In situ salt screening - A useful technique for discovery support and preformulation studies

Pharmaceutical Development and Technology

Volumn 3, Issue 2, 1998, Pages 215-223

  Tong, Wei Qin ^a   Whitesell, Graham ^a  

^a GLAXOSMITHKLINE   (United States)

Author keywords

Discovery support; In situ salt screening; PH solubility profile; Salt selection; Solubility

Indexed keywords

ALPHA 1A ADRENERGIC RECEPTOR; ALPHA ADRENERGIC RECEPTOR BLOCKING AGENT; CHLORIDE; GW 1818X; INORGANIC SALT; MESYLIC ACID; PHOSPHATE; SUCCINIC ACID; UNCLASSIFIED DRUG;

ARTICLE; DIFFERENTIAL SCANNING CALORIMETRY; DRUG FORMULATION; DRUG SCREENING; DRUG SOLUBILITY; PRIORITY JOURNAL; X RAY DIFFRACTION;

EID: 0031806352     PISSN: 10837450     EISSN: None     Source Type: Journal    
DOI: 10.3109/10837459809028498     Document Type: Article

References (10)

1. S. M. Berge, L. D. Bighley, and D. C. Monkhouse, Pharmaceutical salts, J. Pharm. Sci., 66, 1-19 (1977).
2. L. D. Bighley, S. M. Berge, and D. C. Monkhouse, Salt forms of drugs and absorption, in Encyclopedia of Pharmaceutical Technology, Vol. 13 (J. Swarbrick and J. C. Boylan, eds.), Marcel Dekker, Inc., New York, 1995, pp. 453-499.
3. P. L. Gould, Salt selection of basic drugs, Int. J. Pharm., 33, 201-217 (1986).
4. K. R. Morris, M. G. Fakes, A. B. Thakur, A. W. Newman, A. K. Singh, J. J. Venit, C. J. Spagnuolo, and A. T. M. Serajuddin, An integrated approach to the selection of optimal salt form for a new drug candidate, Int. J. Pharm., 105, 209-217 (1994).
5. J. I. Wells, Pharmaceutical Preformulation: The Physicochemical Properties of Drug Substances, Ellis Horwood Limited, Chichester, England, 1988.
6. L. J. Ravin and G. W. Radebaugh, Preformulation, in Remington's Pharmaceutical Sciences, 18th ed. (A. R. Gennaro, ed.), Mack Publishing Company, Easton, PA, 1990.
7. R. M. Shanker, K. V. Carola, P. J. Baltusis, R. T. Brophy, and T. A. Hatfield, Selection of appropriate salt form(s) for new drug candidates, Pharm. Res., 11(10), s-236 (1994).
8. W. Q. Tong, K. Adkison, B. L. Bray, L. A. Gatlin, F. W. Lee, M. A. Patrick, C. W. Spancake, and G. Whitesell, Salt and crystal form selection for GW1818, an Alpha1A antagonist for the treatment of BPH, Pharm. Res., 13(9), s-556 (1996).
9. W. Ramette, Chemical Equilibrium and Analysis, Addison-Wesley Publishing Company, Reading, MA, 1981.
10. S. F. Kramer and G. L. Flynn, Solubility of organic hydrochlorides, J. Pharm. Sci., 61, 1896-1904 (1972).