Sgoutas D, MacMahon W, Love A, Jerkunica I
J Pharm Pharmacol. 1986 Aug;38(8):583-8. doi: 10.1111/j.2042-7158.1986.tb03085.x.
The ultracentrifugal fractionation of human serum after previous incubation with cyclosporin A showed that, in healthy fasting individuals, 8% of cyclosporin A was found in the very low density lipoproteins (VLDL), 31% in the low density lipoproteins (LDL), 46% in the high density lipoproteins (HDL) and 15% in the non-lipoprotein protein fraction. In non-fasted, healthy and in non-fasted, lipaemic individuals, 7 and 6% of cyclosporin A was found in chylomicrons, 9 and 13% in VLDL, 28 and 30% in LDL, 39 and 37% in HDL, and 12 and 13% in the non-lipoprotein protein fraction, respectively. In patients receiving cyclosporin A the distribution varied from 12 to 19% in VLDL, 21 to 28% in LDL, 33 to 43% in HDL, and 13 to 20% in non-lipoprotein proteins. The interaction between cyclosporin A and isolated normal human lipoproteins was also studied by ultrafiltration. All lipoproteins exhibited a non-saturable, low affinity, high capacity uptake for cyclosporin A. Analysis of the uptake by phospholipid vesicles showed a similar uptake, suggesting that cyclosporin A dissolves in the lipophilic portion of the lipoprotein molecule rather than being associated with specific binding sites.
在与环孢素A预先孵育后，对人血清进行超速离心分级分离，结果显示，在健康的空腹个体中，8%的环孢素A存在于极低密度脂蛋白（VLDL）中，31%存在于低密度脂蛋白（LDL）中，46%存在于高密度脂蛋白（HDL）中，15%存在于非脂蛋白蛋白组分中。在非空腹的健康个体和非空腹的血脂异常个体中，分别有7%和6%的环孢素A存在于乳糜微粒中，9%和13%存在于VLDL中，28%和30%存在于LDL中，39%和37%存在于HDL中，12%和13%存在于非脂蛋白蛋白组分中。在接受环孢素A治疗的患者中，其分布情况为：VLDL中占12%至19%，LDL中占21%至28%，HDL中占33%至43%，非脂蛋白蛋白中占13%至20%。还通过超滤研究了环孢素A与分离出的正常人脂蛋白之间的相互作用。所有脂蛋白对环孢素A均表现出非饱和、低亲和力、高容量的摄取。对磷脂囊泡摄取情况的分析显示出类似的摄取情况，这表明环孢素A溶解于脂蛋白分子的亲脂部分，而非与特定结合位点相关联。
