Strategy for the Prediction and Selection of Drug Substance Salt Forms - Pharmaceutical Technology

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Strategy for the Prediction and Selection of Drug Substance Salt Forms
Through consideration of the ionic equilibria of acids and bases, one may readily calculate the formation constant of a salt species solely on the basis of knowledge of the pKA value of the acid and the pKB value of the base.


Pharmaceutical Technology


2. B.D. Anderson and K.P. Flora, "Preparation of Water-Soluble Compounds Through Salt Formation," in The Practice of Medicinal Chemistry, C.G. Wermuth, Ed. (Academic Press, New York, NY, 1996), pp. 739–754.

3. P.H. Stahl and C.G. Wermuth, Handbook of Pharmaceutical Salts (Wiley-VCH, Weinheim, Germany, 2002.)

4. L.D. Bighley, S.M. Berge, and D.C. Monkhouse, "Salt Forms of Drugs and Absorption," in Encyclopedia of Pharmaceutical Technology, J. Swarbrick and J.C. Boylan JC, Eds. (Marcel Dekker, New York, NY, 1995), pp. 453–499.

5. E.C. Ware and D.R. Lu, "An Automated Approach to Salt Selection for New Unique Trazodone Salts," Pharm. Res. 21 (1), 177–184 (2004).

6. D.A. Haynes, W. Jones, and W.D.S. Motherwell, "Occurrence of Pharmaceutically Acceptable Anions and Cations in the Cambridge Structural Database," J. Pharm. Sci. 94 (10), 2111–2120 (2005).

7. P.L. Gould, "Salt Selection for Basic Drugs," Int. J. Pharm. 33 (1–2), 201–217 (1986).

8. K.R. Morris et al., "An Integrated Approach to the Selection of Optimal Salt Form for a New Drug Candidate," Int. J. Pharm. 105 (2), 209–217 (1994).

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

10. M. Sacchetti, "General Equations for In Situ Salt Screening of Multibasic Drugs in Multiprotic Acids," Pharm. Dev. Tech. 5 (4), 579–582 (2000).

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

12. A.T.M. Serajuddin and M. Pudipeddi, "Salt-Selection Strategies," in Handbook of Pharmaceutical Salts, P.H. Stahl and C.G. Wermuth, Eds. (Wiley-VCH, Weinheim, Germany, 2002), pp. 135–160.

13. M.J. Bowker, "A Procedure for Salt Selection and Optimization," in Handbook of Pharmaceutical Salts, P.H. Stahl and C.G. Wermuth, Eds. (Wiley-VCH, Weinheim, Germany, 2002), pp. 161–189.

14. R.B. Hammond et al., "Grid-Based Molecular Modeling for Pharmaceutical Salt Screening: Case Example of 3,4,5,7,8,9-hexahydro-2H-pyrimido-(1,2-a)-primidinium acetate," J. Pharm. Sci. 95 (11), 2361–2372 (2006).

15. Lange's Handbook of Chemistry, J.A. Dean, Ed. (McGraw-Hill, New York, NY, 12th edition, 1979), pp. 5–7.


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