testing

the top 4 reasons to chose our DMPK Services

  • 1

    Faster Troubleshooting

    Our DMPK team is geared up for quick response time.

  • 2

    Quality and Depth

    Data from our DMPK studies is validated and used by clients from the pharmaceutical, biotechnology, agrochemical, tobacco, cosmetics, health care companies and academic organisations. A number of different DMPK reporting options are available.

  • 3

    Quick Turnaround Time

    For most of the core DMPK services is within 3-5 working days. In fact, the turn around time for our DMPK studies is one of the quickest in the industry.

  • 4

    Extended Support

    Our highly trained Principal DMPK Scientists on hand to explain results and suggest the most appropriate experimental strategy. Extended support is provided by the DMPK team to the customers in their drug discovery and development process.

DMPK services across drug discovery

Assessment of Physiochemical & In Vitro ADME/DMPK Properties

• In silico properties
• Solubility
• Log D
• Microsomal stability
• CYP inhibition

Optimisation of Physiochemical & Druggable Properties

• Metabolic stability
• CYP inhibition
• Permeability
• Plasma protein binding
In vivo PK studies (rodent)
• Reactive metabolite

Optimisation of Druggable Properties, IVIVC, PK/PD Correlation

• Permeability
• Plasma protein binding
• PK Studies (rodent)
• PK Studies (non-rodent)
• Target tissue exposure
• Blood/plasma partioning
• IVIVC, renal/biliary CL
• Mass balance
• PK/PD
• Met id (soft spot)

Dose Range Finding, Safety/Tox Assessment, Interspecies Scaling

• Dose range finding (rodent and non-rodent)
• PK/PD
• Tissue distribution
• Food effect
• Metabolite profiling
• Safety profiling
• Toxicokinetics
• CYP induction
• Interspecies scaling

Physicochemical Characterisation

For drugs to be effective they must be able to reach their targets in efficacious concentrations.

A number of physicochemical parameters obtained in the following assays are used to assess the potential utility of compounds as therapeutic agents:

  • Aqueous solubility (pION, Kinetic and Thermodynamic)
  • Partition coefficient (log D) BBB and GIT
  • Ionisation constant (pKa) with spectrophotometer
  • Chemical stability

Case Study: pION Solubility

Absorption/Transporters

The preferred route of drug delivery is oral administration. Intestinal membrane permeability is a critical characteristic that determines the extent and rate of drug absorption and ultimately affects the bioavailability. The human colon adenocarcinoma cell line, Caco-2, and Madin-Darby canine kidney cell line, MDCKII, are used as an alternative in vitro permeability model. PAMPA (parallel artificial membrane permeability assay) is also used to determine the passive permeability of the compounds.

Permeability/Transporters:

  • PAMPA: GIT/BBB/skin
  • Caco-2 (Pgp efflux)/MDCK permeability/BCRP
  • Skin and buccal permeability by Franz Diffusion Method
  • Ongoing Developments
  • MDCK -Transfected ABC transporters (stable cell lines)
  • SLC transporters: OATP1B1, OATP1B3 and OCT1 (Hepatic)
  • OAT1, OAT3 & OCT2 (Renal)

Case Study: Skin Pampa
Case Study: In Vitro: Skin Absorption Studies (OECD TG: 428)

Distribution

Protein Binding
GVK BIO is a specialist provider of DMPK studies and provide a range of in vitro protein binding studies.The free drug concentration is more closely related to the activity of the drug than the total plasma concentration. Drugs with low protein binding have a large volume of distribution and they can equilibrate rapidly with tissues. High protein binding causes a small volume of distribution, slow equilibration with tissues, and are usually a predictor of elimination by metabolism. We employ Rapid Equilibrium Dialysis approach to measure plasma as well as other matrices protein binding taking Warfarin as the reference control.

Blood Partitioning
Knowledge of the partitioning behaviour of a therapeutic compound into red blood cells is important to the interpretation and understanding of a compound’s pharmacokinetic profile. A high partitioning ratio may also lead to the accumulation of the compound in red blood cells and therefore, this parameter serves as an indicator of potential hematotoxicity. We use fresh blood to conduct this study taking chloroquine as the reference control.

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We perform mass balance with non-radiolabeled compounds. We can collect 49 different tissues after perfusion from animals following PK studies.

Case Study: Tissue Distribution

Other Specialised Assays

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