US Food and Drug Administration Center for Veterinary Medicine, Office of New Animal Drug Evaluation, Rockville, Maryland, 20855, USA.
AAPS J. 2018 Jun 25;20(4):78. doi: 10.1208/s12248-018-0238-1.
When in vitro dissolution profile variability prohibits the use of the F2 metric, there currently is no satisfactory alternative available. Published reports evaluating alternative approaches such as Multivariate Statistical Distance and use of a bootstrap F2 identify sources of bias that can limit the utility of these alternatives. Within veterinary medicine, an additional complication is the potential magnitude of interlot variability associated with dosage forms containing "natural" ingredients. In situations when both interlot and intralot variability need to be factored in the test and reference profile comparison, we designed a method that integrates such concepts as F2, USP S1 and S2 criteria and statistical tolerance limits. Unlike F2, this alternative approach integrates a statistical confidence into the determination through the use of tolerance limits about the reference product profile. Moreover, while differences in product variability, along with differences in mean profiles, will influence the comparability assessment, this method does not impose the need to confirm homogeneity of variances: there is not direct statistical comparison of test versus reference dissolution data. For more typical situations when interlot variability is not a concern, the F2 component can be omitted from the profile comparison. Lastly, by being a model-independent approach, we avoid the potential for introducing error into the comparability determination due either to model misspecification or problems associated with a lack of collinearity. This manuscript details this alternative approach and the results of performance characterization efforts to illustrate its behavior under a range of potential situations.
当体外溶出度变异禁止使用 F2 度量标准时,目前尚无令人满意的替代方法。已发表的评估替代方法的报告,如多变量统计距离和使用 bootstrap F2,确定了可能限制这些替代方法效用的偏差来源。在兽医领域,另一个复杂情况是与含有“天然”成分的剂型相关的批间变异性的潜在幅度。在需要将批间和批内变异都纳入测试和参考曲线比较的情况下,我们设计了一种方法,该方法集成了 F2、USP S1 和 S2 标准以及统计公差限制等概念。与 F2 不同,这种替代方法通过使用关于参考产品曲线的公差限制,将统计置信度集成到确定中。此外,尽管产品变异的差异以及平均曲线的差异会影响可比性评估,但该方法并不需要确认方差的同质性:测试与参考溶出度数据之间没有直接的统计比较。对于批间变异性不是问题的更典型情况,可以从曲线比较中省略 F2 成分。最后,作为一种模型独立的方法,我们避免了由于模型指定不当或由于缺乏共线性而导致的比较确定中引入错误的可能性。本文详细介绍了这种替代方法以及性能特征描述工作的结果,以说明其在一系列潜在情况下的行为。