What do we mean by formulation optimisation?
What do we mean by optimisation in the context of pharmaceutical development, and how can we do it better?
Historically, our industry has thought of optimisation in the context of batch production and product longevity – both incredibly important factors to ensure we can keep up with patient demand. However, it can be argued that the modern Pharma industry needs to broaden this term and consider new ways to optimise formulation composition and drug delivery for the promising compounds entering development today.
It is a widely reported fact that new chemical entities transitioning into clinical development increasingly suffer from sub-optimal properties. The true impact of this is established when the first clinical studies are conducted on a new compound. These studies often reveal characteristics such as short half-life, high variability, or a lack of dose proportionality. Therefore, development teams must reformulate to establish a product that meets the drug delivery needs of the molecule in order to demonstrate efficacy and Proof-of-Concept in a marketable format.
Typically, this stage of formulation optimisation starts in the laboratory, where the development team work to identify formulation prototypes to address the drug delivery needs of the molecule, which are screened in dissolution and preclinical studies. Successful formulations are then be scaled up at a Contract Development and Manufacturing Organisation (CDMO) to prepare clinical supplies. Finally, a clinical study can be conducted to determine whether the new product performs in humans.
This process takes a long time, carries considerable cost, and places significant emphasis upon the predictive power of laboratory and preclinical assessments. In itself, it is a non-optimal working model necessitated by the multiple disciplines required to develop, make and test new formulations in our human subjects.
By integrating formulation development, GMP manufacturing and clinical testing functions, we can dramatically improve this process. We can also provide opportunity to optimise the drug delivery element of the formulation optimisation process using a real-time, adaptive manufacturing approach termed Translational Pharmaceutics®.
Under Translational Pharmaceutics, the development team is able to make and dose product in a few days rather than weeks or months. Therefore, optimisation of formulations (RapidFACT®) can become a reality as the development team can access clinical data more quickly, and perform rapid manufacture and test cycles for a variety of compositions.
This capability can be further enhanced through the application of formulation design space where key parameters such as formulation composition can be modified freely to optimise a drug products performance in human subjects. Products can be selected from any point with in a continuous formulation design space where a range of product performance attributes is obtained by varying the quantitative composition of one or more formulation components.
Examples of how this can be utilised include freedom to modify the drug dose or loading to effect complete freedom to select dose within a single unit, or adjust functional excipient content or process parameters.
For further information take a look at our free RapidFACT resources or view one of our webinars
