| Pharmaceutics is an important part of preclinical drug development that is often overlooked until problems emerge. In the early stages, a poor understanding of a drug compound's physicochemical properties (eg stability, impurities) or a poor formulation, can lead to misinterpretation of data generated from efficacy, ADME and toxicology studies. As preclinical development progresses, analysis and formulation requirements increase in importance and in the level of detail required.
In addition to physicochemical characterisation, impurity profiling, formulation development and stability studies, the pharmaceutics laboratory also conducts in vitro assays (eg. Caco-2 cells), dissolution and biowaiver studies. It also has considerable expertise in the development of peptides as drugs, including specialised custom peptide synthesis to increase bioavailability.
Physicochemical characterisation
Dissolution analysis of powders capsules and tablets etc.
Stability investigation to ICH standards
Impurity analysis
Analytical method development and validation
Structure elucidation
Preclinical formulation and dosage form development
in vitro assays (Caco-2 etc)
Specialised peptide synthesis and modification
Physicochemical characterisation
In addition to structural information, we can characterise the physicochemical properties of compounds using the following methods:
- Solubility determination
- Melting point determination
- Microcalorimetry (DSC, DTA, STA, TG, ITC)
- Chromatography separation (HPLC, atmospheric and low pressure chromatography)
Stability testing to ICH guidelines
TetraQ Pharmaceutics offers a range of stability testing services in compliance with ICH guidelines.
- Short-term stability studies
- Long-term stability studies
- Accelerated stability studies
All stability chambers are fully validated to meet strict temperature, humidity and uniformity requirements. All chambers are monitored 24 hours a day.
The following techniques are used to support stability programs:
- Dissolution Testing
- GC with FID or MS detection
- Particle Size
- HPLC
- X-ray Powder Diffraction
- DSC
Impurity analysis
Analysis techniques such as HLPC and LC/MS are used to identify degradation products and impurities derived from the synthesis process
The above methods can be applied in various levels of detail, depending on the stage of drug development.
Structure Elucidation
Using state of the art equipment and standardised techniques, we are able to provide essential structural information about your compound. We use the following techniques:
- UV-Vis spectroscopy
- FTIR & Raman spectroscopy
- NMR analysis
- LC/MS
- GC/MS
In addition to the above methods, we are building a capability to analyse the solid state of compounds to identify polymorphs.
Preclinical formulation and dosage form development
TetraQ performs preclinical formulation service and we are able to design prototype formulations to address issues such as solubility and stability. The conduct of this service depends on the drug in question, so please contact us for more information.
In addition to developing new formulations, we are building our range of techniques that can be used to analyse formulations, both for preclinical drug candidates and for clinical trial material or marketed drugs (depending on accreditation required).
The following techniques are either available now, or will be available soon (please enquire):
- Rheological properties of suspensions and emulsions
- Powder analysis:
- Particle size and shape
- Apparent density
- Angle of repose
- Specific surface area
- Granulation
- Hygroscopic nature
- Tabletting:
- Dissolution analysis
- Disintegration, Friability & Hardness
in vitro assays
In addition to those services offered in the ADME laboratory, the pharmaceutics laboratory offers a range of in vitro tests aimed at determining basic stability, toxicity, membrane permeability and absorption profiles. We currently offer the following in vitro techniques:
- Absorption assay (Caco-2 cells): measures the ability of compounds to pass though a monolayer of Caco-2 cells that have formed tight junctions
- Absorption assay (PAMPA): measures passive transcellular permeability using lipid filled membrane
- Absorption mechanism assay (Caco-2 cells): measures passive, active and efflux transport of a compound through a Caco-2 cell monolayer.
- Caco-2 cell homogenate stability: measures stability of compounds when exposed to homogenate of Caco-2 cells which contains common gut enzymes.
- Red blood cell stability: measures stability of compounds when exposed to red blood cells.
- Red blood cell toxicity: measures cell resistance and disintegration with red blood cells
- Caco-2 cell toxicity: measures cell resistance and disintegration of compounds on Caco-2 cells
Specialised peptide synthesis and modification
We conduct specialised custom synthesis of peptides to improve membrane permeability. Please ask about this service.
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