EMULSION OF PERFLUORORGANIC COMPOUNDS FOR MEDICAL PURPOSES, METHOD FOR PRODUCING SAID EMULSION AND METHODS FOR CURING AND PREVENTING DISEASES WITH THE AID OF THE EMULSION
申请人:Otkrytoe Aktsionernoe Obchestvo Nauchno-Proizvodstvennaya Firma "Perftoran"
公开号:EP1306083A1
公开(公告)日:2003-05-02
An emulsion of perfluoroorganic compounds (PFOCs) with gas-transporting properties for intravascular administration comprises a perfluorocarbon rapidly eliminable from the organism and a perfluorinated tertiary amine slowly eliminable from the organism and further comprises at least three kinds of PFOC admixtures taken in small amounts, which are close in their structure and physicochemical properties to the main components and make up a series of PFOCs with gradually changing properties. The emulsion also contains minor admixtures of H-perfluoroalkanes. Such a composition contributes to the formation of a more homogeneous and stable non-clustered perfluorocarbon phase inside the emulsion particles. The PFOC emulsion is stabilized by a polyoxyethylene-polyoxypropylene copolymer. The formulation of the composition provides stability of the emulsion under storage and on entry into the blood flow, as well as a low viscosity of the PFOC emulsion, which secures a high dynamic oxygen capacity of the preparation and improves the delivery of oxygen to tissues.
When preparing the emulsion, the stabilizing agent is heated at a temperature of up to 75°C, all the components are saturated with carbon dioxide gas, and the homogenization is carried out with feeding carbon dioxide gas, whereby the origination of peroxides is minimized and the reactogenicity is thus reduced.
It is proposed to use PFOC emulsions as a means for treating air-and fat embolism, obliterating vascular injuries of extremities and poisoning with lipophilic poisons, as well as for preventing toxic injuries caused by various xenobiotics.
一种用于血管内给药的具有气体传输特性的全氟有机化合物(PFOC)乳剂,由一种可从生物体内快速消除的全氟碳化合物和一种可从生物体内缓慢消除的全氟叔胺组成,还包括至少三种少量的全氟有机化合物混合物,这些混合物的结构和理化性质与主要成分接近,并构成一系列性质逐渐变化的全氟有机化合物。乳液中还含有少量的全氟烷烃外加剂。这种成分有助于在乳液颗粒内部形成更均匀、更稳定的非成团全氟碳化物相。全氟辛烷磺酸乳液由聚氧乙烯-聚氧丙烯共聚物稳定。该组合物的配方使乳液在储存和进入血流时保持稳定,并使全氟辛烷磺酸乳液的粘度较低,从而确保制剂具有较高的动态氧容量,提高向组织输送氧气的能力。
在制备乳剂时,将稳定剂在高达 75°C 的温度下加热,用二氧化碳气体使所有成分达到饱和,并用二氧化碳气体进行均质,从而最大限度地减少过氧化物的产生,降低反应性。
建议使用 PFOC 乳剂治疗空气和脂肪栓塞、四肢血管损伤和亲脂毒物中毒,以及预防各种异种生物造成的毒性损伤。