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百事可乐®还是可口可乐®?酸对达沙替尼吸收的影响。

Pepsi® or Coke®? Influence of acid on dasatinib absorption.

作者信息

Knoebel Randall W, Larson Richard A

机构信息

1 Department of Pharmacy, University of Chicago Medicine, Chicago, IL, USA.

2 Department of Medicine, University of Chicago Medicine, Chicago, IL, USA.

出版信息

J Oncol Pharm Pract. 2018 Mar;24(2):156-158. doi: 10.1177/1078155217692152. Epub 2017 Feb 28.

Abstract

Dasatinib is a second generation ABL kinase inhibitor used in the management of chronic myeloid leukemia or Philadelphia chromosome positive acute lymphoblastic leukemia (Ph+ ALL). Dasatinib's bioavailability is highly dependent on gastric pH. When proton-pump inhibitors (PPIs) are co-administered with dasatinib, absorption is significantly reduced. Cola intake at the time of drug administration has been demonstrated to lead to relevant increases in the bioavailability for other acid labile drugs during PPI treatment. This manuscript reviews the relevant literature supporting a strategy of temporarily lowering the gastric pH with a carbonated beverage at the time of drug administration. The use of cola provides an easy to implement way to significantly improve dasatinib bioavailability, especially during concomitant use of a PPI.

摘要

达沙替尼是一种第二代ABL激酶抑制剂,用于治疗慢性髓性白血病或费城染色体阳性急性淋巴细胞白血病(Ph+ ALL)。达沙替尼的生物利用度高度依赖于胃内pH值。当质子泵抑制剂(PPI)与达沙替尼合用时,吸收会显著降低。已证明在PPI治疗期间给药时饮用可乐会导致其他酸不稳定药物的生物利用度显著提高。本文综述了支持在给药时用碳酸饮料暂时降低胃内pH值这一策略的相关文献。使用可乐提供了一种易于实施的方法,可显著提高达沙替尼的生物利用度,尤其是在同时使用PPI期间。

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