Stability study of oral pediatric idebenone suspensions

Abstract

Adapted forms for administration to infants are limited. The proposed study was performed to propose oral liquid formulations of idebenone in Ora-Plus and either Ora-Sweet or Ora-Sweet SF, Ora-Blend, Ora-Blend SF and Inorpha. Each formulation was stored in 30 ml amber glass bottle at 5 or 25 °C for 90 days. Idebenone contents in these suspensions, determined by a stability-indicating high-performance liquid chromatography method, remained stable at least 90 days in Inorpha when stored at the two temperatures. In Ora-Blend, the stability was estimated at 14 days and in other suspensions at 20 days at the two temperatures. After 90 days storage, the pH of Ora-Plus and Ora-Sweet or Ora-Sweet SF changed between -0.10 and -0.25 units. For others suspensions, the pH changes were not significant (< -0.09 unit). No change was observed in color, odor or visual microbiology. To conclude, we recommended the use of idebenone in Inorpha vehicle stable for at least 90 days at 25 °C.

Analytical Method and Stability Study for Oral Suspension of Idebenone in Syrspend

“…Similar results have been reported for other oral pediatric IDB suspensions. Specifically, IDB 100 mg/mL is determined stable for 90 days when stored at 5 or 25 • C [5].…”

“…The IDB works as a CoQ10-like compound exhibiting similar antioxidant and electron chain transport (ETC) properties involved in the generation of ATP [4]. IDB acts by transferring electrons directly to complex III of the ETC chain, bypassing the cofactor chain of complex I, restoring the generation of cellular energy (ATP) [5]. It belongs to the group of medicines with psychostimulant and nootropic activity, i.e., substances that increase brain abilities and functions; indeed, IDB is indicated for treatment of brain activities disorders [6].…”

“…So far, no stability studies have been reported for the suspension of IDB in SyrSpend SF. Furthermore, the previously cited methods for IDB stability did not report a suitable extraction protocol for this API in other carrier phases or similar preparations, but only for tablets [5]. Considering the above, it is necessary to develop and validate a method to accurately assess the kinetic degradation of IDB in SyrSpend SF by testing recovery, accuracy, and selectivity, taking into account potential interferences from the matrix and degradation products.…”

Synthesis and Characterization of PCL-Idebenone Nanoparticles for Potential Nose-to-Brain Delivery

“…After oral administration, IDB is rapidly absorbed from the gut and extensively metabolized in the liver, so that less than 1% reaches the circulation. This rate can be improved by incorporating IDB into various liquid formulations, such as suspensions, and by administering it together with fatty food [17]. Even when taking these measures, bioavailability is less than 14% in humans.…”