Journal of Pharmaceutical Investigation

The Korean Society of Pharmaceutical Sciences and Technology (한국약제학회)
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Effect of Crystal Form on Dissolution of Prednisolone

프레드니솔론의 용출에 미치는 결정형의 영향

  • 손영택 (덕성여자대학교 약학대학) ;
  • 도의선 (덕성여자대학교 약학대학)
  • Published : 2003.06.20
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Abstract

Four different crystal forms of prednisolone, two polymorphic forms and two pseudopolymorphic forms, were obtained by the recrystallization from different organic solvents under varying conditions. The isolated crystal forms were characterized by differential scanning calorimetry (DSC), thermogravimetric analysis (TGA) and X-ray powder diffraction (XRD). Form 1 was the most stable form that had the highest melting point and melt at $250.1^{\circ}C$. Form 2 was a monohydrate and Form 3 was a methanol solvate. The endothermic peak of Form 4 was shown at $230.2^{\circ}C$. When stored at different relative humidity over the period of 3 months, all of the modifications did not undergo transformation. The dissolution patterns of these four modifications were also checked in distilled water at $37{\pm}0.5^{\circ}C$, for 120 minutes. The dissolution rate of Form 4 was highest and those of Form 3, Form 2, Form 1 followed. Form 2, Form 3 and Form 4 had higher dissolution rate than Form 1.

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References

  1. Y. T. Sohn, Pharmaceutical application of polymorphism, Pharmacon, 21, 500-516 (1981)
  2. B. D. Sharma, Allotropes and polymorphs, J. Chem. Educ., 64,404-407 (1987) https://doi.org/10.1021/ed064p404
  3. J. Bemstein, Conformational polymorphism, Stud. Org. Chem. (Amsterdam), 32(Org. Solid Statd Chem.), 471-518 (1987)
  4. M. Kitamura, Polymorphism in crystallization, Kagaku kogaku, 55, 263-264 (1991)
  5. J. Haleblian and W. McCrone, Pharmaceutical applications of polymorphism, J. Pharm. Sci., 58, 911-929 (1969). https://doi.org/10.1002/jps.2600580802
  6. W. C. Kind, P. Varlashkin and C. Li, The applicability of powder x-ray diffraction to the quantification of drug substance polymorphs using a model organic system, Powder Diffr., 8, 180-187 (1993) https://doi.org/10.1017/S0885715600018157
  7. J. Bernstein, Polymorphism and the investigation of structure-property relations in organic solids, Int. Union Crystallogr. Crystallogr. Syrnp. 4 (Org. Cryst. Chern.), 6-26(1991)
  8. F. Bayard, C. Decoret and J. Royer, Structural aspects of polymorphism and phase transition in organic molecular crystals, Stud. Phys. Theor. Chern., 69 (Struct. Prop. Mol. Cryst.), 211-234 (1990)
  9. N. Kaneniwa, M. Otsuka, T. Yamaguchi, T. Hayashi, K. Hayashi, T. Matsumoto, N. Watari and O. Unezawa, Preparation of polymorphs of some crystalline drug powders, Funsai, 33, 30-41 (1989).
  10. E. F. Fiese and T. A. Hagen : Preformulation : In Theory and Practice of Industrial Pharmacy, L. Lachman, H. A. Lieberman and J. L. Kanig(Eds.), 3rd Edition, Lea and Febiger, Philadelphia, pp171 (1986)
  11. D. E. Wouster and W.Tailor Jr., Dissolution kinetics of certain crystalline forms of prednisolone, J. Pharm. Sci., 54, 670-676(1965) https://doi.org/10.1002/jps.2600540503
  12. Y. T. Sohn and E. H. Lee, Crystal form of cephazoline sodium hydrate, Yakhak Hoeji, 40, 306-310 (1996)
  13. Y. T. Sohn and S. H. Park, Effects of crystal modification of cephalothin sodium on dissolution and stability, Yakhak Hoeji, 41, 321-327 (1997)
  14. Y. T. Sohn and J. S. Kim, Effect of crystal form on dissolution of cephradin, J. Kor. Pharm. Sci., 28, 115-119 (1998)
  15. Y. T. Sohn and H. K. Kim, Dissolution of crystal form of cephotaxime sodium, J. Kor. Pharm. Sci., 28, 81-85 (1998)
  16. Y. T. Sohn and I. J. Chun, Crystal form of cefaclor, J Kor. Pharm. sa, 30, 201-206 (2000)
  17. A. Bauer-Brandl and Y. T. Sohn, Crystal modifications of cimetidine: Characterization and evaluation for manufacturing of dosage forms, Eur. J. Pharm. Biopharm., 40(Suppl.), 6S(1994)
  18. Y. T. Sohn, Effect of polymorphism on bioavailability of amoxycillin, Yakhak Hoeji., 39, 438-443 (1995)
  19. Y. T. Sohn, M. S. Park and S. K. Kwon, Polymorphism of biphenyldimethyldicarboxy late, J. Kor. Pharm. Sci., 26, 193199(1996).
  20. Y. T. Sohn and S. H. lung, Effect ofcrystal form on dissolution and stability of droperidol, Yakhak Hoeji, 40, 375-381 (1996)
  21. Y. T. Sohn, Dissolution and transformation of crystal form of piroxicam, Yakhak Hoeji, 40, 513-521 (1996)
  22. Y. T. Sohn and B. Y. Urn, Dissolution of crystal form of glibenclamide, J. Kor. Pharm. Sci., 27, 233-239 (1997)
  23. Y. T. Sohn, J. K. Lee and W. B. 1m, Polymorphism of clarithromycin, Arch. Pharm. Res., 23, 381-384 (2000) https://doi.org/10.1007/BF02975451
  24. A. Burger, Zur Interpretation von Polymorphie-untersuchungen, Acta Pharm. Technol., 28, 1-20 (1982)
  25. A. Burger and K. T. Koller, Polymorphism and pseudopolymorphism on nifedifine, Sci. Pharm., 64, 293-301 (1996)
  26. A. David, E. Balogh, G. Csoka and I. Racz, Methodological aspects of examination of the polymorphism of vincristine sulfate, Sci. Pharm., 64, 311-318 (1996).
  27. M. R. Caira, M. Zanol, T. Peveri, A. Gazzaniga and F. Giordano, Structural characterization of two polymorphic forms of piroxicam pivalate, J. Pharm. Sci., 87, 1608-1614 (1998) https://doi.org/10.1021/js980059s