An API that is stable on its own can still fail in the tablet. Our program tests your solid form against the excipients, the process and the moisture it will meet in the product, chemically and in the solid state, before a formulation is locked.
Drug–excipient interactions usually surface during formulation stability studies, months after the excipients were chosen. By then the composition, the process and often the clinical supply depend on it. Changing an excipient at that stage means new batches, a new stability programme and, sometimes, a delay to the clinic.
Chemical degradation is only part of the risk. A salt can disproportionate back to its free form in contact with a basic excipient. A metastable polymorph can convert during wet granulation or compression. An amorphous dispersion can start to crystallize when a hygroscopic excipient draws in water. These are solid-state events, and a purity assay alone will not show them.
The program looks for both kinds of failure at the same time, early enough for the answer to change the formulation rather than delay it.
The study is built around your API, the dosage form you intend and the excipients you are considering.
Binary and multi-component mixtures of the API with candidate fillers, binders, disintegrants, lubricants and surfactants, stored under accelerated conditions.
Assay and related substances on every mixture, with identification of the degradation products that form only in the presence of a specific excipient.
Detection of polymorphic conversion, salt disproportionation, hydrate formation or loss of amorphous character in contact with each excipient.
Simulation of the steps the formulation will see, such as milling, wet granulation, drying and compression, to find which ones change the API.
Moisture uptake of the blends and the effect of excipient pH and water activity on the stability of the API.
Excipients classed as compatible, conditional or to avoid, with the evidence for each, so the formulator can choose with confidence.
The design is agreed with you before any mixture is prepared, and adjusted as results come in.
The solid form, purity and degradation pathways of the API are established first, so every change seen in a mixture can be attributed correctly.
The excipient list, ratios, storage conditions and time points are defined with you, based on the intended dosage form and process.
Mixtures are prepared and stored under accelerated temperature and humidity, with process-stressed samples where the formulation route calls for it.
Samples are analysed at each time point for assay and degradation products with stability-indicating methods.
The same samples are examined by diffraction, thermal analysis and spectroscopy to detect changes in the solid form.
Chemical and solid-state results are read together and summarised in a compatibility matrix with a recommendation for each excipient.
Compatibility is judged on two independent lines of evidence: what happens to the molecule, and what happens to the solid.
The program ends with a detailed technical-scientific report, written for the formulation team and usable in your development documentation.
Preformulation characterizes the API on its own. The compatibility program tests the API together with the excipients and the process it will meet in the product. It usually follows preformulation and precedes the first formulation batches.
The excipients you are considering for your dosage form. If the list is still open, we propose a panel based on the formulation route and on what is known about the molecule.
Because several common failures, such as salt disproportionation, polymorphic conversion or crystallization of an amorphous dispersion, change the API without degrading it. A purity assay does not detect them; diffraction and thermal analysis do.
It depends on the number of excipients, the storage conditions and the time points. We agree the duration with the study design, and share results at each time point rather than only at the end.
It depends on the size of the excipient panel and on the techniques involved. We confirm the quantity when the study is designed, and keep it as low as the methods allow.
Yes. Our laboratory handles high-potency APIs up to OEB5 and controlled substances under Ministry of Health authorization, within its AIFA GMP certification.
Tell us the API, the dosage form and the excipients you are considering. We will propose a study design, the material requirement and a timeline.