Basic Formulation Screening for In Vivo Studies


The selection of the most advantageous compound formulations should meet a variety of requirements, related to intrinsic physicochemical properties of the compound, routes of delivery, stability, adverse effects, interference with bioanalytical methods, etc., which can have a substantial effect on the outcome of such studies. The service is aiming at selecting low-toxic excipients for the formulation of poorly soluble NCEs for further in vivo studies.

Service Details: We perform test solubilization of the test articles in 10-20 different formulation vehicles containing a variety of excipients commonly used in early preclinical formulations. The exact number of vehicles tested depends on the properties of the compound and its behavior in the consecutive solubilization tests. Typically, 2 selected concentration levels are tested through a dilution step. All formulations are checked for complete solubilization of the test article as well as the phase stability of each formulation over a 24-hour period and accomplished by visual observation using a white-light transilluminator. Follow-up studies, such as the longer-term chemical stability of the test article in the selected formulation, can be done for an additional fee.

Deliverable: Report containing compositions of the tested formulation vehicles, preparation of the formulations, solubilization, and stability is provided.

Sample Submission: A minimal accurately weighed aliquot of Pure compound (~1 mg) is required for each formulation recipe to be tested. However, some knowledge of the chemical nature of the tested compounds may facilitate the choice of the most suitable formulation vehicles.