Evaluation of radiostability of some steroid derivatives

Abstract

The effect of ionising radiation (15-100 kGy) on the physico-chemical properties of 6 steroid derivatives in solid state (Hydrocortisone, Hydrocortisone acetate, Prednisolone, Prednisolone acetate, Dexamethasone and Fludrocortisone acetate) was studied by differential scanning calorimetry (DSC), differential thermal analysis (DTA), scanning electron microscopy (SEM), UV spectrophotometry, high-performance liquid chromatography (HPLC), X-ray powder diffraction and polarimetry. DSC and DTA results revealed that the irradiated compounds undergo phase transitions at lower temperatures, show lower melting points and lower enthalpy of the melting process their non-irradiated analogues. The results of HPLC measurements proved a loss in the active substance content after irradiation ranging from 0.5 to 2.88%. No significant effect of irradiation was detected by the UV spectrophotometry or polarimetry in the course of the UV spectrum, absorbancy or optical rotation, as well as in the SEM photographs and X-ray patterns. For some compounds studied a correlation was found between the irradiation dose and the shifts in DSC curves and the loss of content determined by the HPLC method. Similar, but not so much pronounced relations were established in or earlier studies of the derivatives of nitroimidazole and 1,4-dihydropyridine. In general the results have shown relatively high radiochemical stability of the compounds studied and have proved that the DSC method is a sensitive detector of irradiation-caused changes in drugs in solid phase.