Stenz R, Bauer K H
Department of Pharmaceutical Technology, Albert-Ludwigs-University, Freiburg, Germany.
Pharmazie. 1996 May;51(5):283-7.
New physiologically approached in vitro assays are presented which allow rather quick and uncomplicated determinations of the hemolytic activity of surfactants, intended mainly to solubilize poorly soluble drugs in parenteral dosage forms. The extent and the rates of the hemoglobin release from erythrocytes during the incubation of blood with increasing additions of surfactants is thought to be a very suitable and realistic estimation of the membrane damaging side effects of amphiphilic substances. In this study the extent of free hemoglobin released into the plasma is determined by a spectrophotometric method, as well as by an enzymatic determination measuring the lactate dehydrogenase (LDH) activity. LDH is released in a similar way from damaged erythrocytes. The results of these two methods are compared. They correspond satisfactorily.
本文介绍了新的基于生理学方法的体外试验,这些试验能够相当快速且简便地测定表面活性剂的溶血活性,主要用于增溶难溶性药物以制成注射剂型。在血液与不断增加的表面活性剂孵育过程中,红细胞释放血红蛋白的程度和速率被认为是对两亲性物质膜损伤副作用非常合适且现实的评估。在本研究中,通过分光光度法以及测量乳酸脱氢酶(LDH)活性的酶法测定释放到血浆中的游离血红蛋白的程度。LDH以类似方式从受损红细胞中释放出来。比较了这两种方法的结果,它们令人满意地相符。