Oette K, Kühn G, Römer A, Niemann R, Gundermann K J, Schumacher R
Institut für Klinische Chemie der Universität zu Köln.
Arzneimittelforschung. 1995 Aug;45(8):875-9.
Essentiale and Lipostabil contain "essential" phospholipids from the soybean, mainly 1,2-dilinoleoyl-phosphatidylcholine (CAS 998-06-1, DLPC) which is considered as the main active ingredient. A single oral dose of d15-DLPC loaded with deuterium 9 times in the choline and 6 times in the linoleic acid of the 1-position was given to volunteers. Sera from 11 blood samples taken within 48 h after application were examined by means of mass spectrometry with regard to d9-choline and d6-linoleic acid in the 1- and 2-position of serum phosphatidylcholines (PC) as well as in the serum triglycerides. d9-choline, i.e. the total of d15-PC and d9-PC, showed maximum values of 5.6% of the total serum PC concentration. Normally, about 1.3% of PC in the human serum is DLPC. Serum 1-linoleoyl-PC was increased by 32-40% after oral application of d15-DLPC. A minor uptake of d6-linoleic acid into the 2-position of serum PC, which is rich in linoleic acid, and into the serum triglycerides was observed with peak values of 2.3% and 6.1%, resp. The uptake of polyunsaturated PC species like DLPC and 1-linoleoyl-PC into the liver after oral application of drugs containing such species in high amounts like "essential" phospholipids with about 50% of DLPC let expect therapeutic effects on membranes into which this special species is incorporated.
易善力和利波司太含有来自大豆的“必需”磷脂，主要是1,2 - 二亚油酰磷脂酰胆碱（CAS 998 - 06 - 1，DLPC），它被认为是主要活性成分。给志愿者口服单剂量的d15 - DLPC，其胆碱位置含9次氘，1位亚油酸含6次氘。应用后48小时内采集的11份血样的血清，通过质谱法检测血清磷脂酰胆碱（PC）1位和2位以及血清甘油三酯中的d9 - 胆碱和d6 - 亚油酸。d9 - 胆碱，即d15 - PC和d9 - PC的总和，显示出最高值为血清总PC浓度的5.6%。正常情况下，人血清中约1.3%的PC是DLPC。口服d15 - DLPC后，血清1 - 亚油酰 - PC增加了32 - 40%。观察到d6 - 亚油酸少量摄取到富含亚油酸的血清PC的2位以及血清甘油三酯中，峰值分别为2.3%和6.1%。口服含有大量此类物质（如含约50% DLPC的“必需”磷脂）的药物后，像DLPC和1 - 亚油酰 - PC这样的多不饱和PC种类被肝脏摄取，这让人预期对含有这种特殊种类的膜会有治疗效果。
