Background and objective

Swallowing difficulties (i.e., dysphagia) occur in up to 40% of the adult general population, particularly among the elderly prescribed solid oral dosage forms. Pimavanserin is approved for the treatment of hallucinations and delusions in patients with Parkinson’s disease psychosis (PDP) as a 34-mg capsule formulation. Patients with PDP may be at-risk for dysphagia that could affect administration of intact pimavanserin capsules. The stability of oral pimavanserin was evaluated in different liquid/soft food vehicles.

Methods

The stability of pimavanserin intended for oral administration was assessed by sprinkling the contents of 1 pimavanserin 34-mg capsule into water (40 mL), applesauce (40 g), vanilla Ensure (60 mL), or non-pulp orange juice (60 mL).

Results

The stability study demonstrated >95% recovery within 24 hours after contents of a 34-mg pimavanserin capsule were dispersed in applesauce, vanilla Ensure®, orange juice, or water. Assay values at 24 h for individual capsules were within 5% of time zero, and no significant change in the impurity profile was observed in any vehicle. Pimavanserin degradation products recovered from various food vehicles for individual and total degradation products were < 0.5% at all time points. In addition, the impurity profile of compatibility samples matched that obtained for a control sample.

Conclusion

These results support the ability of pimavanserin to be given orally by emptying the capsule contents into soft foods or liquids in accordance with the product label.

中文翻译：

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匹马万色林在水中和口服给药的不同载体中的体外稳定性和回收率研究

背景和目标

吞咽困难（即吞咽困难）发生在高达 40% 的普通成年人中，特别是在处方固体口服剂型的老年人中。Pimavanserin 被批准用于治疗帕金森病精神病 (PDP) 患者的幻觉和妄想，为 34 毫克胶囊制剂。PDP 患者可能存在吞咽困难的风险，这可能会影响完整匹马万色林胶囊的给药。在不同的液体/软食品载体中评估口服匹马万色林的稳定性。

方法

通过将 1 个匹马万色林 34 毫克胶囊的内容物洒入水 (40 毫升)、苹果酱 (40 克)、香草确保 (60 毫升) 或非果肉橙汁 (60 毫升) 来评估用于口服给药的匹马万色林的稳定性）。

结果

稳定性研究表明，将 34 毫克匹马万色林胶囊的内容物分散在苹果酱、香草 Ensure®、橙汁或水中后 24 小时内回收率 > 95%。单个胶囊在 24 小时的测定值在时间零的 5% 以内，并且在任何载体中均未观察到杂质谱的显着变化。从各种食品载体中回收的匹马万色林降解产物的单个和总降解产物在所有时间点均 < 0.5%。此外，相容性样品的杂质谱与对照样品的杂质谱相匹配。

结论

这些结果支持通过根据产品标签将胶囊内容物倒入软食物或液体中来口服给予匹马万色林的能力。