Levy M Y, Langerman L, Gottschalk-Sabag S, Benita S
Department of Pharmacy, School of Pharmacy, Hebrew University of Jerusalem, Israel.
Pharm Res. 1989 Jun;6(6):510-6. doi: 10.1023/a:1015928825882.
Diazepam has been incorporated into a stable, submicronized injectable emulsion. Venous sequela induction in rabbits following iv administration of diazepam in a marketed hydroalcoholic solution and in the emulsion were determined and compared over a 5-day period. There was a marked difference in the local reactions induced by the iv administration of the marketed diazepam hydroalcoholic solution and the diazepam emulsion, even on the first postinjection day. This difference was confirmed by pathological analysis. The highest mean venous sequela score was reached by the rabbit group injected with the marketed diazepam solution. It should be noted that no statistical difference was observed between the saline and the diazepam emulsion rabbit groups during the 5 days of the observation period. The moderate increase in the venous sequela score values compared to that for the saline solution should be attributed to the intrinsic effect produced by diazepam itself, and not to the emulsion vehicle, which was shown not to induce any vascular reaction in the present study.
地西泮已被制成一种稳定的、亚微米化的注射用乳剂。测定并比较了市售含醇水溶液中的地西泮和乳剂静脉注射后5天内家兔静脉后遗症的诱发情况。即使在注射后的第一天，静脉注射市售地西泮含醇水溶液和地西泮乳剂所引起的局部反应也存在显著差异。这一差异通过病理分析得到了证实。注射市售地西泮溶液的家兔组静脉后遗症平均得分最高。应当指出，在观察期的5天内，生理盐水组和地西泮乳剂组家兔之间未观察到统计学差异。与生理盐水相比，静脉后遗症得分值的适度增加应归因于地西泮本身产生的内在效应，而不是乳剂载体，在本研究中已表明该载体不会诱发任何血管反应。
