Influence of simulated gastrointestinal fluids on polymorphic behavior of anhydrous carbamazepine form III and biopharmaceutical relevance

PDA Journal of Pharmaceutical Science and Technology

Volumn 64, Issue 1, 2010, Pages 28-36

  Bhise, S B ^a   Rajkumar, M ^a  

^a Govt College of Pharmacy   (India)

Author keywords

Carbamazepine dihydrate; Dissolution; Polymorphism; Simulated gastric fluids; Solubility

Indexed keywords

CARBAMAZEPINE; PEPSIN A; POLYMER; SURFACTANT; TYLOXAPOL; POWDER;

ARTICLE; CORRELATION COEFFICIENT; CRYSTALLIZATION; DIFFERENTIAL SCANNING CALORIMETRY; DISSOLUTION; DRUG BIOAVAILABILITY; DRUG RELEASE; DRUG SOLUBILITY; IN VITRO STUDY; IN VIVO STUDY; INTESTINE FLUID; OUTCOME ASSESSMENT; PH; POLYMORPHIC LOCUS; SIMULATION; SOLUBILITY; STOMACH JUICE; THERMOGRAPHY; X RAY DIFFRACTION; MEDICINAL CHEMISTRY; POWDER;

CALORIMETRY, DIFFERENTIAL SCANNING; CARBAMAZEPINE; CHEMISTRY, PHARMACEUTICAL; CRYSTALLIZATION; POWDERS; SOLUBILITY; SURFACE-ACTIVE AGENTS;

EID: 78149299421     PISSN: 10797440     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (27)

