088,414 B2 1 OO x x X A A X X x A* A A e ‘a 8 75 XXa & XXA AA 8 aS X A A C> KX o A <> S;O 2. & KX 50 o° as x 30% . A 20% s & 10% 25 0% O O 0.00005 0.0001 0.00015 0.0002 time?thickness, hi?um? Figure 10 U.S. Patent Jan. 3, 2012 Sheet 11 of 45 US 8,088,414 B2 60 X 10% A 5.0% 40 (> 2.5 O% 0.0% - theory O 2 4. 6 8 time, h Figure 11 U.S. Patent Jan. 3, 2012 Sheet 12 of 45 US 8,088,414 B2 8 6 {0 Water g Otheophylline E (9 se d O 2.5 5 7.5 10 Kollicoat IR content, % Figure 12 U.S. Patent Jan. 3, 2012 Sheet 13 of 45 US 8,088,414 B2 100 KX C 90 - SS C us () v E 80 E -- 0.0% O -(-2.5% 70 - A - 5.0% - x - 10.0% 60 O 2 4. 6 8 time, h Figure 13 U.S. Patent Jan. 3, 2012 Sheet 14 of 45 US 8,088,414 B2 100 5 O 25 O 0.00005 0.000 1 0.00015 0.0002 time/thickness, hlum? Figure 14 U.S. Patent Jan. 3, 2012 Sheet 15 of 45 US 8,088,414 B2 Figure 15(a) -O-20% PVA-PEG graft copolymer 100 57 O5 2 5 Figure 15(b) -O-20% PVA-PEG graft copolymer 100 57O5 2 5 U.S. Patent Jan. 3, 2012 Sheet 16 of 45 US 8,088,414 B2 Figure 15(c) 100 75 5 O -- 5% coating level 25 O -o- 10% - A - 15% -O-20% O CO O 2 4 6 8 time, h Figure 15(d) 100 7 5 5 O -H 5% coating level 25 O -o- 10% - A - 15% & C -o- 20%O O %g O 2 4. 6 8 time, h U.S. Patent Jan. 3, 2012 Sheet 17 of 45 US 8,088,414 B2 Figures 16(a)-16(d) 10% coating level 20% coating level (a) (b) 100 - - - 10% carrageenant-- 100 - A - 10% carrageenan -o- 5.0% -- 0.0% 75 7 5 5 O 5 O 1.0 2 5 2 5 O O O 2 4 6 O 2 4. 6 time,h time,h (c) (d) 100 - - A - 10% caragena- 100 - A - 10% carrageenan -o-, 5.0% -- 0.0% 75 7 5 5 O 5 O 7. 4 2 5 2 5 U.S. Patent Jan. 3, 2012 Sheet 18 of 45 US 8,088,414 B2 Figure 16(e) 100 7 5 - A - Carrageenan - - -o- - - PGalginate - - - - - PVA-PEG graft copolymer 5 O 2 5 O O 2 4 6 8 time, h Figure 16(f) 100 75 5 O -A - Carrageenan - - -o- - - PG alginate 2 5 - - - - - PVA-PEG graft copolymer U.S. Patent Jan. 3, 2012 Sheet 19 Of 45 US 8,088,414 B2 Figures 16(g)-16(i) 10% coating level 20% coating level (g) (h) 100 100 -- uncured -c- 1 c 60°C -- uncured -0-2 d 60C --> 1 d 60 °C 75 ... c60 °C 75% RH 75 -- 2d 60 °C - 260 °C 75% RH A 1 c 60°C 75% RH -- 2d 60 °C 75% RH pH 5 O 5 1.0 25 2 5 O (i) (j) OO 100 -- uncured -o-, 1 d 6OC -- uncured 75 -- 2d 6OC 75 -&- 1 c 60°C SS -- 2d 6OC -A-1 desOC 75% RH "G s - 26OC 75 RH - 1 c 60°C 75% RH S 50 - -2d 60°C 5% RH pH 5 O E " 7.4 25 2 5 U.S.
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