von Dardel O, Mebius C, Mossberg T, Svensson B
Br J Anaesth. 1983 Jan;55(1):41-7. doi: 10.1093/bja/55.1.41.
Conventional preparations of diazepam for i.v. use contain solvents which cause pain on injection and thrombophlebitis in a high percentage of cases. However, diazepam can be dissolved with advantage in the oleaginous phase of an oil-in-water emulsion (Diazemuls). Diazemuls has been given to 9492 patients without serious side-effects. Following i.v. injection, 2435 patients were studied with respect to pain and clinical effect. Only 0.4% experienced pain. The intended clinical effect was recorded in 99% of the patients. I.m. injection of Diazemuls resulted in a significantly smaller frequency of pain in connection with the injection than did the injection of Valium (7% and 43% respectively). Pharmacokinetic studies have been made after i.v. and i.m. injection of Diazemuls and Valium. The distribution and elimination phases after i.v. injection were the same with both forms. Thus the drug probably quickly separates from the oil particles of the emulsion after injection. After i.m. administration, the plasma concentration shows a wide spread with both preparations. A brief survey of other substances tested in emulsion form is presented.
传统的静脉注射用地西泮制剂含有溶剂,这些溶剂在注射时会引起疼痛,并且在很大比例的病例中会导致血栓性静脉炎。然而,地西泮可以有利地溶解在水包油乳液(Diazemuls)的油相中。已给9492例患者使用Diazemuls,未出现严重副作用。静脉注射后,对2435例患者的疼痛和临床效果进行了研究。只有0.4%的患者感到疼痛。99%的患者记录到了预期的临床效果。肌肉注射Diazemuls与注射安定相比,注射时疼痛的发生率显著更低(分别为7%和43%)。已对静脉注射和肌肉注射Diazemuls及安定后的药代动力学进行了研究。两种制剂静脉注射后的分布和消除阶段相同。因此,药物在注射后可能很快从乳液的油颗粒中分离出来。肌肉注射后,两种制剂的血浆浓度都有很大差异。本文简要介绍了以乳液形式测试的其他物质。