Subcutaneous injection of oral cyclosporin A solution

✍ Scribed by Rajiv Midha; Susan E. Mackinnon; Peter J. Evans; Timothy J. Best; P. Y. Wong

• Book ID: 102508744
• Publisher: John Wiley and Sons
• Year: 1992
• Tongue: English
• Weight: 265 KB
• Volume: 13
• Category: Article
• ISSN: 0738-1085
• DOI: 10.1002/micr.1920130208

✦ Synopsis

Abstract

Cyclosporin A (CyA) is the agent of choice for immunesuppression in the majority of rodent organ and tissue allotransplantation experiments. Subcutaneous injection of suitably dissolved pure CyA powder preparation is the acceptable standard of drug administration. We investigated the possibility of using oral CyA solution in an injectable form and compared its availability with that of the standard solution in a rat model. Oral CyA solution diluted in placebo (olive oil) and standard solution prepared from pure compound were injected subcutaneously at a dose of 5 mg/kg/day to two groups of rats. Trough whole blood CyA concentrations were measured on day 10 following initiation of treatment. Blood CyA levels of the standard solution group (1,167 ± 246 μg/liter, mean ± SD) were virtually identical to those of the oral solution group (1,105 ± 179 μg/liter; P > 0.05). In addition, the oral solution was easier to prepare and caused less injection site morbidity than the standard solution. We conclude that placebo‐diluted oral CyA solution may be safely injected subcutaneously to rats and results in consistent blood levels, comparable to those achieved with standard solution prepared from pure compound. © Wiley‐Liss, Inc.