Faculty of Pharmacy, Musashino University, Tokyo, Japan.
Biomed Mater Eng. 2021;32(2):115-129. doi: 10.3233/BME-201167.
Warfarin potassium (Wf) commercial tablets originally formulated for adults are ground before administration to pediatric patients and elderly patients with dysphagia.
The present study investigated the effect of tablet grinding on the photostability of four types of commercial Wf tablets and predicted the photostability of the tablet powders by chemometric analysis.
The photodegradation of Wf content was evaluated by reversed-phase column high-performance liquid chromatography with ultraviolet (HPLC-UV).
The bulk Wf powder was relatively photostable, whereas ground Wf tablets underwent substantial photodegradation. The photostability of the ground powders of a brand-name Wf commercial tablet and three generic Wf commercial tablets was quantitatively assessed and compared. In certain cases, the Wf in all the three ground generic tablets was less photostable than in the ground brand-name tablets. After 28 days of light irradiation, the Wf content decreased to 69.79% in the brand-name tablets, while it was 31.90% in some generic tablets. To clarify the factors influencing the relative photostability in various Wf formulations, we analyzed the intermolecular interactions between the active ingredient and the excipients by partial least-squares regression analysis based on photostability screening for each additive.
The results suggested that the additives light anhydrous silicic acid and povidone adversely affect the stability of Wf tablets. In addition, the light stability of ground tablets was affected considerably by their formulation.
华法林钾（Wf）商业片剂最初是为成人配方的，在给儿科患者和吞咽困难的老年患者服用前需要先磨碎。
本研究考察了片剂研磨对华法林钾（Wf）四种商业片剂光稳定性的影响，并通过化学计量分析预测了片剂粉末的光稳定性。
采用反相高效液相色谱法结合紫外检测（HPLC-UV）评估 Wf 含量的光降解情况。
原粉 Wf 相对稳定，而磨碎的 Wf 片剂则发生了大量光降解。对品牌 Wf 商业片剂和三种通用 Wf 商业片剂的磨碎粉末的光稳定性进行了定量评估和比较。在某些情况下，三种通用磨碎片剂中的 Wf 不如品牌片剂稳定。经过 28 天的光照，品牌片剂中的 Wf 含量降至 69.79%，而某些通用片剂中则降至 31.90%。为了阐明各种 Wf 制剂中相对光稳定性的影响因素，我们通过偏最小二乘回归分析基于对每种添加剂的光稳定性筛选，分析了活性成分与赋形剂之间的分子间相互作用。
结果表明，添加剂无水硅和聚维酮会对 Wf 片剂的稳定性产生不利影响。此外，片剂的光稳定性还受到其配方的显著影响。
