Science and technology

Science and technology

Twelve Major Advantage Platforms

  • Product Description
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    • Commodity name: ADME platform

    ADME is an acronym for a drug’s “Absorption, Distribution, Metabolism, and Excretion,” representing the processes by which the body handles a drug after it enters the organism. These four properties determine a drug’s in vivo concentration, tissue distribution, and metabolic pathways, and they provide critical insights for predicting its bioavailability and biological activity—namely, whether the drug can reach its target site and elicit the desired therapeutic effect. Consequently, understanding a compound’s ADME characteristics is of paramount importance throughout the drug discovery and development process.

    Drug development is a high-risk, high-investment process that also offers substantial returns. Throughout this process, the earlier drug ADME properties are assessed and prioritized, the more effectively compounds with unfavorable ADME profiles can be eliminated, thereby minimizing unnecessary expenditures and resource waste in later stages.

    ADME classification

     

     

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    • CYP450 Enzyme Metabolic Phenotyping (Chemical Inhibition)
    • Caco-2 permeation and transport assay (unidirectional or bidirectional)
    • Permeability Assay in Membrane (PAMPA)
    • Plasma-to-Whole-Blood Distribution Ratio
    • Hepatic microsomal enzyme inhibition
    • MDCK/MDR1–MDCK Permeability Assay
    • Oil-water partition coefficient LogD
    • Solubility (kinetic solubility)
    • Matrix stability (whole blood, plasma, culture media, alteplase, etc.)
    • Stability of liver/kidney homogenates
    • Hepatic microsomal stability
    • Plasma protein binding (equilibrium dialysis method) Hemolysis

     

  • Case Study on In Vitro Plasma Stability in Mice

    Key method:

    1. Quality control: The positive control is Tat-NR2B9C (NA-1), and three parallel samples are included.
    2. Sample incubation concentration: 1 μM
    3. Reaction times: 0, 15, 30, 60, 90, and 120 minutes.
    4. Result Evaluation: The peak areas of peptides at different time points were determined by LC-MS/MS, and the results are expressed as the percentage of the parent drug remaining.
    5. Using the software GraphPad Prism, non-linear regression with a one-phase decay model was employed to determine the compound’s plasma half-life (T1/2, min), rate constant (K), and coefficient of determination (R²).

    Compound Number

    Compound

    Concentration

    Time (min)

    Prism software fitting

    0 

    15 

    30 

    60 

    90 

    120 

    k

    T1/2(min)

    R2

    1

    Tat-NR2B9c

    1 μM

    100

    92.6 

    75.7 

    63.6 

    54.1 

    44.7 

    0.007103

    97.59

    0.9666

    2

    Teriparatide

    1 μM

    100

    64.6 

    44.2 

    20.7 

    11.1 

    7.3 

    0.02658

    26.08

    0.9957

     

  • Case Analysis of In Vitro Human Plasma Protein Binding

    Key method:

    1. Key method: Dialysis equilibrium method (Teflon membrane)
    2. Administration route: Plasma
    3. Receiver: PBS
    4. The final drug concentration was 10 μM, with the stock solution at 1 mM in DMSO, diluted 100-fold to achieve the plasma concentration.
    5. The incubation time is 6 hours.
    6. Equilibration dialysis membrane: 50 kDa.
    7. Unbound fraction (%) = Cd,6h/Cp,6h × 100
    8. Cd,6h and Cp,6h represent the peak area ratios in the dialysate and plasma samples from 6 h incubation, respectively

     

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