Hespe W, Blankwater Y J, Wieriks J
Arzneimittelforschung. 1975 Oct;25(10):1561-7.
With the purpose of studying the influence of polyvinylpyrrolidone (PVP) on the disposition of oxytetracycline (OTC), OTC was administered i.v. to male rats in two formulations, one of which contained 14C-labelled PVP. From the rats, whole-body sections (30 mum) were taken which were subjected to three analytical procedures: autoradiography to determine the distribution of the PVP-14C, fluorography and bioautography to obtain information on the OTC-distribution. The experimental results suggest equilibrium complex formation between OTC and PVP, it being mainly the complex which is i.v. injected when both products are combined in an injection formulation. Such complex formation can explain the lower toxicity of OTC when injected in combination with PVP as well as the slower build-up of OTC-levels in some organs, compared with that after OTC administration without PVP. Beyond this kinetic effect of PVP on the fate of OTC no evidence was obtained for an influence of PVP on the OTC distribution pattern per se, or on its ultimate antibiotic activity in the different organs. Some details of the OTC and especially of the PVP distribution are discussed.
为研究聚乙烯吡咯烷酮（PVP）对土霉素（OTC）处置的影响，将OTC以两种制剂静脉注射给雄性大鼠，其中一种制剂含有14C标记的PVP。从大鼠身上获取全身切片（30μm），并对其进行三种分析程序：放射自显影以确定PVP-14C的分布，荧光自显影和生物自显影以获取有关OTC分布的信息。实验结果表明OTC与PVP之间形成了平衡复合物，当两种产品在注射制剂中混合时，静脉注射的主要是复合物。这种复合物的形成可以解释与未添加PVP的OTC给药相比，与PVP联合注射时OTC毒性较低以及某些器官中OTC水平升高较慢的现象。除了PVP对OTC命运的这种动力学影响外，未获得PVP对OTC本身分布模式或其在不同器官中的最终抗生素活性有影响的证据。讨论了OTC尤其是PVP分布的一些细节。
