Influences of Polysorbate 80 Pretreatment Process on Related Substances in Pranoprofen Eye Drops

OBJECTIVE  To investigate the influence of the excipient polysorbate 80 and its pretreatment process on related substances in pranoprofen eye drops.

METHODS  A full factorial experimental design was utilized to analyze the effects of heating time and alkaline conditions during polysorbate 80 pretreatment on related substances. The interaction effects with other excipients during co-pretreatment were investigated. Additionally, a stability prediction model was established based on the Arrhenius equation.

RESULTS  Polysorbate 80 accelerates the formation of oxidative impurities in pranoprofen eye drops. The minimal impurity level was achieved when polysorbate 80 was co-treated with borax and disodium edetate for 2 h. The stability prediction model indicated that the optimized formulation could maintain stability for 36 months at 25 ℃.

CONCLUSION  When formulating preparations containing polysorbate 80, pretreatment processes should be specifically designed according to API characteristics. For oxidation-prone actives, appropriate pretreatment of polysorbate 80 can effectively reduce its impact on related substances.