Establishment of an in vivo analytical method for detecting total anti-UFH activity and pharmacokinetic study in PS and R15 in rats.

ABSTRACT: Protamine sulfate (PS), the only U.S. Food and Drug Administration (FDA)-approved heparin antagonist, is encumbered by several drawbacks. R15, a synthetic polyarginine peptide, has proven to be a promising protamine substitute in prior studies. PS and R15 undergo biotransformation to active metabolites, underscoring the need for an analytical method that quantifies their total anti-heparin activity in vivo. Here, we reported the development and validation of such a method and described the pharmacokinetic profiles of PS and R15 in rats. Total anti-heparin activity in plasma was quantified by fortifying each sample with a fixed concentration of heparin and subsequently measuring the residual heparin. The method was fully validated for PS and R15 in accordance with Chinese bioanalytical guid

SUBMITTER: Li H 

PROVIDER: S-EPMC12503259 | biostudies-literature | 2025

REPOSITORIES: biostudies-literature