Frame Bill, Beal Stuart L, Miller Raymond, Barrett Jeannette, Burger Paula
Department of Clinical Pharmacology, Pfizer Global Research and Development, 2800 Plymouth Rd, Ann Arbor, MI 48105, USA.
J Pharmacokinet Pharmacodyn. 2007 Dec;34(6):753-70. doi: 10.1007/s10928-007-9067-z. Epub 2007 Aug 10.
To characterize change from baseline weight over time for pregabalin and placebo administration.
Asymptotic fraction of baseline weight was modeled with a nonmixture model and a mixture model as a function of baseline weight, exposure, time, covariate effects, and subject-specific random effects. Model fit was assessed using standard diagnostic plots. Predictive performance was assessed using both data similar to the original data, and open-label data.
The nonmixture model indicated that a typical patient (baseline weight 82 kg) receiving placebo or 300 mg/day pregabalin approached an asymptotic fractional change from baseline weight of [mean (95% prediction interval for typical individual)] 0.7% (-5.5% to 7.4%) or 2.5% (-3.8% to 9.1%), respectively, with a half-life of 17 days. Substantial between-subject variability is observed, with some drug-treated subjects remaining weight neutral or losing weight, at all levels of exposure. Structural fixed effects parameters for the two submodels (mixture model) were in close agreement with each other and with those for the nonmixture model. The mixture model described two subpopulations differing in interindividual variability. No significant interindividual-varying covariates influencing the mixture probabilities were identified other than exposure. Both models had adequate fit; both models performed well during external validation. Predictive performance (nonmixture model) was adequate to ~900 days.
The weight of a typical 82-kg patient receiving placebo or pregabalin (300 mg/day) approaches an asymptotic fractional change from baseline weight of 0.7%, or 2.5%, respectively, with a half-life of 17 days. Substantial between-subject variability remains unexplained.
描述加巴喷丁和安慰剂给药后随时间变化相对于基线体重的改变情况。
采用非混合模型和混合模型,将基线体重的渐近分数作为基线体重、暴露量、时间、协变量效应以及个体特异性随机效应的函数进行建模。使用标准诊断图评估模型拟合情况。使用与原始数据相似的数据以及开放标签数据评估预测性能。
非混合模型表明,接受安慰剂或300毫克/天加巴喷丁的典型患者(基线体重82千克)相对于基线体重的渐近分数变化分别为[平均值(典型个体的95%预测区间)]0.7%(-5.5%至7.4%)或2.5%(-3.8%至9.1%),半衰期为17天。在所有暴露水平下,均观察到个体间存在较大差异,一些接受药物治疗的受试者体重保持不变或减轻。两个子模型(混合模型)的结构固定效应参数彼此之间以及与非混合模型的参数密切一致。混合模型描述了个体间变异性不同的两个亚组。除暴露量外,未发现影响混合概率的显著个体间变化协变量。两个模型拟合良好;在外部验证期间,两个模型均表现良好。预测性能(非混合模型)在约900天内足够。
接受安慰剂或加巴喷丁(300毫克/天)的典型82千克患者的体重相对于基线体重的渐近分数变化分别为0.7%或2.5%,半衰期为17天。个体间的巨大差异仍无法解释。