Solution formulations
Solution formulations are used frequently throughout pharmaceutical development and are especially attractive for the earlier stages of development as they offer the ability to cover a wide dosing range via simple adjustment of the administration volume. In addition, they are generally rapidly developed and do not require complex machinery for production.
Administration of the API as a solution bypasses the dissolution step and presents the API directly in predissolved form to the gastrointestinal fluids which creates a high driving force for absorption. The criticality of using solution formulations for poorly water-soluble APIs is to inhibit API precipitation on in-vivo dilution for long enough to allow for absorption to occur. This may be achieved via the addition of precipitation inhibitors to the formulation. Another challenge is to achieve a high enough payload in the formulation such that the target dose can be delivered with an acceptable volume of formulation. Our miniaturized screens allow us to identify combinations of excipients that offer synergistic effects on solubilization while consuming only mg-quantities of API.
Our approach to solution formulation design, development and manufacture
1
Solubility profiling
Detailed assessment of the API's solubility in pharmaceutical excipients such as cosolvents, surfactants, cyclodextrins and pH-modifiers. The chemical stability of the API in the excipients is also assessed at this time.
2
Formulation design
Construct of a series of formulations based on the solubility data. Formulations are subsequently assessed for their susceptibility to API precipitation on dilution in biorelevant media.
3
Formulation development
The most performant formulations are assessed for physical and chemical stability. Manufacturing processes are developed for one or more lead formulations.
4
GMP-manufacture
Manufacturing of clinical supplies in a neighbouring third-party GMP-plant.
Discuss your solution formulation project
If you would like to learn more about our approach to solution formulation development, you can reach out to one of our experts here. We are happy to make an assessment of the developability of your compound, as a solution formulation or otherwise.
