Particle Size Distribution Equivalency as Novel Predictors for Bioequivalence

Crowder TM, Hickey AJ, Louey MD, Orr NA. Guide to pharmaceutical particulate science. London: Interpharm/CRC; 2003.

U.S. National Archives and Records Administration. Title 21: Food and drugs. Chapter1-Food and Drug Administration. Code of Federal Regulations: part 320-bioavailability and bioequivalence requirements. 2017.

Food and Drug Administration. Draft guidance on cyclosporine: emulsion form/ophthalmic route. 2013.

Azzalini A, Capitanio A. The skew-normal and related families: Cambridge University Press; 2014. URL https://www.R-project.org/

Bikhazi AB, Higuchi WI. Interfacial barriers to the transport of sterols and other organic compounds at the aqueous polysorbate 80-hexadecane Interface. Biochim Biophys Acta Biomembr. 1971;233(3):676–87.

Sweeney R, Langenberg JP, Maxwell DM. A physiologically based pharmacokinetic (PB/PK) model for multiple exposure routes of soman in multiple species. Arch Toxicol. 2006;80(11):719–31.

Pamela N, Roy L, Celin D, Diana I, Emma P, Ian B, et al. Tolerability of Velcade (Bortezomib) subcutaneous administration using a maximum volume of 3 mL per injection site. J Oncol Pharm Pract. 2015;21(4):285–92.

Nguyen HQ, Stamatis SD, Kirsch E. A novel method for assessing drug degradation product safety using physiologically-based pharmacokinetic models and stochastic risk assessment. J Pharm Sci. 2015;104(9):3101–19.

Valentin J. Basic Anatomical and Physiological data for use in radiological protection: reference values. A report of age- and gender-related differences in the anatomical and physiological characteristics of reference individuals. ICRP Publication 89. Ann ICRP. 2002;32(3–4):5–265.

Drugs.com . Diprivan Information from Drugs.com . https://www.drugs.com/diprivan.html .

Gill KL, Houston JB, Galetin A. Characterization of in vitro Glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin. Drug Metab Dispos. 2012;40(4):825–35.

Hospira. Propofol Injectable Emulsion. https://www.pattersonvet.com/msds/078889390 .

Avdeef A, Nielsen PE, Tsinman O. PAMPA-a drug absorption in vitro model 11. Matching the in vivo unstirred water layer thickness by individual-well stirring in microtitre plates. Eur J Pharm Sci. 2004;22(5):365–74.

Gill KL, Gertz M, Houston JB, Galetin A. Application of a physiologically based pharmacokinetic model to assess propofol hepatic and renal glucuronidation in isolation: utility of in vitro and in vivo data. Drug Metab Dispos. 2013;41(4):744–53.

Rodgers T, Leahy D, Rowland M. Physiologically-based pharmacokinetic modeling 1: predicting the tissue distribution of moderate-to-strong bases. J Pharm Sci. 2005;94:1259–76.

Rodgers T, Rowland M. Physiologically-based pharmacokinetic modeling 2: predicting the tissue distribution of acids, very weak bases, neutrals and zwitterions. J Pharm Sci. 2006;95(6):1238–57.

Poulin P, Schoenlein K, Theil F-P. Prediction of adipose tissue:plasma partition coefficients for structurally unrelated drugs. J Pharm Sci. 2001;90(4):436–47.

Poulin P, Theil FP. Prediction of pharmacokinetics prior to in vivo studies. 1. Mechanism-based prediction of volume of distribution. J Pharm Sci. 2002;91(1):129–56.

Peters SA. Evaluation of a generic physiologically based pharmacokinetic model for lineshape analysis. Clin Pharmacokinet. 2008;47(4):261–75.

Doenicke AW, Roizen MF, Rau J, O'Connor M, Kugler J, Klotz U, et al. Pharmacokinetics and pharmacodynamics of propofol in a new solvent. Anesth Analg. 1997;85(6):1399–403.

Food and Drug Administration. Guidance for Industry: Bioequivalence Guidance. 2006.

Inman HF, Bradley EL. The overlapping coefficient as a measure of agreement between probability distributions and point estimation of the overlap of two normal densities. Commun Stat Theory Methods. 1989;18(10):3851–74.

Gastwirth JL. Statistical measures of earnings differentials. Am Stat. 1975;29(1):32–5.

Food and Drug Administration. Guidance for Industry: Bioavailability and Bioequivalence Studies for Orally Administered Drug Products-General Considerations. 2003.

Food and Drug Administration. Guidance for Industry: immediate-release solid oral dosage forms: scale-up and post-approval changes: chemistry, manufacturing and controls, in vitro dissolution testing, and in vivo bioequivalence documentation. 1995.

Food and Drug Administration. Guidance for industry: Dissolution testing of immediate release solid oral dosage forms. 1997.

Food and Drug Administration. Guidance for Industry: SUPAC-MR: modified release solid oral dosage forms. Scale-up and post-approval changes: chemistry, manufacturing, and controls; in vitro dissolution testings and in vivo bioequivalence documentation. 1997.

Food and Drug Administration. Guidance for Industry: Extended release oral dosage forms: development, evaluation, and application of in vitro/in vivo correlations. 1997.

Moore JW, Flanner HH. Mathematical comparison of dissolution profiles. Pharm Technol. 1996:64–74.

O’Hara T, Dunne A, Butler J, Devane J. A review of methods used to compare dissolution profile data. Pharmaceutical Science & Technology Today. 1998;1(5):214–23.

Duan J, Riviere K, Marroum P. In vivo bioequivalence and in vitro similarity factor (f2) for dissolution profile comparisons of extended release formulations: how and when do they match? Pharm Res. 2011;28(5):1144–56.

