Abstract
Simulated intestinal fluids (SIFs) are described in the United States Pharmacopoeia (USP) and the International Pharmacopoeia (IntPh) as recommended dissolution media for the characterization of solid drugs. This study was carried out to compare their wettability properties. Six different model substrates were used as surrogates for solid drugs. These surrogate solid substrates were characterized by the Lifshitz-van der Waals, electron donor and electron acceptor terms, which are the three components of the total surface energy obtained by the van Oss model, which is based upon Young’s equation. Contact angles of the SIFs on the surrogate solid-substrates were determined dynamically by image analysis up to five minutes after applying a drop of the fluid on the solid surface. Observed time-dependent spreading behavior was accounted for by a linear extrapolation of the experimental data to zero contact time to obtain the apparent equilibrium contact angle at zero time. Additionally, the pH, osmolality and buffer capacity of the SIFs were experimentally determined. Although some differences in osmolality and buffer capacity were observed, no statistically significant differences in the wetting properties of the three SIFs were detected. This confirms recent findings that there are no observed differences in dissolution behavior among these simulated intestinal fluids. Harmonization of these SIFs is thus recommended.
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References
Dressman, J., Krämer, J.: Pharmaceutical Dissolution Testing. Taylor and Francis Informa, New York (2005)
Young, D., Devane, J., Butler, J.: In vitro–in vivo correlations. Plenum, New York (1997)
European Pharmacopoeia, European Directorate for the Quality of Medicines of the Council of Europe (EDQM), Strassbourg, France, 5th edn. (2005)
Stippler, E., Kopp, S., Dressman, J.B.: Comparison of US Pharmacopeia Simulated Intestinal Fluid TS (without pancreatin) and phosphate standard buffer pH 6.8, TS of the International Pharmacopoeia with respect to their use in in vitro dissolution testing. Dissol. Technol. 11, 6–10 (2004)
United States Pharmacopeia and National Formulary, United States Pharmacopeial Convention Inc., Rockville, USA, 26th edn. (2003)
The International Pharmacopoeia, WHO, Geneva, Switzerland, 3rd (1979) and 5th (2003) edns.
Amidon, G.L., Lennernas, H., Shah, V.P., Crison, J.R.: 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)
Parfitt, G.D.: Dispersion of powders in liquids, 2nd edn. Applied Science, London (1973)
Dove, J.W., Buckton, G., Doherty, C.: A comparison of two contact angle measurement methods and inverse gas chromatography to assess the surface energies of theophylline and caffeine. Int. J. Pharm. 138, 199–206 (1996)
Luner, P.E.: Wetting properties of bile salt solutions and dissolution media. J. Pharm. Sci. 89, 382–395 (2000)
Gu, Y.: In Encyclopedia of Surface and Colloid Science, 1st edn. Hubbard, A. ed., Dekker, New York, pp. 1213–1215 (2002)
van Oss, C.J., Good, R.J., Chaudhury, M.K.: Additive and nonadditive surface-tension components and the interpretation of contact angles. Langmuir 4, 884–891 (1988)
Oh, E., Luner, P.E.: Surface free energy of ethylcellulose films and the influence of plasticizers. Int. J. Pharm. 188, 203–219 (1999)
Muster, T.H., Prestidge, C.A.: Application of time-dependent sessile drop contact angles on compacts to characterize the surface energetics of sulfathiazole crystals. Int. J. Pharm. 234, 43–54 (2002)
Van Remoortere, P., Joos, P.: About the kinetics of partial wetting. J. Colloid Interface Sci. 160, 387–396 (1993)
Choi, J.Y., Lee, H.G.: Wetting of solid Al2O3 with molten CaO-Al2O3-SiO2. ISIJ Int. 43, 1348–1355 (2003)
Galet, L., Vu, T., Oulahna, D., Fages, J.: The wetting behaviour and dispersion rate of cocoa powder in water. Food Bioprod. Process. 82, 298–303 (2004)
Michel, T., Mock, U., Roisman, I.V., Ruhe, J., Tropea, C.: The hydrodynamics of drop impact onto chemically structured surfaces. J. Phys.: Condens. Matter 17, S607–S622 (2005)
Luner, P.E., Vander Kamp, D.: Wetting behaviour of bile salt-lipid dispersions and dissolution media patterned after intestinal fluids. J. Pharm. Sci. 90, 348–359 (2001)
Buckton, G.: Surface characterization—understanding sources of variability in the production and use of pharmaceuticals J. Pharm. Pharmacol. 47, 265–275 (1995)
Zhang, D., Flory, J.H., Panmai, S., Batra, U., Kaufman, M.J.: Wettability of pharmaceutical solids: its measurement and influence on wet granulation. Colloids Surfaces A Physicochem. Eng. Aspects 206, 547–554 (2002)
Turunen, M.P.K., Laurila, T., Kivilahti, J.K.: Evaluation of the surface free energy of spin-coated photodefinable epoxy. J. Polym. Sci. B Polym. Phys. 40, 2137–2149 (2002)
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De Spiegeleer, B., Baert, B., Vangheluwe, E. et al. Comparison of the Wetting Properties of Three Commonly Used Simulated Intestinal Fluids Used as Dissolution Media in the Characterization of Drugs. J Solution Chem 36, 835–843 (2007). https://doi.org/10.1007/s10953-007-9150-5
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DOI: https://doi.org/10.1007/s10953-007-9150-5