Permeability values and efflux ratios of test compounds atenolol, propranolol & loperamide in differentiated CACO-2 cultures CACO-2 Master Cell Bank (09042001) A-to-B B-to-A - Efflux - Papp (x10 6 cms 1) Papp (x10-6 cms-1) Compound Papp Papp Mean SD N Papp Papp Mean SD ratio N Loperamide 2.7 2.2 2.45 0.25 2 8.96 8.41 8.685 0.39 2 3.54
The Caco-2 cell monolayer model is a popular surrogate in predicting the in vitro human intestinal permeability of a drug due to its morphological and functional similarity with human enterocytes. A quantitative structureproperty relationship (QSPR) study was carried out to predict Caco-2 cell permeability of a large data set consisting of 1272 compounds. Caco-2 Permeability Assay - CyprotexThe Caco-2 permeability screen is considered to be more representative of human absorption in vivo than PAMPA (parallel artificial membrane permeability assay). PAMPA solely provides a measure of passive diffusion whereas the Caco-2 model provides better prediction of the human absorption for compounds which display active uptake or efflux or pass through the membrane via the paracellular route.
Caco-2 permeability assay is a part of our portfolio of in vitro ADME screening services. Creative Bioarray delivers consistent, high quality Caco-2 assay data with cost-efficiency that comes from a highly automated approach. Available Caco-2 Permeability Assay at Creative Bioarray. Passive permeability in Caco-2; Evaluation of MDR1 substrate Caco-2 Permeability Assay - IONTOXThese data are then used to determine the apparent permeability coefficient (P app; units are cm/s), which is calculated using the following equation:P app = (dQ/dt) (1/(AC 0)) where dQ/dt is the steady-state ux (mmol/second), A is the surface area of the lter (cm 2) and C 0 is the initial concentration in the donor chamber (mM). The mass balance (experimental recovery) is also calculated.
The parameters P app (apparent permeability) and efflux ratio are calculated as follows:P app = (dQ/dt) × (1/C 0) × (1/A) Efflux ratio = P app [B A] / P app [A B] where dQ/dt is the permeability rate, C 0 is the initial concentration in the donor compartment, and Determination of drug permeability and prediction of Aug 23, 2007 · Permeability coefcients across monolayers of the human colon carcinoma cell line Caco-2, cultured on permeable supports, are commonly used to predict the absorption of orally administered drugs
Prediction:logP 0 = -2.8, optimal pH region:6.0 7.5. Oxycodone showed excellent agreement between membrane permeability in Double-Sink PAMPA and transcellular (A B) Caco-2 permeability, see Figure 7. Analysis reveals that 60% of Intestinal permeability of the constituents from the roots The bidirectional intestinal permeability of the active constituents from the roots of Saposhnikovia divaricata, including four coumarins, anomalin (1), 5-methoxy-7-(3,3-dimethylallyloxy)coumarin (2), decursin (3), and decursinol angelate (4), as well as four chromones, cimifugin (5), prim-O-glucosylcimifugin (6), 3'- O-angeloylhamaudol (7), and sec-O-glucosylhamaudol (8), was studied by
MDR1-MDCK Permeability Assay for P-glycoprotein Substrate Identification. In addition to predicting passive permeability, MDCK cells can be used to study drug efflux and active transport, usually efflux by P-gp (P-glycoprotein, a well-recognized efflux transporter in Physiologically based pharmacokinetic/pharmacodynamic Mar 04, 2021 · Apparent permeability (Papp, cm/s) was calculated using the following equation:(1) Where Vr is the volume of the receiver compartment (mL), S is the surface area of the transwell insert (0.33 cm 2 ), C0 is the initial concentration in the donor compartment, and dCr/dt is the measured rate of change in concentration in the receiver compartment
prediction model. RESULTS:The correlation coefficients (r) of the experimental and predicted Caco-2 apparent permeability for the training set and the test set were 0.88 and 0.85, respectively. CONCLUSIONS:The results suggest that the SVM method is effective for predicting Caco-2 permeability. Membrane permeability of Predicting a Drugs Membrane Permeability:A Mar 27, 2017 · govern the permeability.19 For prediction of passive membrane permeability, the most critical parameter in QSPR studies is lipophilicity.20 Lip-ophilicity is a crucial factor governing passive membrane partitioning,21 and calculated lipophilicity metrics are often utilized to predict drug absorption.22 The parameter that
Caco-2 permeability profile took into account, transcellular passive (neutral and charged species), paracellular, aqueous boundary layer (ABL), and filter-limited permeability. Fig. 2. Prediction of the intrinsic Caco-2 permeability, using intrinsic Double-Sink PAMPA permeability, calculated apparent (PDF) Predicting apparent passive permeability of Caco-2 Dec 27, 2017 · Predicting apparent passive permeability of Caco-2 and MDCK cell-monolayers:A mechanistic model