Solid State Screening

Solid State Services

Solid State Services at Pharmaterials

Supporting the development of new and existing active drug substances and drug product formulations

As a specialist contract research organisation, Pharmaterials provides its clients with a comprehensive package of advanced solid-state screening (polymorph, salts, co-crystals and amorphous forms), characterisation and interpretation services.

The Pharmaterials Advantage

We offer a range of services fitted to your needs, with the communication and advice that you need to move your project forward.

With £1m of investment, including our industry leading transmission X-ray powder diffraction with 96 well plate and 96 well plate reading Raman microscope we have state-of-the-art instrumentation. Multiple DSC, TGA and GVS instruments give vast capacity, a wealth of supporting services and robotics allow us to provide an excellent and rapid service at great value. Our staff are outstanding and dedicated to provide the help you need to inform your choices.

Polymorph Screening

To systematically investigate the crystallisation behaviour of drug substances, Pharmaterials offers a range of conventional and high-throughput screening platforms designed around the properties of the molecule under study as well as the budget and timeframes available to our clients. Since most of the candidate drug substances for screening are in the early stages of drug development (preclinical to phase I clinical trials), our crystallisation screening and analytical technology is scaled down to ensure minimise sample use.

  • High Throughput Screening Using robotic systems with 96 well plates on our analytical equipment we can do high throughput screen (e.g 300 solvent systems) in a week.
  • Medium Throughput Screening With a minimal amount of API, we can screen a broad and diverse parameter space in a short space of time. Intelligent experimental planning and procedures yield an impressive throughput of conditions and results reported in a week or two (depending on the size of screen required).
  • Low Throughput Screening and Scale Up The final stage of any screen will be to scale up and define the crystallization conditions and carry out a full characterization of the polymorphs including DSC, TGA, X-ray (powder and single crystal if required), GVS, intrinsic solubility and a range of other tests as agreed with the client.
Pharmaceutical Co-crystals

The application of co-crystal technologies has only recently been recognised as a way to enhance solubility, stability and the IP position with respect to the development of active pharmaceutical ingredients (APIs).

Unlike salt formation, co-crystallisation does not rely on ionisation of the API and the counterion to make a solid. Instead, both components utilise prominent intermolecular interactions, such as hydrogen bonding, to combine and yield a uniform crystalline material. Combining an API with a pharmaceutically acceptable agent in this guest/host manner has become an increasingly attractive route for developing pharmaceutical products.

At Pharmaterials, we are at the forefront of co-crystal screening. Our unique co-crystallisation platform follows on from extensive internal research and incorporates a combination of high-through-put grinding, slurrying, evaporation and sonication techniques. In addition to screening, we provide extensive solid form analysis aimed at selecting the most developable pharmaceutical co-crystal.

Salt Screening / Salt Selection

In order to produce a desirable drug dosage form of an active pharmaceutical ingredient (API), developmental chemists often start by considering the possible formation of various salt forms of the API.

By formulating salts with different specific counter ion functionalities, it is possible to alter the physical properties of the drug active, such as improve its aqueous solubility, degree of crystallinity, hygroscopic nature and solid-state stability. Such factors also contribute directly to the drugs effectiveness and safety, as well as improving commercial suitability such as shelf life and manufacturing process simplification etc.

As well as identifying suitable salt forms to alter the physicochemical properties of the API, our technologies may also be used for increased patent protection. For more information please contact us.

Developability / Formulation Screen

When selecting the best candidate to take into full development, it is important to consider the key issues of:

  • Chemical stability
  • Solubility / dissolution rate
  • Processability (melting point and others)

To ensure that the form is optimised we will assess the best form (salt or co-crystal) and make suggestions about the crystallinity, complexity, stability, dissolution and processing challenges for your active.

When taken in connection with our formulation screen you will rapidly be in a position to begin your development process with confidence.

The formulation screen will focus on assessing the solubility, limpidity and amorphous dispersion of the compound. Pharmaterials can provide state of the art instruments and a wealth of experience and expertise to aid the first stage of pre-clinical and clinical formulation development.

At Pharmaterials we do not believe in one method being best for every sample. We use our decades of experience in multiple methods in order to find and use the best science and solution for you.