Amorphous carvedilol dihydrogen phosphate
The invention encompasses novel amorphous and crystalline forms of carvedilol phosphate, carvedilol hydrogen phosphate, and carvedilol dihydrogen phosphate as well as methods of making the novel amorphous and crystalline forms. Also disclosed are pharmaceutical compositions comprising the novel amor...
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Format | Patent |
Language | English |
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14.02.2012
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Abstract | The invention encompasses novel amorphous and crystalline forms of carvedilol phosphate, carvedilol hydrogen phosphate, and carvedilol dihydrogen phosphate as well as methods of making the novel amorphous and crystalline forms. Also disclosed are pharmaceutical compositions comprising the novel amorphous and crystalline forms and uses thereof. |
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AbstractList | The invention encompasses novel amorphous and crystalline forms of carvedilol phosphate, carvedilol hydrogen phosphate, and carvedilol dihydrogen phosphate as well as methods of making the novel amorphous and crystalline forms. Also disclosed are pharmaceutical compositions comprising the novel amorphous and crystalline forms and uses thereof. |
Author | Abramov, Mili Turgeman, Eran Levi, Sigalit Ini, Santiago |
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References | Brittain et al. #2 "Effects of pharmaceutical processing on drug polymorphs and solvates" in Polymorphism in Pharmaceutical Solids, vol. 95, p. 331-361. Brittain, "Polymorphism in Pharmaceutical Sciences." 183-226 (1999). Tarur et al. (2007/0191456) 20070800 Hildesheim et al. (6699997) 20040300 Eagleson, "Concise Encyclopedia Chemistry," p. 872-873 (1993). (WO 99/05105) 19990200 (WO 2007/077111) 20070700 Hildesheim et al. (2002/0143045) 20021000 Express-Phama-Online (http://www.expresspharmaonline.com/2003/edit02.shtml). (0893440) 19990100 Leinert (4985454) 19910100 Kor et al. (2003/0166702) 20030900 (0 918 055) 19990500 Leinert (5071868) 19911200 (WO 2004/094378) 20041100 Chawla, et al. "Challenges in Polymorphism of Pharmaceuticals", CRIPS vol. 5, No. 1 Jan.-Mar. 2004, p. 9-12. Kumar et al. (2007/0027202) 20070200 Scalone et al. (7169935) 20070100 (WO 2007/144900) 20071200 Chen et al. (2004/0152756) 20040800 Burke et al. (2006/0182804) 20060800 Kor et al. (6710184) 20040300 Hildesheim et al. (7056942) 20060600 Hildesheim et al. (7126008) 20061000 Bubendorf et al. (2004/0198812) 20041000 Chen et al. "Synthesis and Crystal Structure of Carvedilol" Jiegou Huaxue, vol. 17, No. 5, Sep. 1998, pp. 325-328. Offer of Information, dated Sep. 19, 2007, from related Japanese Patent Application No. 2002-504998 with translation. Express-Pharma-Online (http://www.expresspharmaonline.com/20031023/edit02.shtml). Bryn et al., Solid-State Chemistry of Drugs, SSCI, Inc., Second edition, p. 62-63 (1999). (WO2008122105) 20081000 Wall, "Pharmaceutical Applications of Drug Crystal Studies", Pharmaceutical Manufacturing, vol. 3, No. 2, pp. 33-42, Feb. 1986. Lukas-Laskey et al. (5902821) 19990500 Bubendorf et al. (2006/0148878) 20060700 "X-Ray Diffraction," U.S. Pharmacopia #23, National Formulatry #18, p. 1843-1844 (1995). Wiedemann et al. (4503067) 19850300 Newman, et al. "Solid-State analysis of the active pharmaceutical ingredient in drug prodcuts" DDT vol. 8 Oct. 2003, p. 898-905. Ramanjaneyulu et al. (2007/0055069) 20070300 (WO 2004/041783) 20040500 (WO 2005/115981) 20051200 Japanese Office Action from related Japanese Patent Application No. 2002-504998, mailed May 7, 2008, with English translation. Beyer et al. (6730326) 20040500 (WO 01/35938) 20010500 (WO 2005/080329) 20050900 Zolss et al. (4767784) 19880800 Rouhi et al., "The Right Stuff," Chemical & Engineering News, p. 31-35 (2003). Mai et al. (4990668) 19910200 Autant et al. (6022562) 20000200 Wiedemann et al. (4438128) 19840300 (WO 2005/113502) 20051200 (WO 2006/061364) 20060600 Brook et al. (2005/0240027) 20051000 Chhabada et al. (2006/0270858) 20061100 Brittain, "Polymorphism in Pharmaceutical Sciences." 1-2, 178-179, 185-186, 199-201, 219, 235, 237-238(1999). Harrington (2007/0197797) 20070800 Brittain, "Polymorphism in Pharmaceutical Solids", p. 228-229 (1999). (929/MUM/2007) 20070500 Scalone et al. (2004/0127723) 20040700 (WO 2005/021504) 20050300 Brook et al. (2005/0277689) 20051200 Hildesheim et al. (2004/0225132) 20041100 Leinert (4697022) 19870900 (WO 2005/051383) 20050600 Hercek et al. (2006/0167077) 20060700 Lukas-Laskey et al. (5760069) 19980600 Kor et al. (2004/0171665) 20040900 (WO 03/059807) 20030700 Knipp et al. (2007/0112054) 20070500 Leinert (4824963) 19890400 Haleblian, "Characterization of Habits and Crystalline Modification of Solids and Their Pharmaceutical Applications", Journal of Pharmaceutical Sciences, vol. 64, No. 8, pp. 1269-1288, Jul. 1975. Haleblian et al., "Pharmaceutical Applications of Polymorphism", Journal of Pharmaceutical Sciences, vol. 58, No. 8, pp. 911-929, Jul. 1969. Scalone et al. (6777559) 20040800 Brittain, "Polymorphism in Pharmaceutical Solids", p. 331-361 (1999). Carey, et al. "Advanced Organic Chemistry" Third Edition, Part A: Structure and Mechanisms; Plenum Press, pp. 232-239 (1993). (WO 2007/097504) 20070800 |
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Snippet | The invention encompasses novel amorphous and crystalline forms of carvedilol phosphate, carvedilol hydrogen phosphate, and carvedilol dihydrogen phosphate as... |
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