Prancan A V, Ecanow B, Bernardoni R J, Sadove M S
J Pharm Sci. 1980 Aug;69(8):970-1. doi: 10.1002/jps.2600690828.
The significant occurrence of thrombophlebitis in patients administered diazepam intravenously was described recently. This side effect has been attributed to the crystallization of diazepam and its subsequent precipitation upon contact with blood or intravenous fluids. The current study was designed to reveal whether the solubilizing capability of poloxamer 188 reduces the incidence of thrombotic and inflammatory effects of diazepam in rabbits. The incidence of early (3-hr) ear vein necrosis was 72% in the diazepam-treated ears, while the incidence of necrosis in the ears that received poloxamer 188 as a vehicle for diazepam was 25%. The occurrence of thrombosis and loss of vessel integrity also was higher in diazepam-treated ears than in those treated with diazepam plus poloxamer 188. Solubilization of diazepam with poloxamer 188 may decrease the incidence of the tested side effects.
最近有文献报道了静脉注射地西泮的患者中血栓性静脉炎的显著发生率。这种副作用被归因于地西泮的结晶及其与血液或静脉输液接触后的沉淀。本研究旨在揭示泊洛沙姆188的增溶能力是否能降低地西泮在兔体内的血栓形成和炎症反应发生率。地西泮处理的耳朵早期（3小时）耳静脉坏死发生率为72%，而接受泊洛沙姆188作为地西泮载体的耳朵坏死发生率为25%。地西泮处理的耳朵中血栓形成和血管完整性丧失的发生率也高于地西泮加泊洛沙姆188处理的耳朵。泊洛沙姆188对地西泮的增溶作用可能会降低所测试的副作用的发生率。
