We found a match
Your institution may have access to this item. Find your institution then sign in to continue.
- Title
Pharmaceutical Excipients and Drug Metabolism: A Mini-Review.
- Authors
Patel, Rahul; Barker, James; ElShaer, Amr
- Abstract
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.
- Subjects
DRUG metabolism; DRUGS; PHARMACOKINETICS; PHARMACOLOGY; DRUG bioavailability; PHARMACEUTICAL powders; ENZYME metabolism; BIOAVAILABILITY
- Publication
International Journal of Molecular Sciences, 2020, Vol 21, Issue 21, p8224
- ISSN
1661-6596
- Publication type
Article
- DOI
10.3390/ijms21218224