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Research Article

Selecting the particle size distribution for drugs with low water solubility – mathematical model

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Pages 940-951 | Received 01 May 2011, Accepted 18 Oct 2011, Published online: 10 Feb 2012

References

  • Kasim NA, Whitehouse M, Ramachandran C, Bermejo M, Lennernäs H, Hussain AS et al. (2004). Molecular properties of WHO essential drugs and provisional biopharmaceutical classification. Mol Pharm, 1:85–96.
  • Noyes A, Whitney W. (1897). The rate of solution of solid substrate in their own solutions. J Am Chem Soc, 19:930–934.
  • Yu LX. (1999). An integrated model for determining causes of poor oral drug absorption. Pharm Res, 16:1883–1887.
  • Willmann S, Schmitt W, Keldenich J, Lippert J, Dressman JB. (2004). A physiological model for the estimation of the fraction dose absorbed in humans. J Med Chem, 47:4022–4031.
  • Ho NFH, Park JY, Ni PF, Higuchi WI. (1983). Advancing quantitative and mechanistic approaches in interfacing gastrointestinal drug absorption studies animals and human. In Crouthamel W, Sarapu AC, eds. Animal Models for Oral Drug Delivery in Man: In Situ and In Vivo Approaches. Washington D.C.: American Pharmaceutical Association, 27–103.
  • Agoram B, Woltosz WS, Bolger MB. (2001). Predicting the impact of physiological and biochemical processes on oral drug bioavailability. Adv Drug Deliv Rev, 50 Suppl 1:S41–S67.
  • Johnson KC. (2003). Dissolution and absorption modeling: model expansion to simulate the effects of precipitation, water absorption, longitudinally changing intestinal permeability, and controlled release on drug absorption. Drug Dev Ind Pharm, 29:833–842.
  • Hintz R, Johnson K. (1989). The effect of particle size distribution on dissolution rate and oral absorption. Int J Pharm, 51:517–519.
  • Takano R, Sugano K, Higashida A, Hayashi Y, Machida M, Aso Y et al. (2006). Oral absorption of poorly water-soluble drugs: computer simulation of fraction absorbed in humans from a miniscale dissolution test. Pharm Res, 23:1144–1156.
  • Mathews B, Rhodes C. (1967). Particle size of commercial griseofulvin with reference to official standards. J Pharm Sci, 56:838–842.
  • Yu L, Crison J, Amidon G. (1995). A strategic approach for predicting for predicting oral drug absorption. Pharm Res, 12:S8–S8.
  • Yu LX, Lipka E, Crison JR, Amidon GL. (1996). Transport approaches to the biopharmaceutical design of oral drug delivery systems: prediction of intestinal absorption. Adv Drug Deliv Rev, 19:359–376.
  • Bhaskarwar A. (1989). General-population balance model of dissolution of polydisperse particles. AIChE J, 35:658–661.
  • Leblanc S, Fogler H. (1987). Population balance modeling of the dissolution of polydisperse solids - rate limiting regimes. AIChE J, 33:54–63.
  • Mangin D, Garcia E, Gerard S, Hoff C, Klein J, Veesler S. (2006). Modeling of the dissolution of a pharmaceutical compound. J Cryst Growth, 286:121–125.
  • Ozturk SS, Palsson BO, Dressman JB. (1988). Dissolution of ionizable drugs in buffered and unbuffered solutions. Pharm Res, 5:272–282.
  • Higuchi WI, Hiestand EN. (1963). Dissolution rates of finely divided drug powders. I. Effect of a distribution of particle sizes in a diffusion-controlled process. J Pharm Sci, 52:67–71.
  • Harriott P. (1962). Mass transfer to particles. I. Suspended in agitated tanks. AIChE J, 8:93–101.
  • Okazaki A, Mano T, Sugano K. (2008). Theoretical dissolution model of poly-disperse drug particles in biorelevant media. J Pharm Sci, 97:1843–1852.
  • Charman WN, Porter CJ, Mithani S, Dressman JB. (1997). Physiochemical and physiological mechanisms for the effects of food on drug absorption: the role of lipids and pH. J Pharm Sci, 86:269–282.
  • Oberle RL, Chen TS, Lloyd C, Barnett JL, Owyang C, Meyer J et al. (1990). The influence of the interdigestive migrating myoelectric complex on the gastric emptying of liquids. Gastroenterology, 99:1275–1282.
  • Davis SS, Hardy JG, Fara JW. (1986). Transit of pharmaceutical dosage forms through the small intestine. Gut, 27:886–892.
  • Priebe MG, Wachters-Hagedoorn RE, Stellaard F, Heiner AM, Elzinga H, Vonk RJ. (2004). Oro-cecal transit time: influence of a subsequent meal. Eur J Clin Invest, 34:417–421.
  • DeSesso JM, Jacobson CF. (2001). Anatomical and physiological parameters affecting gastrointestinal absorption in humans and rats. Food Chem Toxicol, 39:209–228.
