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THERMAL COMPATIBILITY ASSESSMENT OF SELECTED EXCIPIENTS USED IN THE ORAL ANTI-CANCER FORMULATION CONTAINING BUSULFAN

PAWEŁ RAMOS *

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Oral anti-cancer drugs such as busulfan served in tablet forms except active pharmaceutical ingredient contain excipients in the formulation. Excipients must be selected so as not to cause an interaction with the API. This is especially important in the design of anti-cancer drugs. Each interaction between the excipient and the API may be translated into the deterioration of the therapeutic effects by changing the properties of the API in the final formulation. The thermogravimetry analysis can be used as a quick and cheap method of testing the compatibility of API with an excipient in preformulation studies. In this assessed examination, the compatibility of busulfan with selected excipients used in the manufacturing of tablet form was studied. TG/DTG/D2TG analysis was done for busulfan, tested excipients, and binary mixture API with an excipient. The study has shown that busulfan is incompatible with anhydrous glucose, sucrose, lactose monohydrate, microcrystalline cellulose, and starch, but the tested API is compatible with chitosan and stearate magnesium. Additionally, thermogravimetry analysis has shown that stearate magnesium causes increased thermal stability of the busulfan.