Improving drug solubility for oral delivery using solid dispersions.

https://www.gastrojournal.org/article/0016-5085(89)90897-4/pdf

Characterization of the human colon carcinoma cell line (Caco-2) as a model system for intestinal epithelial permeability

According to linear pharmacokinetics, the time course of plasma concentration of a drug, Cp,is expressed by a sum of exponential functions, Cp=ei=1nai\(C_p = \sum\nolimits_{i = 1}^n {a_i e^{ - b_i t} } \).This article describes a statistical technique to estimate the number of exponential terms, n,for the time course of drug by the application of Akaike's information criterion (AIC). Plasma concentrations of ethoxybenzamide, sulfisoxazole, bishydroxycoumarin, and diazepam measured following bolus intravenous injection were used as clinical examples for this method. Selection of models is compared between the AIC method and an Ftest method at significance levels of 5% and 1%.

Application of Akaike's information criterion (AIC) in the evaluation of linear pharmacokinetic equations.

https://onlinelibrary.wiley.com/doi/pdf/10.1002/jps.2600600902

Pharmaceutical Applications of Solid Dispersion Systems

Correlation between oral drug absorption in humans and apparent drug permeability coefficients in human intestinal epithelial (Caco-2) cells

Several important statistical aspects of pharmacokinetic analyses by digital computer are discussed. These include selection of appropriate equations, weighting of data, precision of parameter estimates, comparisons of parameters, analysis of weighted residuals, and criteria useful in the selection of particular models. Data obtained after administration of isoniazid and isonicotinuric acid to man are analyzed to illustrate the usefulness of the discussed methods.

Statistical estimations in pharmacokinetics

Moments analysis has been applied to the calculation of mean (in vivo)dissolution time (MDT) and mean absorption time (MAT) from plasma level of drug versus time data. Methods for accurately estimating the MDT under varying conditions, limitations of the methods, and interpretation of the data are presented. The importance of accurate estimates of the terminal rate constant (λz) and the drug concentration at the time of withdrawing the final plasma sample (Ĉz)is emphasized in connection with extrapolation to t=∞.The appropriate use of a logarithmic trapezoidal equation for calculating the area under the moments curve (AUMC) is shown to increase the accuracy of estimating MDT.

The application of statistical moment theory to the evaluation of in vivo dissolution time and absorption time

https://onlinelibrary.wiley.com/doi/pdf/10.1002/jps.2600570602

Sidney Riegelman

Papers

Pharmaceutical Applications of Solid Dispersion Systems

Statistical estimations in pharmacokinetics

The application of statistical moment theory to the evaluation of in vivo dissolution time and absorption time

New Method for Calculating the Intrinsic Absorption Rate of Drugs

Shortcomings in Pharmacokinetic Analysis by Conceiving the Body to Exhibit Properties of a Single Compartment