Background and Service Details:

Pharmacokinetic  (PK)  studies  can  significantly  vary  in  design  depending  on  their  goals  and  parameters of  the  tested  compounds.  We offer PK in widely used mouse inbred (C57BL/6, BALB/c), or outbred (CD1, NMRI) strains, and Wistar, or Sprague Dawley rats.  A typical PK study in mice involves two drug delivery routes (e.g. PO and IV), 6 time points for each route (for example: 5, 15, 30, 60, 120, 240 min for IV and 15, 30, 60, 120, 240 and 360 min for PO) and 4 animals per  each  time  point  group/route,  plus  the  common control  plasma  of Vehicle dosed group,  50  animals  in  total.  We will prepare blood plasma samples and measure compound concentrations by LC-MS/MS using AB Sciex API4000/3000 mass spectrometers and Shimadzu (Prominence, VP) HPLC systems.

We offer:

  • Measurements of various pharmacokinetic and pharmacodynamics parameters;

  • Compound absorption/liberation dynamics following different routes of administration;

  • Biodistribution (brain, liver, kidney, lung, spleen, heart, liquor, etc);

  • Metabolism/biotransformation – metabolite ID services;

  • Compound excretion dynamics (urine/feces, bile);

  • End-point or serial sampling;

  • Single compound or cassette pharmacokinetics for mix of 2-3-4-5 compounds;

  • Wide range of time points;

  • Native or perfused tissue sampling;

  • Development of  optimized  drug  delivery formulations to improve the bioavailability (Formulation Screen)

Deliverable: A detailed study report including full description of study design, analytical method, measured test article concentrations, all common PK parameters and PK graphs. Raw experimental data are available upon request.

Typical plasma concentration-time curve for single compound testing:

PK curve

Sample Submission.  Dry compound or compound in a pre-made animal dosing formulation. Amounts depend on the dosing levels. For a PK study in mice at 10 mg/kg PO and 10 mg/kg IV about 16 mg of compound is required. We do not need to know structures of the molecules for ADME testing. However, brutto formulas have to be provided for all studies involving MS detection.

 

Bienta/Enamine Animal Work Statement