美国食品药品监督管理局应消除当前生物药剂分类系统生物豁免指导原则中的歧义，并公布已获得生物药剂分类系统生物豁免的药物。
The FDA should eliminate the ambiguities in the current BCS biowaiver guidance and make public the drugs for which BCS biowaivers have been granted.
机构信息
Department of Bioengineering and Therapeutic Sciences, Schools of Pharmacy and Medicine, University of California, San Francisco, San Francisco, California, USA.
出版信息
Clin Pharmacol Ther. 2010 Sep;88(3):405-7. doi: 10.1038/clpt.2010.149. Epub 2010 Jul 28.
Abstract
Although US Food and Drug Administration (FDA)-approved Biopharmaceutics Classification System (BCS) class 1 drugs are designated as high-permeability drugs, in fact, the criterion utilized is high extent of absorption. This ambiguity should be eliminated, and the FDA criterion should explicitly be stated as > or =90% absorption based on absolute bioavailability or mass balance. Maintaining confidentiality regarding the drugs for which the FDA has approved BCS waivers of in vivo bioequivalence studies is not good public policy and should be reversed.
摘要
虽然美国食品和药物管理局 (FDA) 批准的生物药剂学分类系统 (BCS) 1 类药物被指定为高渗透性药物，但实际上，所使用的标准是高吸收率。这种模糊性应该消除，FDA 的标准应该明确规定为基于绝对生物利用度或质量平衡的 > 或 = 90%吸收。对 FDA 已批准 BCS 豁免体内生物等效性研究的药物保密不是良好的公共政策，应该予以扭转。
相似文献
1
The FDA should eliminate the ambiguities in the current BCS biowaiver guidance and make public the drugs for which BCS biowaivers have been granted.美国食品药品监督管理局应消除当前生物药剂分类系统生物豁免指导原则中的歧义，并公布已获得生物药剂分类系统生物豁免的药物。
Clin Pharmacol Ther. 2010 Sep;88(3):405-7. doi: 10.1038/clpt.2010.149. Epub 2010 Jul 28.
2
BCS Biowaivers: Similarities and Differences Among EMA, FDA, and WHO Requirements.生物药剂学分类系统生物豁免：欧洲药品管理局、美国食品药品监督管理局和世界卫生组织要求之间的异同
AAPS J. 2016 May;18(3):612-8. doi: 10.1208/s12248-016-9877-2. Epub 2016 Mar 4.
3
Feasibility of biowaiver extension to biopharmaceutics classification system class III drug products: cimetidine.生物豁免扩展至生物药剂学分类系统III类药品的可行性：西咪替丁
Clin Pharmacokinet. 2006;45(4):385-99. doi: 10.2165/00003088-200645040-00004.
4
Impact of the US FDA "Biopharmaceutics Classification System" (BCS) Guidance on Global Drug Development.美国 FDA“生物药剂学分类系统”（BCS）指导原则对全球药物开发的影响。
Mol Pharm. 2017 Dec 4;14(12):4334-4338. doi: 10.1021/acs.molpharmaceut.7b00687. Epub 2017 Nov 7.
5
Evaluation of Excipient Risk in BCS Class I and III Biowaivers.BCS 分类 I 和 III 生物豁免辅料风险评估。
AAPS J. 2022 Jan 5;24(1):20. doi: 10.1208/s12248-021-00670-1.
6
A comparative analysis of biopharmaceutics classification system and biopharmaceutics drug disposition classification system: a cross-sectional survey with 500 bioequivalence studies.生物药剂学分类系统与生物药剂学药物处置分类系统的比较分析：一项涉及 500 项生物等效性研究的横断面调查。
J Pharm Sci. 2013 Sep;102(9):3136-44. doi: 10.1002/jps.23515. Epub 2013 Apr 11.
7
Biopharmaceutics classification system: the scientific basis for biowaiver extensions.生物药剂学分类系统：生物豁免扩展的科学依据。
Pharm Res. 2002 Jul;19(7):921-5. doi: 10.1023/a:1016473601633.
8
Classification of torasemide based on the Biopharmaceutics Classification System and evaluation of the FDA biowaiver provision for generic products of CLASS I drugs.基于生物药剂学分类系统对托拉塞米进行分类以及对FDA关于I类药物仿制药生物等效性豁免规定的评估。
J Pharm Pharmacol. 2006 Nov;58(11):1475-82. doi: 10.1211/jpp.58.11.0008.
9
The Effect of Excipients on the Permeability of BCS Class III Compounds and Implications for Biowaivers.辅料对BCS III类化合物渗透性的影响及生物豁免的意义
Pharm Res. 2016 Jan;33(1):167-76. doi: 10.1007/s11095-015-1773-4. Epub 2015 Aug 19.
10
Impact of Biopharmaceutics Classification System-based biowaivers.基于生物药剂学分类系统的生物豁免的影响。
Mol Pharm. 2010 Oct 4;7(5):1539-44. doi: 10.1021/mp1001747. Epub 2010 Sep 7.
