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dispersion were characterized for thermal behavior (DSC), crystallinity (PXRD), and compatibility (FT-IR). Solubility and dissolution studies were carried out in different simulated gastrointestinal fluids and de-ionized water. Solubility studies in simulated gastric fluid (SGF) revealed that acidic pH favors formation of CBZ dihydrate.Triton X 100 in blank fast-state simulated gastric fluid (FaSSGF) prevents the formation of CBZ dihydrate in acidic pH. A maximum solubility of 268.77 Î¼g/mL was achieved with fed-state simulated intestinal fluid (FeSSIF). Correlation between solubility and pH could not be established. Both solubility and dissolution studies revealed that HPMC had a profound effect of enhancement of solubility and dissolution of CBZ form III in both physical mixtures and solid dispersions. HPMC prevents the formation of CBZ dihydrate and thereby
improves the solubility and dissolution. This was further correlated with results obtained from DSC and XRD. There was no drastic difference in solubility and dissolution of CBZ form III with different media. It was observed that there was no existing relationship between solubility and dissolution of CBZ form III in different media.
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Amidon G, Lennernas H, Shah VP. A theortical basis for a biopharmaceutic drug classification: The correlation of in vitro drug product dissolution and in vivo bioavailability. Pharm Res 1995;12:413-20.
Bertilsson L. Clinical pharmacokinetics of carbamazepine. Clin
Marazban S, Judith B, Xiaoxia C. Enhanced drug dissolution using
evaporative precipitation into aqueous solution. Int J Pharm
Yumiko K, Shusei I, Shigeru I. Physicochemical properties and
bioavailability of carbamazepine polymorphs and dehydrate. Int J Pharm
Haiyan MQ, Kallas LJ. Solubility and stability of anhydrate/hydrate in
solvent mixtures. Int J Pharm 2006;321:101-7.
Sethia S, Squillante E. Solid dispersion of carbamazepine in PVP K30
by conventional solvent evaporation and supercritical methods. Int
J Pharm 2004;272:1-10.
Katzhendler I, Azoury R, Friedman M. Crystalline properties of
carbamazepine in sustained release hydrophilic matrix tablets based
on hydroxypropyl methyl cellulose. J Control Release 1998;54:69-
Mitchell SA, Reynolds TD, Dasbach TP. A compaction process to enhance
dissolution of poorly water soluble drugs using hydroxypropyl methyl
cellulose. Int J Pharm 2003;250:3-11.
Fang T, Niklas S, Jaakko A. Influence of polymorphic form, morphology,
and excipients interactions on the dissolution of carbamazepine
compacts. J Pharma Sci 2006;10:1002- 13.
Thorsteinn L, Hafrun F. The effect of water-soluble polymers on the
aqueous solubility and complexing abilities of beta cyclodextrin. Int
J Pharma 1998;163:115-21.
Behme RJ, Brooke D. Heat of fusion measurement of a low melting
polymorph of carbamazepine that undergoes multiple-phase
changes during differential scanning calorimetry analysis. J Pharm Sci
Dressman J, Johannes K. Pharmaceutical dissolution testing, Taylor and
Francis, Boca Raton; 1, 2005. p. 206.
Agarwal S, Ashokraj Y, Bharatam PV. Solid-state characterization of
rifampicin samples and its biopharmaceutic relevance. Eur J Pharm Sci
Jez-Willian BB, Ronei JP. Figures of merit for the determination of the
polymorphic purity of carbamazepine by infrared spectroscopy and
multivariate calibration. J Pharm Sci 2004;93:2124-35.
Kalantzi L, Furat T, Abrahamsson B, Characterization of the human upper gastrointestinal contents under conditions simulation bioavailability
studies in the fasting and fed states. Salt Lake City, UT: AAPS Annual
James EP, Michael BJ, Angus HF. The influence of thermal and mechanical preparative techniques on the amorphous state of four poorly soluble compounds. J Pharm Sci 2005;94:1998-2013.
Otsuka M, Ohfusa T, Matsuda Y. Effect of binders on polymorphic
transformation kinetics of carbamazepine in aqueous solution. Colloids
Surfaces B Biointerf 2000;17:145-52.