Salt Selection in Drug Development - Pharmaceutical Technology

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Salt Selection in Drug Development
The selection of an appropriate salt form for a potential drug candidate is an opportunity to modulate its characteristics to improve bioavailability, stability, manufacturability, and patient compliance.


Pharmaceutical Technology
Volume 3, Issue 32

24. R. Hilfiker, F. Blatter, and M.V. Raumer, "Relevance of Solid-State Properties for Pharmaceutical Products," in Polymorphism in the Pharmaceutical Industry, R. Hilfiker, Ed. (Wiley–VCH, Weinheim, Germany, 2006), pp. 1–19.

25. S. Balbach and C. Korn, "Pharmaceutical Evaluation of Early Development Candidates—the 100-mg Approach," Int. J. Pharm. 275 (1–2), 1–12 (2004).

26. G. Davies, "Changing the Salt, Changing the Drug," Pharm. J. 266 (7138), 322–323 (2001).

27. J.D. Higgins and W.L. Rocco, "Pharma Preformulation: A Stop Along the Drug Development Highway," Today's Chemist at Work 12 (7), 22–26 (2003).

28. A.T.M. Serajuddin et al., "Preformulation Study of a Poorly Water Soluble Drug α-pentyl-3-(2-quinolinylmethoxy) benzenemethanol: Selection of the Base for Dosage Form Design," J. Pharm. Sci. 75 (5), 492–496 (1986).

29. R.J. Bastin, M.J. Bowker, and B.J. Slater, "Salt Selection and Optimisation Procedures for Pharmaceutical New Chemical Entities," Org. Proc. Res. Dev. 4 (5), 427–435 (2000).

30. "Orinase Diagnostic-Product Information," http://www.pfizer.com/pfizer/download/uspi_orinase.pdf, accessed Jan. 21, 2006.

31. R.M. Everett et al., "Nephrotoxicity of Pravadoline Maleate (WIN 48098-6) in Dogs: Evidence of Maleic Acid-Induced Acute Tubular Necrosis," Fundam. Appl. Toxicol. 21 (1), 59–65 (1993).

32. D. J. Snodin, "Residues of Genotoxic Alkyl Mesylates in Mesylate Salt Drug Substances: Real or Imaginary Problems?," Regul.Toxicol. Pharmacol. 45 (1), 79–90 (2006).

33. A. Allerman, "New Drug Watch," http://www.pec.ha.osd.mil/Updates/0307web/Aug-Sep_03_Update_Page_5.htm, accessed Dec. 15, 2006.

34. W.Q. Tong and G. Whitesell, "In situ Salt Screening—A Useful Technique for Discovery Support and Preformulation Studies," Pharm. Dev. Technol. 3 (2), 215–223 (1998).

35. C.R. Gardner et al., "Application of High Throughput Technologies to Drug Substance and Drug Product Development," Comput. Chem. Eng. 28 (6–7), 943–953 (2004).

36. A.W. Newman and G.P. Stahly, "Form Selection of Pharmaceutical Compounds," in Handbook of Pharmaceutical Analysis, vol. 117, L. Ohannesian and A.J. Streeter, Eds. (Marcel Dekker, New York, 2002), pp. 1–58.

37. G.L. Engel et al., "Salt Form Selection and Characterization of LY333531 Mesylate Monohydrate," Int. J. Pharm. 198 (2), 239–247 (2000).


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