引用本文的文献
1
An Overview on Dietary Polyphenols and Their Biopharmaceutical Classification System (BCS).膳食多酚及其生物药剂学分类系统（BCS）概述。
Int J Mol Sci. 2021 May 24;22(11):5514. doi: 10.3390/ijms22115514.
2
Few Drugs Display Flip-Flop Pharmacokinetics and These Are Primarily Associated with Classes 3 and 4 of the BDDCS.很少有药物呈现出双翻转药代动力学，并且这些药物主要与生物药剂学分类系统（BDDCS）的3类和4类相关。
J Pharm Sci. 2015 Sep;104(9):3229-35. doi: 10.1002/jps.24505. Epub 2015 May 25.
3
Distinguishing between the permeability relationships with absorption and metabolism to improve BCS and BDDCS predictions in early drug discovery.区分与吸收和代谢相关的渗透性，以改善早期药物发现中的BCS和BDDCS预测。
Mol Pharm. 2014 Apr 7;11(4):1335-44. doi: 10.1021/mp4007858. Epub 2014 Mar 28.
4
Drug discovery and regulatory considerations for improving in silico and in vitro predictions that use Caco-2 as a surrogate for human intestinal permeability measurements.药物发现和监管方面的考虑因素，以提高使用 Caco-2 作为人体肠道通透性测量替代物的计算和体外预测的准确性。
AAPS J. 2013 Apr;15(2):483-97. doi: 10.1208/s12248-013-9456-8. Epub 2013 Jan 24.
5
The role of BCS (biopharmaceutics classification system) and BDDCS (biopharmaceutics drug disposition classification system) in drug development.BCS（生物药剂学分类系统）和 BDDCS（生物药剂学药物处置分类系统）在药物开发中的作用。
J Pharm Sci. 2013 Jan;102(1):34-42. doi: 10.1002/jps.23359. Epub 2012 Nov 12.
6
Bioequivalence requirements in the European Union: critical discussion.欧盟生物等效性要求：批判性讨论。
AAPS J. 2012 Dec;14(4):738-48. doi: 10.1208/s12248-012-9382-1. Epub 2012 Jul 24.
7
Elucidating the role of dose in the biopharmaceutics classification of drugs: the concepts of critical dose, effective in vivo solubility, and dose-dependent BCS.阐明剂量在药物生物药剂学分类中的作用：关键剂量、有效体内溶解度和剂量依赖性 BCS 的概念。
Pharm Res. 2012 Nov;29(11):3188-98. doi: 10.1007/s11095-012-0815-4. Epub 2012 Jul 4.
9
Toward global standards for comparator pharmaceutical products: case studies of amoxicillin, metronidazole, and zidovudine in the Americas.迈向全球标准的对照药品：在美洲的阿莫西林、甲硝唑和齐多夫定案例研究。
AAPS J. 2012 Sep;14(3):462-72. doi: 10.1208/s12248-012-9350-9. Epub 2012 Apr 19.
10
BDDCS applied to over 900 drugs.BDDCS 应用于超过 900 种药物。
AAPS J. 2011 Dec;13(4):519-47. doi: 10.1208/s12248-011-9290-9. Epub 2011 Aug 5.
本文引用的文献
1
The use of drug metabolism for prediction of intestinal permeability (dagger).利用药物代谢预测肠道通透性（剑号）。
Mol Pharm. 2009 Jan-Feb;6(1):74-81. doi: 10.1021/mp8001864.
2
The use of BDDCS in classifying the permeability of marketed drugs.采用生物药剂学分类系统（BDDCS）对市售药物的渗透性进行分类。
Pharm Res. 2008 Mar;25(3):483-8. doi: 10.1007/s11095-007-9523-x. Epub 2008 Jan 31.
3
Intestinal permeability and its relevance for absorption and elimination.肠道通透性及其与吸收和排泄的相关性。
Xenobiotica. 2007 Oct-Nov;37(10-11):1015-51. doi: 10.1080/00498250701704819.
4
Biopharmaceutics classification of selected beta-blockers: solubility and permeability class membership.选定β受体阻滞剂的生物药剂学分类：溶解度和渗透性类别归属
Mol Pharm. 2007 Jul-Aug;4(4):608-14. doi: 10.1021/mp070028i. Epub 2007 Jul 18.
5
What is the objective of the mass balance study? A retrospective analysis of data in animal and human excretion studies employing radiolabeled drugs.质量平衡研究的目的是什么？对使用放射性标记药物的动物和人体排泄研究中的数据进行回顾性分析。
Drug Metab Rev. 2007;39(1):17-43. doi: 10.1080/03602530600952172.
6
Permeability classification of representative fluoroquinolones by a cell culture method.通过细胞培养法对代表性氟喹诺酮类药物进行通透性分类
AAPS PharmSci. 2004 Apr 5;6(2):e13. doi: 10.1208/ps060213.
7
A theoretical basis for a biopharmaceutic drug classification: the correlation of in vitro drug product dissolution and in vivo bioavailability.生物药剂学药物分类的理论基础：体外药物溶出度与体内生物利用度的相关性。
Pharm Res. 1995 Mar;12(3):413-20. doi: 10.1023/a:1016212804288.
Zotero 插件