Improvement of dissolution rates of poorly water soluble APIs using novel spray freezing into liquid technology

Pharmaceutical Research

Volumn 19, Issue 9, 2002, Pages 1278-1284

  Hu, J ^a   Rogers, T L ^a   Brown, J ^a   Young, T ^b,c   Johnston, K P ^c   Williams III, R O ^a  

^a UNIVERSITY OF TEXAS AT AUSTIN   (United States)

^b DOW CHEMICAL COMPANY   (United States)

^c The University of Texas at Austin   (United States)

Author keywords

Carbamazepine; Danazol; Dissolution; Spray freezing into liquid; Stability

Indexed keywords

CARBAMAZEPINE; DANAZOL; POLOXAMER; SOLVENT; TETRAHYDROFURAN; WATER;

ARTICLE; DISSOLUTION; DRUG FORMULATION; DRUG SOLUBILITY; DRUG STABILITY; DRUG STORAGE; ENGINEERING; FREEZING; LIQUID; NEBULIZATION; PARTICLE SIZE; PHASE TRANSITION; POROSITY; POWDER; PRIORITY JOURNAL; SCANNING ELECTRON MICROSCOPY; X RAY DIFFRACTION;

DRUG COMPOUNDING; FREEZING; PARTICLE SIZE; PHARMACEUTICAL PREPARATIONS; SOLUBILITY; TECHNOLOGY, PHARMACEUTICAL; WATER;

EID: 0036746811     PISSN: 07248741     EISSN: None     Source Type: Journal    
DOI: 10.1023/A:1020390422785     Document Type: Article

References (30)

1. G. L. Amidon, H. Lnnernas, V. P. Shah, and J. R. Crison. A theoretical basis for a biopharmaceutic drug classification: the correlation of in vitro drug product dissolution and in vivo bioavailability. Pharm. Res. 12:413-420 (1995).
2. L. Bertisson. Clinical pharmacokinetics of carbamazepine. Clin. Pharmacokinet. 3:128-143 (1978).
3. T. Loftsson and H. Frioriksdottir. The effect of water-soluble polymers on the aqueous solubility and complexing abilities of β-cyclodextrin. Int. J. Pharm. 163:115-121 (1998).
4. Y. F. Maa, P. A. Nguyen, T. Sweeney, S. J. Shire, and C. C. Hsu. Protein inhalation powders: spray drying vs. spray freeze drying. Pharm. Res. 16:249-254 (1999).
5. 2 and cryogenic spray-freezing technologies. Drug Dev. Ind. Pharm. 27:1003-1015 (2001).
6. W. Wang. Lyophilization and development of solid protein pharmaceuticals. Int. J. Pharm. 203:1-60 (2000).
7. T. H. Adams, J. P. Beck, and R. C. Menson. Novel particulate compositions. US4323478 (1982).
8. A. R. Briggs and T. J. Maxwell. Method of preparation of lyophilized biologic products. US3932943 (1976).
9. D. B. Dunn, G. J. Masavage, and H. A. Sauer. Method of freezing solution droplets and the like using immiscible refrigerants of differing densities. US3653222 (1972).
10. I. R. Buxton and J. M. Peach. Process and apparatus for freezing a liquid medium. US4470202 (1984).
11. H. A. Sauer. Method and apparatus for freeze-freeze drying. US3484946 (1969).
12. The Montreal Protocol on Substances That Deplete the Ozone Layer. 1987.
13. R. O. Williams, T. L. Rogers, and J. Liu. Study of solubility of steroids in hydrofluoroalkane propellants. Drug Dev. Ind. Pharm. 25:1227-1234 (1999).
14. W. R. Gombotz, M. S. Healy, L. R. Brown, and H. E. Auer. Process for producing small particles of biologically active molecules. WO90/13285 (1990).
15. M. I. Gusman and S. M. Johnson. Cryochemical method of preparing ultrafine particles of high-purity superconducting oxides. US4975415 (1990).
16. B. D. Cullity. Chemical analysis by X-ray diffraction. In B. D. Cullity (eds.), Elements of X-ray Diffraction, Addison-Wesley, Massachusetts, 2001 pp. 397-420.
17. S. Brunauer, P. H. Emmett, and E. Teller. Adsorption of gases in multimolecular layer. J. Am. Chem. Soc. 60:309-319 (1938).
18. E. Galia, E. Nicolaides, D. Horter, R. Lobenberg, C. Reppas, and J. B. Dressman. Evaluation of various dissolution media for predicting in vivo performance of class I and II drugs. Pharm. Res. 15:698-705 (1998).
19. S. Brown, G. Rowley, and J. T. Pearson. Surface treatment of the hydrophobic drug danazol to improve drug dissolution. Int. J. Pharm. 165:227-237 (1998).
20. B. L. Pedersen, A. Mullertz, H. Brondsted, and H. C. Kristensen. A comparison of the solubility of danazol in human and simulated gastrointestinal fluids. Pharm. Res. 17:891-894 (2001).
21. M. Shibata, H. Kokubo, K. Morimoto, T. Ishida, and M. Inoue. X-ray structural studies and physicochemical properties of cimetidine polymorphism. J. Pharm. Sci. 72:1436 (1983).
22. G. G. Liversidge and K. C. Cundy. Particle size reduction for improvement of oral bioavailability of hydrophobic drugs: 1. Absolute oral bioavailability of nanocrystalline danazol in beagle dogs. Int. J. Pharm. 125:91-97 (1995).
23. M. J. Lowes, M. R. Caira, A. P. Lotter, and J. G. VanderWatt. Physicochemical properties and X-ray structure studies of the trigonal polymorph of carbamazepine. J. Pharm. Sci. 76:744-752 (1987).
24. N. Kondo, T. Iwao, H. Masuda, K. Yamanouchi, Y. Ishihara, N. Yamada, T. Haga, Y. Ogawa, and K. Yokoyama. Improved oral absorption of a poorly water soluble drug, HO-221, by wet-bead milling producing particles in submicron region. Chem. Pharm. Bull. 41:737-740 (1993).
25. A. H. Lefebvre. Atomization and Sprays, Hemisphere Publishing Corp., New York, 1989.
26. H. R. Costantino, L. Firouzabadian, K. Hogeland, C. Wu, C. Beganski, K. G. Carrasquillo, M. Córdova, K. Griebenow, S. E. Zale, and M. A. Tracy. Protein spray-freeze drying. Effect of atomization condition on particle size and stability. Pharm. Res. 17:1374-1383 (2000).
27. V. Bakatselou, R. C. Oppenheim, and J. B. Dressman. Solubilization and wetting effects of bile salts on the dissolution of steroids. Pharm. Res. 8:1461-1469 (1991).
28. A. P. Martin. Interfacial phenomena. In A. P. Martin (ed.), Physical Pharmacy, Lea & Febiger, Philadelphia, 1993 pp. 384-386.
29. A. W. Adamson and A. P. Gast. Physical Chemistry of Surfaces, Wiley, New York, 1997.
30. V. P. Shah, Y. Tsong, P. Sathe, and J.-P. Liu. In vitro dissolution profile comparison-statistics and analysis of the similarity factor, f2. Pharm. Res. 15:889-896 (1998).