1. Amidon, G.; Lennernas, H.; Shah, V. P. A theortical basis for a biopharmaceutic drug classification: the correlation of in vitro drug product dissolution and in vivo bioavailability. Pharm. Res. 1995, 12 (3), 413-420.
2. Bertilsson, L. Clinical pharmacokinetics of carbamazepine. Clin. Pharmacokinet. 1978, 3 (2), 128-143.
3. Carino, S. R.; Sperry, D. C.; Hawley, M. Relative bioavailability estimation of carbamazepine crystal forms using an artificial stomach-duodenum model. J. Pharm. Sci. 2006, 95 (1), 116-125.
4. Lang, M.; Kampf, J. W.; Matzger, A. J. Form IV of carbamazepine. J. Pharm. Sci. 2002, 91 (4), 1186-1190.
5. Qu, H.; Louhi-Kultanen, M.; Kallas, J. Solubility and stability of anhydrate/hydrate in solvent mixtures. Int. J. Pharm. 2006, 321 (1-2), 101-107.
6. Vishweshwar, P.; McMahon, J. A.; Bis, J. A.; Zaworotko, M. J. Pharmaceutical co-crystals. J. Pharm. Sci. 2006, 95 (3), 499-516.
7. rd ed.; Academic Press: San Diego, CA, 2005; pp 87-106.
8. Young, W. W. L.; Suryanarayanan, R. Kinetics of transition of anhydrous carbamazepine to carbamazepine dihydrate in aqueous suspensions. J. Pharm. Sci. 1991, 80 (5), 496-500.
9. Meyer, M. C.; Straughn, A. B.; Jarivi, E. J.; Woods, G. C.; Pelsor, F. R.; Shah, V. P. The bioinequivalence of carbamazepine tablets with a history of clinical failures. Pharm. Res. 1992, 9 (12), 1612-1616.
10. Salameh, A. K.; Taylor, L. S. Physical stability of crystal hydrates and their anhydrates in the presence of excipients. J. Pharm., Sci. 2006, 95 (2), 446-461.
11. Kaneniwa, N.; Ichikawa, J. I.; Yamaguchi, T.; Hayashi, K.; Watari, N.; Sumi, M.; Dissolution behavior of carbamazepine polymorphs. Yakugaku Zasshi (Journal of the Pharmaceutical Society of Japan) 1987, 107 (10), 808-813.
12. Yumiko, K.; Shusei, I.; Shigeru, I. Physicochemical properties and bioavailability of carbamazepine polymorphs and dihydrate. Int. J. Pharm. 2000, 193 (2), 137-146.
13. McMahon, L. E.; Timmins, P.; Williams, A. C.; York, P. Characterization of dihydrates prepared from carbamazepine polymorphs. J. Pharm. Sci. 1996, 85 (10), 1064-1069.
14. Bhise, S. B.; Rajkumar, M. Effect of HPMC on solubility and dissolution of carbamazepine form III in simulated gastrointestinal fluids. A. J. Pharm. 2007, 2 (1), 235-240.
15. Rodriguez-Hornedo, N.; Murphy, D. Surfactant-facilitated crystallization of dihydrate carbamazepine during dissolution of anhydrous polymorph. J. Pharm. Sci. 2004, 93 (2), 449-460.
16. Rodriguez-Hornedo, N.; Murphy, D. Significance of controlling crystallization mechanisms and kinetics in pharmaceutical systems. J. Pharm. Sci. 1999, 88 (7), 651-660.
17. Crison, J. R.; Weiner, N. D.; Amidon, G. L. Dissolution media for in vitro testing of waterinsoluble drugs: Effect of surfactant purity and electrolyte on in vitro dissolution of carbamazepine in aqueous solutions of sodium lauryl sulfate. J. Pharm. Sci. 1997, 86 (3), 384-388.
18. Katzhendler, I.; Azoury, R.; Friedman, M. Crystalline properties of carbamazepine in sustained release hydrophilic matrix tablets based on hydroxypropyl methyl cellulose. J. Controlled Release 1998, 54 (1), 69-85.
19. Crison, J. R.; Shah, V. P.; Skelly, J. P.; Amidon, G. L. Drug dissolution into micellar solutions: Development of a convective diffusion model and comparison to the film equilibrium model with application to surfactant-facilitated dissolution of carbamazepine. J. Pharm. Sci. 1996, 85 (9), 1005-1011.
20. Gu, C. H.; Grant, D. J. W. Estimating the relative stability of polymorphs and hydrates from heats of solution and solubility data. J. Pharm. Sci. 2001, 90 (9), 1277-1287.
21. Rustichelli, C.; Gamberini, G.; Ferioli, V.; Gamberini, M. C.; Ficarra, R.; Tommasini, S. Solidstate study of polymorphic drugs: carbamazepine. J. Pharm. Biol. Anal. 2000, 23 (1), 41-54.
22. st ed.; Taylor and Francis: Boca Raton, FL, 2005; p 206.
23. Zingone, G.; Rubessa, F. Release carbamazepine from polyvinyl pyrrolidine/vinyl acetate (PVA/ VA) copolymer. STP Pharma. Sci. 1994, 4 (2), 122-127.
24. Luhtala, S. Effect of sodium lauryl sulphate and polysorbate 80 on crystal growth and aqueous solubility of carbamazepine. Acta Pharm Nord. 1992, 4 (2), 85-90.
25. Luhtala, S.; Kinos, E.; Yliruusi, J.; Tanninen, V. P. X-ray powder diffraction study of carbamazepine crystals grown in surfactant solutions. Acta Pharm Nord. 1992, 4 (4), 283-290.
26. Ono, M.; Tozuka, Y.; Oguchi T., Yamamura S.; Yamamoto, K. Effects of dehydration temperature on water vapor adsorption and dissolution behavior of carbamazepine. Int. J. Pharm. 2002, 239 (1-2), 1-12.
27. Murphy, D.; Rodriguez-Cintrin, F.; Langevin, B.; Kelly, R. C.; Rodriguez-Hornedo, N. Solution-mediated phase transformation of anhydrous to dihydrate carbamazepine and the effect of lattice disorder. Int. J. Pharm. 2002, 246 (1-2), 121-134.