速食总是更好吗?对乙酰氨基酚片剂与颗粒剂在体弱老年人中的药代动力学

J. Hias, K. Walgraeve, L. Linden, P. Mian, B. Koch, K. Allegaert, P. Annaert, J. Tournoy, I. Spriet
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Samples were collected at trough levels (T0) and at +0.5 (T0.5), +1 (T1), +2 (T2), +4 (T4), +5 (T5) and +6 hours (T6). PK parameters were evaluated for both paracetamol formulations. Results 36 patients were included, with a mean age (±SD) of 86.78 (±4.20) years. Most of the patients (n=26/36, 72%) received the tablet; 10 patients (28%) were prescribed the granulate formulation. Seven (21%) patients achieved an average plasma concentration (Css) above the analgesic target of 10 mg/L. Median Css (IQR) for the tablet group was 7.76 (6.31–9.08) mg/L and 9.27 (4.94–11.03) mg/L for the granulate group. Tmax was 50.5 (31.50–92.50) min and 42.50 (33.75–106.75) min for the tablet and granulate formulation, respectively (p=1.00). Cmax for tablet users was 15.95 (12.38–21.19) mg/L and 15.59 (10.80–21.77) mg/L for the granulate users (p=0.698). Conclusion and relevance Large interindividual differences in PK parameters were found in a very old patient sample. 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引用次数: 0

摘要

背景和重要性疼痛在年老体弱的成年人中非常普遍,扑热息痛是主要的治疗方法。疼痛管理通常是次优的,使用不同的扑热息痛配方可能会改善疼痛控制。目前尚不清楚快速溶解的扑热息痛颗粒制剂是否会改善暴露。目的和目的我们的目的是确定两种不同配方的口服扑热息痛在老年体弱成人中的药代动力学(PK)。材料和方法80岁及以上的老年住院患者在上午8点、下午2点和晚上8点接受1000mg扑热息痛片剂或颗粒剂治疗,符合入选条件。样品在低谷水平(T0)和+0.5 (T0.5)、+1 (T1)、+2 (T2)、+4 (T4)、+5 (T5)和+6小时(T6)采集。对两种扑热息痛制剂的PK参数进行了评价。结果本组患者36例,平均年龄(±SD)为86.78(±4.20)岁。大多数患者(n=26/36, 72%)服用了该药;10例患者(28%)采用颗粒剂处方。7例(21%)患者达到平均血药浓度(Css)高于止痛目标10mg /L。片剂组的中位Css (IQR)为7.76 (6.31 ~ 9.08)mg/L,颗粒剂组的中位Css (IQR)为9.27 (4.94 ~ 11.03)mg/L。片剂和颗粒剂的Tmax分别为50.5 (31.50 ~ 92.50)min和42.50 (33.75 ~ 106.75)min (p=1.00)。片剂服用者Cmax为15.95 (12.38 ~ 21.19)mg/L,颗粒剂服用者Cmax为15.59 (10.80 ~ 21.77)mg/L (p=0.698)。结论及相关性在一个非常老的患者样本中发现了很大的个体间PK参数差异。片剂和颗粒剂的Tmax、Cmax等吸收参数无显著差异。在颗粒组患者中观察到更高的Css趋势。参考文献和/或致谢利益冲突无利益冲突
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5PSQ-181 Is instant always better? Pharmacokinetics of tablet versus granulate formulation of paracetamol in frail older adults
Background and importance Pain is highly prevalent in old, frail adults with paracetamol as the mainstay treatment. Pain management is regularly suboptimal and using different paracetamol formulations might improve pain control. It is not known whether faster dissolving formulations of paracetamol granulate result in improved exposure. Aim and objectives Our objective was to determine the pharmacokinetics (PK) of two different formulations of oral paracetamol in old, frail adults. Material and methods Geriatric inpatients aged 80 years or older were eligible for inclusion if they received 1000 mg of paracetamol as a tablet or a granulate formulation at 8am, 2pm and 8pm. Samples were collected at trough levels (T0) and at +0.5 (T0.5), +1 (T1), +2 (T2), +4 (T4), +5 (T5) and +6 hours (T6). PK parameters were evaluated for both paracetamol formulations. Results 36 patients were included, with a mean age (±SD) of 86.78 (±4.20) years. Most of the patients (n=26/36, 72%) received the tablet; 10 patients (28%) were prescribed the granulate formulation. Seven (21%) patients achieved an average plasma concentration (Css) above the analgesic target of 10 mg/L. Median Css (IQR) for the tablet group was 7.76 (6.31–9.08) mg/L and 9.27 (4.94–11.03) mg/L for the granulate group. Tmax was 50.5 (31.50–92.50) min and 42.50 (33.75–106.75) min for the tablet and granulate formulation, respectively (p=1.00). Cmax for tablet users was 15.95 (12.38–21.19) mg/L and 15.59 (10.80–21.77) mg/L for the granulate users (p=0.698). Conclusion and relevance Large interindividual differences in PK parameters were found in a very old patient sample. Absorption parameters such as Tmax and Cmax were not significantly different between the tablet and granulate formulation. A trend for a higher Css was observed for patients in the granulate group. References and/or acknowledgements Conflict of interest No conflict of interest
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