Barone J A, Colaizzi J L
Drug Intell Clin Pharm. 1985 Nov;19(11):847-58. doi: 10.1177/106002808501901124.
The phenothiazines have exhibited a history of problems associated with the bioequivalence of solid oral dosage forms. The more recent availability of chemically equivalent forms of thioridazine has raised new and interesting questions about the appropriateness of generic product interchange, even among brands that have been designated "therapeutically equivalent" by the Food and Drug Administration. The scrutiny that has accompanied the consideration of thioridazine products for inclusion into various state generic substitution formularies has offered an opportunity to examine issues involving bioequivalency in considerable detail. Specific bioequivalency concerns relate to: correct analysis of drug in biological fluids; the importance of evaluating active metabolites: single-dose vs. multiple-dose crossover studies; appropriate statistical power analysis; the "70/70" rule, and comparison of product variabilities. Examples of problems are cited to illustrate that significant questions still remain about the appropriate factors that should be used to establish bioequivalency.
吩噻嗪类药物在固体口服剂型的生物等效性方面一直存在问题。最近硫利达嗪化学等效剂型的出现,引发了关于通用产品互换适用性的新的有趣问题,即使是在那些被美国食品药品监督管理局指定为“治疗等效”的品牌之间。在考虑将硫利达嗪产品纳入各种州通用替代处方集的过程中所进行的审查,提供了一个详细研究生物等效性问题的机会。具体的生物等效性问题涉及:生物流体中药物的正确分析;评估活性代谢物的重要性;单剂量与多剂量交叉研究;适当的统计功效分析;“70/70”规则以及产品变异性的比较。文中列举了一些问题实例,以说明在确定生物等效性时应使用哪些适当因素方面,仍然存在重大疑问。