Amin Ketan, Dannenfelser Rose-Marie
Johnson & Johnson Co., Global Pharmaceutical Supply Group, 1150 Route 22 East, Bridgewater, NJ 08807, USA.
J Pharm Sci. 2006 Jun;95(6):1173-6. doi: 10.1002/jps.20627.
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.
药物辅料通常被添加到注射用制剂中，以提高活性药物成分的溶解度和稳定性。在制剂研发过程中，这些辅料的生物相容性是一个重要的考量因素。尽管注射用制剂的溶血潜力很重要，但文献中关于各种辅料溶血潜力的信息存在相当大的矛盾。通过体外溶血试验比较了各种制剂载体在犬、兔和人血液中的溶血潜力。所选的制剂载体存在于目前市场上销售的药品中。此处给出的指导意见认为，溶血值<10%的制剂为非溶血制剂，而溶血值>25%的制剂有溶血风险。
