Pharmacie, Hôpital Universitaire Necker - Enfants Malades, Paris, France.
Pharmacie, Institut Gustave Roussy, Villejuif, France.
J Oncol Pharm Pract. 2022 Mar;28(2):337-342. doi: 10.1177/1078155221991200. Epub 2021 Jan 31.
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.
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.
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.
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.
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.
伊马替尼是一种蛋白酪氨酸激酶抑制剂，目前仅以 100mg 和 400mg 片剂形式在商业上销售。新的口服液体制剂的研制适用于儿科和吞咽困难的患者，特别是在没有商业制剂的情况下。这使得剂量能够得到调整，并确保了给药的安全性。
研制伊马替尼的口服儿科混悬液，浓度为 30mg/mL，并评估其在治疗费城染色体阳性慢性髓性白血病的儿科患者中的稳定性。
在 2-8°C 下储存 30 天时，评估制剂的物理化学稳定性参数：外观、pH 值、渗透压和药物含量。使用经验证的高效液相色谱法（HPLC）结合紫外吸收检测器测定溶液的浓度。同样进行了微生物稳定性测试。
在冰箱温度下储存 30 天后，伊马替尼的剩余浓度至少为初始浓度的 95%。在研究期间，制剂的物理性质没有观察到任何变化。
稳定性研究表明，浓度为 30mg/mL 的伊马替尼口服溶液为儿科患者和吞咽困难的患者提供了一种替代商业片剂剂型的选择。
