In vitro study of the embolic characteristics of imipenem/cilastatin particles

Abstract

Imipenem/cilastatin (IPM/CS) has long been administered intravenously as a carbapenem antibiotic. However, since this agent is poorly soluble in liquid, occasional reports have described its use as a short-acting, temporary embolic agent. The purpose of this study was to elucidate the characteristics of IPM/CS particles, which are thought to have pain-relieving effects against osteoarthritis-related pain, as an embolic agent. Three aspects of IPM/CS as an embolic agent were evaluated in vitro: particle size; particle shape; and change in particle size over time. For particle size, the long diameter was measured. Mean particle size (n=244) was 29.2±12.0 µm (range, 1–60 µm). Shape (n=109) was round in 18.35%, elliptical in 11.93%, and polygonal in 69.72%, showing that most particles were polygonal. In observations of changes in particle size over time (n=9), particles had decreased to 75% of their original size at 82±10.7 min, 50% at 89.3±9.14 min, 25% at 91.3±8.74 min, complete dissolved at 91.8±9.02 min. A rapid shrinkage in diameter was seen in the final period. IPM/CS particles are ultrafine and the majority display a polygonal shape. This substance shows ultra-short embolic activity. This study revealed the characteristics of a substance that demonstrates an embolic effect not found in existing embolic materials.