In vitro hemolysis: guidance for the pharmaceutical scientist.
Pharmaceutical excipients are commonly incorporated into parenteral formulations to increase solubility and stability of active pharmaceutical ingredients. The biocompatibility of these excipients is an important consideration during formulation development. Despite the importance of hemolytic potential of parenteral formulations, there is considerable contradictory information in the literature related to the hemolytic potential of various excipients. The hemolytic potential of various formulation vehicles in dog, rabbit, and human blood by means of an in vitro hemolysis assay is compared. The selected formulation vehicles are found in currently marketed drug products. The guidance presented here considers formulations with a hemolysis value of <10% to be nonhemolytic while values > 25% to be at risk for hemolysis.
Amin
Ketan
K
Johnson & Johnson Co., Global Pharmaceutical Supply Group, 1150 Route 22 East, Bridgewater, NJ 08807, USA. kamin1@gpsus.jnj.com
Dannenfelser
Rose-Marie
RM
D000818:Animals; D002626:Chemistry, Pharmaceutical; D064420:Drug-Related Side Effects and Adverse Reactions; D004912:Erythrocytes / Q000187:drug effects; D005079:Excipients / Q000737:chemistry* / Q000494:pharmacology*; D017408:Guidelines as Topic / Q000592:standards*; D006461:Hemolysis / Q000187:drug effects*; D006801:Humans; D066298:In Vitro Techniques; D007263:Infusions, Parenteral; D007275:Injections, Intravenous; D004364:Pharmaceutical Preparations / Q000008:administration & dosage / Q000737:chemistry*
D005079:Excipients; D004364:Pharmaceutical Preparations