Pharmaceutical Excipients and Drug Metabolism: A Mini-Review

International Journal of Molecular Sciences

James Barker¹  Rahul Patel¹  Amr ElShaer¹ 

[1] Drug Discovery, Delivery and Patient Care (DDDPC), School of Life Sciences, Pharmacy and Chemistry, Kingston University, Kingston upon Thames, Surrey KT1 2EE, UK;

关键词: Pharmaceutical excipients;    metabolism;    cytochrome P450;   

DOI  :  10.3390/ijms21218224

来源: DOAJ

【 摘 要 】

Conclusions from previously reported articles have revealed that many commonly used pharmaceutical excipients, known to be pharmacologically inert, show effects on drug transporters and/or metabolic enzymes. Thus, the pharmacokinetics (absorption, distribution, metabolism and elimination) of active pharmaceutical ingredients are possibly altered because of their transport and metabolism modulation from the incorporated excipients. The aim of this review is to present studies on the interaction of various commonly-used excipients on pre-systemic metabolism by CYP450 enzymes. Excipients such as surfactants, polymers, fatty acids and solvents are discussed. Based on all the reported outcomes, the most potent inhibitors were found to be surfactants and the least effective were organic solvents. However, there are many factors that can influence the inhibition of CYP450, for instance type of excipient, concentration of excipient, type of CYP450 isoenzyme, incubation condition, etc. Such evidence will be very useful in dosage form design, so that the right formulation can be designed to maximize drug bioavailability, especially for poorly bioavailable drugs.

【 授权许可】

Unknown