BACKGROUND:Warfarin potassium (Wf) commercial tablets originally formulated for adults are ground before administration to pediatric patients and elderly patients with dysphagia. OBJECTIVE:The present study investigated the effect of tablet grinding on the photostability of four types of commercialWf tablets and predicted the photostability of the tablet powders by chemometric analysis. METHODS:The photodegradation of Wf content was evaluated by reversed-phase column high-performance liquid chromatography with ultraviolet (HPLC-UV). RESULTS: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-name 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. CONCLUSION: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.

中文翻译：

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粉状药片中华法林钾的光化学稳定性

背景：最初为成人配制的华法林钾 (Wf) 市售片剂在用于患有吞咽困难的儿科患者和老年患者之前是研磨的。目的：本研究调查了片剂研磨对四种商品 Wf 片剂光稳定性的影响，并通过化学计量学分析预测了片剂粉末的光稳定性。方法:采用反相柱高效液相色谱-紫外色谱法(HPLC-UV)评价Wf含量的光降解。结果：散装 Wf 粉末相对耐光，而磨碎的 Wf 片剂经历了显着的光降解。对一种商品名 Wf 市售片剂和三种通用名 Wf 市售片剂的研磨粉末的光稳定性进行了定量评估和比较。在某些情况下，所有三种磨碎的仿制药中的 Wf 的光稳定性都低于磨碎的品牌药片。光照射28天后，品牌药片Wf含量降至69.79%，而部分仿制药片Wf含量降至31.90%。为了阐明影响各种 Wf 制剂中相对光稳定性的因素，我们通过基于每种添加剂的光稳定性筛选的偏最小二乘回归分析来分析活性成分和赋形剂之间的分子间相互作用。结论：结果表明，添加剂轻质无水硅酸和聚维酮对Wf片的稳定性有不利影响。此外，研磨片剂的光稳定性受其配方的影响很大。光照射28天后，品牌药片Wf含量降至69.79%，而部分仿制药片Wf含量降至31.90%。为了阐明影响各种 Wf 制剂中相对光稳定性的因素，我们通过基于每种添加剂的光稳定性筛选的偏最小二乘回归分析来分析活性成分和赋形剂之间的分子间相互作用。结论：结果表明，添加剂轻质无水硅酸和聚维酮对Wf片的稳定性有不利影响。此外，研磨片剂的光稳定性受其配方的影响很大。光照射28天后，品牌药片Wf含量降至69.79%，而部分仿制药片Wf含量降至31.90%。为了阐明影响各种 Wf 制剂中相对光稳定性的因素，我们通过基于每种添加剂的光稳定性筛选的偏最小二乘回归分析来分析活性成分和赋形剂之间的分子间相互作用。结论：结果表明，添加剂轻质无水硅酸和聚维酮对Wf片的稳定性有不利影响。此外，研磨片剂的光稳定性受其配方的影响很大。为了阐明影响各种 Wf 制剂中相对光稳定性的因素，我们通过基于每种添加剂的光稳定性筛选的偏最小二乘回归分析来分析活性成分和赋形剂之间的分子间相互作用。结论：结果表明，添加剂轻质无水硅酸和聚维酮对Wf片的稳定性有不利影响。此外，研磨片剂的光稳定性受其配方的影响很大。为了阐明影响各种 Wf 制剂中相对光稳定性的因素，我们通过基于每种添加剂的光稳定性筛选的偏最小二乘回归分析来分析活性成分和赋形剂之间的分子间相互作用。结论：结果表明，添加剂轻质无水硅酸和聚维酮对Wf片的稳定性有不利影响。此外，研磨片剂的光稳定性受其配方的影响很大。结果表明，添加剂轻质无水硅酸和聚维酮对Wf片剂的稳定性有不利影响。此外，研磨片剂的光稳定性受其配方的影响很大。结果表明，添加剂轻质无水硅酸和聚维酮对Wf片剂的稳定性有不利影响。此外，研磨片剂的光稳定性受其配方的影响很大。