Quantitative Structure - Pharmacokinetics Relationships for Plasma Protein Binding of Basic Drugs.

CONCLUSIONS: PPB of basic drugs is favored by the lipophilicity, the presence of aromatic C-atoms (either non-substituted, or involved in bridged aromatic systems) and molecular volume.  The fraction ionized as a base fB and the presence of quaternary C-atoms contribute negatively to PPB. A short checklist of criteria for high PPB is defined, and an empirical rule for distinguishing between low, high and very high plasma protein binders is proposed based. This rule allows correct classification of 69% of the very high binders, 71% of the high binders and 91% of the low binders in plasma. This article is open to POST-PUBLICATION REVIEW. Registered readers (see "For Readers") may comment by clicking on ABSTRACT on the issue's contents page. PMID: 29145933 [PubMed - in process]
Source: Journal of Pharmacy and Pharmaceutical Sciences - Category: Drugs & Pharmacology Tags: J Pharm Pharm Sci Source Type: research