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Updated: Nov 19, 2025
Scaled-Up Preparation of an Intermediate of Upatinib, ACT051-3
Published on: April 7, 2023
Design and stability of pediatric oral formulation of imatinib
Mélanie Hinterlang1, Amandine Gendron2, Thomas Fleury2
1Pharmacie, Hôpital Universitaire Necker - Enfants Malades, Paris, France.
Insights
A new imatinib oral solution (30 mg/mL) is stable for 30 days under refrigeration. This provides a crucial alternative for pediatric cancer patients and those with swallowing difficulties.
Area of Science:
- Pharmaceutical Sciences
- Oncology
- Drug Formulation
Background:
- Imatinib, a tyrosine kinase inhibitor, is primarily available as tablets (100mg, 400mg).
- Pediatric patients and those with dysphagia require alternative oral formulations.
- Lack of commercial liquid forms necessitates development for tailored dosing and administration.
Purpose of the Study:
- To formulate a stable pediatric oral solution of imatinib at 30 mg/mL.
- To assess the physicochemical and microbiological stability of the imatinib oral solution.
- To support treatment of pediatric Philadelphia chromosome-positive chronic myeloid leukemia.
Main Methods:
- Physicochemical stability evaluated (appearance, pH, osmolality, drug content) over 30 days at 2-8°C.
- Drug concentration quantified using validated High-Performance Liquid Chromatography (HPLC) with UV detection.
- Microbiological stability assessments were also conducted.
Main Results:
- Imatinib concentration remained above 95% of the initial value after 30 days of refrigerated storage.
- No significant changes in the physical properties of the oral solution were observed.
- The formulation demonstrated microbiological stability.
Conclusions:
- The 30 mg/mL imatinib oral solution is a stable alternative to commercial tablet formulations.
- This formulation is suitable for pediatric use and patients with swallowing impairments.
- It offers improved dosage flexibility and administration safety.
Background:
Imatinib is a protein-tyrosine kinase inhibitor which is currently only commercially available as a tablet dosage form in the strength of 100mg and 400mg. The elaboration of new oral liquid formulations is suitable in pediatrics and for patients who have difficulties to swallow, notably in the absence of commercial forms. This enables the adaptation of dosage and secure the administration.
Objectives:
The formulation of an oral pediatric solution of imatinib at a concentration of 30 mg/mL and the evaluation of its stability for the treatment of pediatric patients with Philadelphia chromosome positive chronic myeloid leukemia.
Methods:
The physicochemical stability parameters: appearance, pH, osmolality, and drug content of formulation were evaluated for 30 days when stored at 2-8°C. Concentration of solution was measured with a validated method using high performance liquid chromatography (HPLC) coupled with an absorbance UV detector. Equally, microbiological stability was performed.
Results:
The remaining imatinib concentration was at least 95% of the initial concentration after 30 days stored in fridge temperature. No changes were observed regarding the physical properties of the formulation during the study period.
Conclusions:
The stability study showed that the imatinib oral solution at a concentration of 30 mg/mL provides an alternative option at the commercial tablet dosage forms for pediatric patients and patients who have difficulties to swallow.
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