  • Lennernas H, Palm K, Fagerholm U, Artursson P. (1996). Comparison between active and passive drug transoprt in human intestinal epithelial (Caco-2) cells in vitro and human jejenum in vivo. Int J Pharm 127:103–107.
  • Watts P, Illum L. (1997). Colonic drug delivery. Drug Dev Ind Pharm, 23:813–913.
  • Yu L, Crison J, Amidon G. (1996). Compartmental transit and dispersion model analysis of small intestine transit flow in humans. Int J Pharm, 140:111–118.
  • Dressman JB, Fleisher D. (1986). Mixing-tank model for predicting dissolution rate control or oral absorption. J Pharm Sci, 75:109–116.
  • Zhao YH, Abraham MH, Le J, Hersey A, Luscombe CN, Beck G et al. (2002). Rate-limited steps of human oral absorption and QSAR studies. Pharm Res, 19:1446–1457.
  • Fujiwara S, Yamashita F, Hashida M. (2002). Prediction of Caco-2 cell permeability using a combination of MO-calculation and neural network. Int J Pharm, 237:95–105.
  • Dressman JB, Reppas C. (2000). In vitro-in vivo correlations for lipophilic, poorly water-soluble drugs. Eur J Pharm Sci, 11 Suppl 2:S73–S80.
  • Watanabe E, Takahashi M, Hayashi M. (2004). A possibility to predict the absorbability of poorly water-soluble drugs in humans based on rat intestinal permeability assessed by an in vitro chamber method. Eur J Pharm Biopharm, 58:659–665.
  • Rowland M, Tozer T. (1995). Clinical pharmacokinetics. Baltimore: Lippinicott Williams & Wilkins.
  • Shaw TR, Carless JE. (1974). The effect of particle size on the absorption of digoxin. Eur J Clin Pharmacol, 7:269–273.
  • Marchuk G. (1990). Splitting and alternating direction methods. In Ciarlet P, Lions JL, eds. Handbook of Numerical Analysis. North-Holland: Elsevier science publishers B.V.
  • Leveque R. (2002). Finite volume methods for hyperbolic problems. Cambridge: Cambridge University Press.
  • Crank J. (1975). The mathematics of diffusion. Oxford: Clarendon Press.
  • MathWorks. (2007a). Matlab Technical report. Natick: The MathWorks Inc.
  • Lu AT, Frisella ME, Johnson KC. (1993). Dissolution modeling: factors affecting the dissolution rates of polydisperse powders. Pharm Res, 10:1308–1314.
  • Chiou WL, Riegelman S. (1971). Absorption characteristics of solid dispersed and micronized griseofulvin in man. J Pharm Sci, 60:1376–1380.
  • Kraml M, Dubuc J, Gaudry R. (1962). Gastrointestinal absorption of griseofulvin. II. Influence of particle size in man. Antibiot Chemother, 12:239–242.
  • Kabasakalian P, Katz M, Rosenkrantz B, Townley E. (1970). Parameters affecting absorption of griseofulvin in a human subject using urinary metabolite excretion data. J Pharm Sci, 59:595–600.
  • Yu LX, Amidon GL. (1999). A compartmental absorption and transit model for estimating oral drug absorption. Int J Pharm, 186:119–125.
  • Straughn AB, Meyer MC, Raghow G, Rotenberg K. (1980). Bioavailability of microsize and ultramicrosize griseofulvin products in man. J Pharmacokinet Biopharm, 8:347–362.
  • Yazdanian M, Glynn SL, Wright JL, Hawi A. (1998). Correlating partitioning and caco-2 cell permeability of structurally diverse small molecular weight compounds. Pharm Res, 15:1490–1494.
  • Takagi T, Ramachandran C, Bermejo M, Yamashita S, Yu LX, Amidon GL. (2006). A provisional biopharmaceutical classification of the top 200 oral drug products in the United States, Great Britain, Spain, and Japan. Mol Pharm, 3:631–643.
  • Aoyagi N, Ogata H, Kaniwa N, Ejima A. (1982). Effect of food on the bioavailability of griseofulvin from microsize and PEG ultramicrosize (GRIS-PEG) plain tablets. J Pharmacobio-dyn, 5:120–124.
  • Aoyagi N, Ogata H, Kaniwa N, Koibuchi M, Shibazaki T, Ejima A. (1982). Bioavailability of griseofulvin from tablets in humans and the correlation with its dissolution rate. J Pharm Sci, 71:1165–1169.
  • Barret W, Bianchine J. (1975). The biovailability of ultramicronized griseofulvin (Gris-PEG) tablets in man. Curr Ther Res Clin Exp, 18:501–509.
  • Hidalgo IJ, Raub TJ, Borchardt RT. (1989). Characterization of the human colon carcinoma cell line (Caco-2) as a model system for intestinal epithelial permeability. Gastroenterology, 96:736–749.
  • Gramatté T. (1994). Griseofulvin absorption from different sites in the human small intestine. Biopharm Drug Dispos, 15:747–759.

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