Assay for Predicting Intestinal Permeability & Volume of Distribution

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Predicting the pharmacokinetics of new chemical entities in humans is a powerful ability for drug discovery and development.

Off-the-shelf Intestinal Permeability and Volume Distribution Kit

Scientists involved in the discovery of new drugs can select only those compounds with the best potential to be successful therapeutic agents for further development faster and easier than ever before.

Sovicell has developed an ideal off-the-shelf solution. the TRANSIL Intestinal Absorption kit is a 20 minute, high-throughput assay kit which measures the affinity of drugs to phosphatidylcholine membranes.

Intestinal permeability and tissue binding prediction kit

It is not only a screening tool to predict intestinal permeability coefficients, but also to predict compounds’ tissue binding. As drug-membrane interactions are key to both the process of membrane permeability and to binding to and permeating into the cell membranes of tissues the assay kit is an ideal tool to predict intestinal permeability rates as well as the volume of distribution already early in drug discovery.

Identifying drug candidates with a higher chance for success

Absorption of an orally administered drug from the GI tract is a complex process that is influenced by various factors. The permeability and/or solubility can limit the fraction dose absorbed of a drug. During the lead optimization process, identifying the causes of poor bioavailability is very important, because it can help to guide the synthesis program toward candidates with a more suitable pharmacokinetic profile and, thus, a higher chance for successful development.

Predicting the volume of distribution

The volume of distribution (VD) represents a complex combination of multiple chemical and biochemical phenomena. It is a measure of the relative partitioning of a drug between plasma (the central compartment) and the tissues. Thus, the VD term considers all of the tissues as a single homogeneous compartment. VD has a strong influence on a drug’s half-life and thus affects the dosing regimen. Drugs with short half-lives are likely to be administered more frequently than those with long half-lives. Early prediction of the volume of distribution is, therefore, an instrumental parameter for compound selection.

Five-step assay kit for predicting intestinal permeability & volume of distribution

The kit consists of ready-to-use 96 well microtiter plates. One plate can be used for predicting intestinal permeability and volume of distribution of up to 12 compounds. The assay requires only 5 steps:

The TRANSIL Intestinal
Absorption bead with a single lipid
bilayer reconstituted from egg yolk
phosphatidylcholine
  1. addition of drug candidate
  2. mixing and incubation for 12 minutes
  3. removal of beads by centrifugation
  4. sampling of supernatant
  5. quantification of the drug candidate

Features & Benefits of the Plasma Protein Binding Assay Kit

  • Fast, requires only 20 minutes total assay time
  • Measures the affinity to phosphatidylcholine membranes and predicts intestinal permeability and the volume of distribution
  • Ready-to-use format in 96-well plate format generating highly reproducible results
  • Rapid compound quantification due to immobilized brain membranes
  • Kit includes a spreadsheet for calculation of final results and traffic light system for data quality rating

For more information please contact Sovicell today.

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