Cocktail-solvent screening to enhance solubility, increase crystal yield, and induce polymorphs

Pharmaceutical Technology

Volumn 32, Issue 1, 2008, Pages 76-95

  Lee, Tu ^a   Shi, Ting Hung ^a  

^a NATIONAL CENTRAL UNIVERSITY   (Taiwan)

Author keywords

[No Author keywords available]

Indexed keywords

CRYSTALLIZATION; POLYMORPHISM; RECRYSTALLIZATION (METALLURGY); SCREENING; SOLUBILITY;

COCKTAIL-SOLVENT SCREENING; SINGLE-SOLVENT SYSTEM; TERNARY SOLVENT MIXTURES;

SOLVENTS;

ACETONITRILE; PROPANOL; SOLVENT; SULFATHIAZOLE; WATER;

ARTICLE; CRYSTAL STRUCTURE; CRYSTALLIZATION; DRUG INDUSTRY; DRUG MANUFACTURE; DRUG SCREENING; DRUG SOLUBILITY; DRUG STRUCTURE; MISCIBILITY; PHARMACEUTICAL ENGINEERING;

EID: 38549117408     PISSN: 15432521     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (29)

1. C. Sanchez, H. Arribart, and M.M. Giraud-Guille,"Biomimetism and Bioinspiration as Tools for the Design of Innovative Materials and Systems," Nature Mater. 4 (4), 277-288 (2005).
2. J. W. Schroer and K.M. Ng, "Process Paths of Kinetically Controlled Crystallization: Enantiomers and Polymorphs," Ind. Eng. Chem. Res. 42 (10), 2230-2244 (2003).
3. W. Beckmann, "Seeding the Desired Polymorph: Background, Possibilities, Limitations, and Case Studies," Org. Proc. Res. Dev. 4 (5), 372-383 (2000).
4. R. A. Granberg and Å.C. Rasmuson, "Solubility of Paracetamol in Pure Solvents," J. Chem. Eng. Data 44 (6), 1391-1395 (1999).
5. R. A. Granberg and Å.C. Rasmuson, "Solubility of Paracetamol in Binary and Ternary Mixtures of Water + Acetone + Toluene," J. Chem. Eng. Data 45 (3), 478-483 (2000).
6. D.J.C. Constable, C. Jimenez-Gonzalez, and R.K. Henderson, "Perspective on Solvent Use in the Pharmaceutical Industry," Org. Proc. Res. Dev. 11 (1), 133-137 (2007).
7. J.W. Mullin, Crystallization, (Butterworth Heinemann, Boston, MA, 3rd ed., 1997), pp. 90-92.
8. 2 and its Desolvation Reaction," Chem. Eur. J. 8 (19), 4454-4460 (2002).
9. N. Blagden et al., "Crystal Chemistry and Solvent Effects in Polymorphic Systems Sulfathiazole," J. Chem. Soc. Faraday Trans. 94 (8), 1035-1044 (1998).
10. 2," Pharm. Res. 18 (5), 682-688 (2001).
11. T. Lee and M.S. Lin, "Sublimation Point Depression of Tris(8-hydroxyquinoline) aluminum (III) (Alq3) by Crystal Engineering," Cryst. Growth Des. 7 (9), 1803-1810 (2007).
12. Y. Kawashima, M. Okumura and H. Takenaka, "Spherical Crystallization: Direct Spherical Agglomeration of Salicylic Acid Crystals During Crystallization," Science 216 (4550), 1127-1128 (1982).
13. R.A. Granberg and Å.C. Rasmuson, "Crystal Growth Rates of Paracetamol in Mixtures of Water + Acetone + Toluene," AIChE Journal 51 (9), 2441-2456 (2005).
14. M.L. Peterson et al., "Iterative High-Throughput Polymorphism Studies on Acetaminophen and an Experimentally Derived Structure for Form III," J. Am. Chem. Soc. 124 (37), 10958-10959 (2002).
15. J.E. Anderson et al., "Determination of the Onset of Crystallization of N1-2-(thiazolyl)sulfanilamide (sulfathiazole) by UV-Vis and Calorimetry Using an Automated Reaction Platform; Subsequent Characterization of Polymorphic Forms Using Dispersive Raman Spectroscopy," Spectrochimica Acta Part A 57 (9), 1793-1808 (2001).
16. S. Khoshkhoo and J. Anwar, "Crystallization of Polymorphs: the Effect of Solvent," J. Phys. D: Appl. Phys. 26 (8B), B90-B93 (1993).
17. J. Anwar, S.E. Tarling, and P. Barnes, "Polymorphism of Sulfathiazole," J. Pharm Sci. 78 (4), 337-342 (1989).
18. D.C. Grove and G. Keenan, "The Dimorphism of Sulfathiazole," J. Am. Chem. Soc. 63 (1), 97-99 (1941).
19. A.L. Bingham et al., "Over One Hundred Solvates of Sulfathiazole," Chem. Commun. (7), 603-604 (2001).
20. E. Tedesco, D. Giron, and S. Pfeffer, "Crystal Structure Elucidation and Morphology Study of Pharmaceuticals in Development," Cryst. Eng. Comm. 4 (67), 393-400 (2002).
21. N. Blagden and R.J. Davey, "Review: Polymorph Selection - Challenges for the Future?" Cryst. Growth Des. 3 (6), 873-885 (2003).
22. D. Winn and M.F. Doherty, "Modeling Crystal Shapes of Organic Materials Grown from Solution," AIChE J. 46 (7), 1348-1367 (2000).
23. S. Byrn, K. Morris, and S. Comella, "Reducing Time to Market with a Science-Based Product," Pharm. Technol. Outsourcing Resources for the Pharmaceutical Industry supplement, 46-56 (2005).
24. T. Lee, C.S. Kuo, and Y.H. Chen, "Solubility, Polymorphism, Crystallinity, and Crystal Acetaminophen and Ibuprofen by Initial Solvent Screening," Pharm. Technol. 30 (10), 72-92 (2006).
25. N.G. Anderson, Practical Process Research and Development, (Academic Press, New York, 2000), pp. 81-111.
26. E.B. Hershberg and J.E. Christensen, "Manufacture of Soluble Sulfathiazole," US Patent 4070356, (1978).
27. A. Burger and R.D. Dialer, "Neue Untersuchungsergebnisse zur Polymorphic von Sulfathiazol," Pharm. Acta Helv. 58 (3), 72-78 (1983).
28. T.L. Threlfall, "Analysis of Organic Polymorphs: A Review," Analyst 120 (10), 2435-2460 (1995).
29. D. Giron, "Thermal Analysis and Calorimetric Methods in the Characterization of Polymorphs and Solvates," Therm. Acta 248, 1-59 (1995).