Xie F, Ji S, Cheng Z. In vitro dissolution similarity factor (f2) and in vivo bioequivalence criteria, how and when do they match? Using a BCS class II drug as a simulation example. Eur J Pharm Sci. 2015;66(0):163–72.

Costa P, Sousa Lobo JM. Modeling and comparison of dissolution profiles. Eur J Pharm Sci. 2001;13(2):123–33.

Shah VP, Tsong Y, Sathe P, Liu JP. In vitro dissolution profile comparison-statistics and analysis of the similarity factor, f2. Pharm Res. 1998;15(6):889–96.

LeBlond D, Altan S, Novick S, Peterson J, Shen Y, Yang H. In vitro dissolution curve comparisons: a critique of current practice. Dissolution Technologies. 2016;23:14–23.

Food and Drug Administration. Guidance for Industry: dissolution testing and specification criteria for immediate-release solid oral dosage forms containing biopharmaceutics classification system class 1 and 3 drugs. 2015.

Food and Drug Administration. Guidance for industry: statistical approaches to establishing bioequivalence. 2001.

Artursson P. Epithelial transport of drugs in cell culture. I: a model for studying the passive diffusion of drugs over intestinal absorbtive (Caco-2) cells. J Pharm Sci. 1990;79(6):476–82.

Artursson P, Karlsson J. Correlation between oral drug absorption in humans and apparent drug permeability coefficients in human intestinal epithelial (Caco-2) cells. Biochem Biophys Res Commun. 1991;175(3):880–5.

Haeberlin B, Rubas W, Nolen IIIHW, Friend DR. In vitro evaluation of dexamethasone-β-D-glucuronide for colon-specific drug delivery. Pharm Res. 1993;10(11):1553–62.

Rubas W, Jezyk N, Grass GM. Comparison of the permeability characteristics of a human colonic epithelial (Caco-2) cell line to colon of rabbit, monkey, and dog intestine and human drug absorption. Pharm Res. 1993;10(1):113–8.

Hovgaard L, Brøndsted H, Buur A, Bundgaard H. Drug delivery studies in Caco-2 monolayers. Synthesis, hydrolysis, and transport of O-cyclopropane carboxylic acid ester prodrugs of various β-blocking agents. Pharm Res. 1995;12(3):387–92.

Augustijns P, D'Hulst A, Van Daele J, Kinget R. Transport of artemisinin and sodium artesunate in Caco-2 intestinal epithelial cells. J Pharm Sci. 1996;85(6):577–9.

Collett A, Sims E, Walker D, He Y-L, Ayrton J, Rowland M, et al. Comparison of HT29-18-C1 and Caco-2 cell lines as models for studying intestinal paracellular drug absorption. Pharm Res. 1996;13(2):216–21.

Yee S. In vitro permeability across Caco-2 cells (colonic) can predict in vivo (small intestinal) absorption in man-fact or myth. Pharm Res. 1997;14(6):763–6.

Yazdanian M, Glynn SL, Wright JL, Hawi A. Correlating partitioning and Caco-2 cell permeability of structurally diverse small molecular weight compounds. Pharm Res. 1998;15(9):1490–4.

Zhu C, Jiang L, Chen T-M, Hwang K-K. A comparative study of artificial membrane permeability assay for high throughput profiling of drug absorption potential. Eur J Med Chem. 2002;37(5):399–407.

Saha P, Kou JH. Effect of bovine serum albumin on drug permeability estimation across Caco-2 monolayers. Eur J Pharm Biopharm. 2002;54(3):319–24.

Camenisch G, Alsenz J, van de Waterbeemd H, Folkers G. Estimation of permeability by passive diffusion through Caco-2 cell monolayers using the drugs’ lipophilicity and molecular weight. Eur J Pharm Sci. 1998;6(4):313–9.

Takano R, Sugano K, Higashida A, Hayashi Y, Machida M, Aso Y, et al. Oral absorption of poorly water-soluble drugs: computer simulation of fraction absorbed in humans from a miniscale dissolution test. Pharm Res. 2006;23(6):1144–56.

Yang Y, Faustino PJ, Volpe DA, Ellison CD, Lyon RC, Yu LX. Biopharmaceutics classification of selected β-blockers: solubility and permeability class membership. Mol Pharm. 2007;4(4):608–14.

Sjögren E, Westergren J, Grant I, Hanisch G, Lindfors L, Lennernäs H, et al. In silico predictions of gastrointestinal drug absorption in pharmaceutical product development: application of the mechanistic absorption model GI-Sim. Eur J Pharm Sci. 2013;49(4):679–98.

Schipper NGM, Osterberg T, Wrange U, Westberg C, Sokolowski A, Rai R, et al. In vitro intestinal permeability of factor Xa inhibitors: influence of chemical structure on passive transport and susceptibility to efflux. Pharm Res. 2001;18(12):1735–41.

National Center for Biotechnology Information. PubChem compound database. Available from: https://pubchem.ncbi.nlm.nih.gov/ .

Gertz M, Harrison A, Houston JB, Galetin A. Prediction of human intestinal first-pass metabolism of 25 CYP3A substrates from in vitro clearance and permeability data. Drug Metab Dispos. 2010;38(7):1147–58.

Schmitt JM, Zhou GX, Walker EC. Multilayer model of photon diffusion in skin. J Opt Soc Am A. 1990;7(11):2141–53.

Shalizi CR. Logistic Regression. In: Advanced data analysis from an elementary point of view. Carnegie Mellon University; 2017. p. 251–280.