Separation, Identification, and Characterization of Degradation Products of Erlotinib Hydrochloride Under ICH-Recommended Stress Conditions by LC, LC-MS/TOF

Stability and Formulation of Erlotinib in Skin Creams

“…However, when following the stability of 0.2% ERL ( w / w ) formulated in Nourivan Antiox ® , the physico-chemical environment of ERL again seemed to require improvement in so far that only 57% of the ERL remained in the cream after three weeks. Based on the results of the pH of the formulation (pH ~ 3.5), and on the propensity of ERL to degrade upon acidic stress [ 12 ], the loss of ERL in this formulation may be due to the low/acidic pH. Thus, the optimization of the stability consisted of increasing the pH of the formulation to 7.0, a pH close to the skin and better tolerated by the tissues.…”

“…Analysis was performed by a high-performance liquid chromatograph (HPLC) (U3000 Ultimate, Thermo Fisher Scientific, Courtaboeuf, France) coupled to diode array detection (DAD). The conditions proposed by Mahajan et al and Pujeri et al were taken as a starting point for optimization [ 12 , 19 ]. A Zorbax ® C18 column (dimensions, 75 by 4.6 mm; particle size, 3.5 µm) was used for separation.…”

“…However, since the change from a solid form to a solubilized form induces a significant change in the chemical environment, the drug is often much more prone to chemical instability [ 11 ]. As ERL is known to degrade upon hydrolytic and oxidative stress, with degradation products having been detected in the presence of hydrochloric acid (HCl), sodium hydroxide (NaOH), and hydrogen peroxide (H 2 O 2 ) [ 12 , 13 ], the impact of formulation change needs to be assessed.…”