Bioavailability Studies Based on DCL™

Background & Overview

In recent years, the increased availability of chemical intermediates and automated instrumentation has led to an expanded use of stable isotopes in bioavailability and bioequivalence studies. Initially, stable isotopes were limited to labeling mass internal standard compounds for gas chromatography/mass spectrometry. Recently, their in vivo application has been shown to be a powerful pharmacological tool. Not only do stable isotopes (especially deuterium) lack toxicity, they offer advantages in terms of safety, sensitivity, specificity, and reducing the amount of sample tested and analytical assays required for certain types of pharmacological studies. BOC Sciences is able to study bioavailability using our DCL™ technology, which offers significant cost and time savings.

Fig.1 Schematic representation of the study design of a comparative bioavailability study with (a) or without stable isotope technology (b)^[1]

Our Services

Bioavailability studies

To make research easier and better for researchers, BOC Sciences offers a wide range of deuterated compounds in a competitive manner and can combine advanced LC/APCI-MS (Liquid Chromatography/Atmospheric Pressure Chemical Ionization Mass Spectrometry) to complete quantitative analysis of absorption and relative bioavailability. Our deuterated reagents are safe, reliable and effective.

Determining the release profile of a drug delivery system

BOC Sciences can evaluate modified-release oral drug delivery systems using deuterium isotope technology. The labelled substance can be the drug itself or a tracer that marks the site of release. Our technology has many distinct advantages, such as the fact that test subjects are not exposed to radioactive radiation.

Enhanced bioavailability

We have developed methods to increase the bioavailability of compounds by selectively replacing hydrogen atoms with deuterium at key metabolic sites of ligands. Deuteration was shown to have a positive effect on metabolic stability while retaining the pharmacological profile of the active compound. We provide a more effective way to increase the number of new drugs, greatly shorten the development cycle, and reduce development costs.

Fig.2 General strategy of this work to improve the bioavailability of the ligands.^[2]

Service Features

• Accurate bioavailability outcome prediction
• Average two weeks from receipt of compound to final report
• Complete data package to fully support IND and NDA filings
• Competitive quotations, lower development costs

Why choose BOC Sciences?

Our experienced researchers have high scientific level and solid technical ability. We provide protocol development, data interpretation, and timely assistance for your bioavailability studies. We understand the uniqueness of each project. At the same time, our professional technical laboratory is equipped with advanced research equipment to provide comprehensive support to ensure that the data meets the high standards in the field of scientific research.

If you are interested in our services, please contact us immediately, then fill in the complete inquiry form, and we will reply to you as soon as possible.

References

1. Schellekens R C A, et al. Applications of stable isotopes in clinical pharmacology. British journal of clinical pharmacology. 2011, 72(6): 879-897.
2. Knutson D E, et al. Design and synthesis of novel deuterated ligands functionally selective for the γ-aminobutyric acid type A receptor (GABAAR) α6 subtype with improved metabolic stability and enhanced bioavailability. Journal of medicinal chemistry. 2018, 61(6): 2422-2446.