An Injectable Oil-Based Depot Formulation of <i>N</i>-Acyloxymethyl Prodrug of Ropivacaine for Long-Acting Local Analgesia: Formulation Development and In Vitro/In Vivo Evaluation.

ABSTRACT: Objectives: The development of novel long-acting injectables for local anesthetics is necessary to effectively manage the acute postoperative pain. The aim of this study was to prepare an injectable oil-based formulation of ropivacaine (ROP) prodrug (ropivacaine stearoxil, ROP-ST) and to investigate the pharmacokinetics and pharmacodynamics after injectable administration. Methods: A novel N-acyloxymethyl prodrug of ROP, i.e., ROP-ST, was synthesized and its physicochemical properties such as log P, solubility and stability characterized. A soybean oil-based depot of ROP-ST was prepared, and the in-vitro release of ROP-ST was evaluated using an "inverted-cup" method. Pharmacokinetic profiles and tissue retention properties were investigated after intramuscular administ

SUBMITTER: Liu X 

PROVIDER: S-EPMC11768344 | biostudies-literature | 2024 Dec

REPOSITORIES: biostudies-literature