Lemaire M, Tillement J P
J Pharm Pharmacol. 1982 Nov;34(11):715-8. doi: 10.1111/j.2042-7158.1982.tb06206.x.
The distribution of cyclosporin A between plasma, leucocytes and erythrocytes was studied in vitro by means of sedimentation in Ficoll-Paque and dextran. The uptake by erythrocytes was found to be about 50% and the fraction of cyclosporin A bound to leucocytes amounted to 15%. Fractionation of plasma by ultracentrifugation also showed that two thirds of the drug were associated with lipoproteins whereas binding studies with isolated lipoproteins and plasma also indicated that lipoproteins were the major complexing constituents for cyclosporin A in plasma. The binding of cyclosporin A to erythrocytes and lipoproteins seems to be a linear process. The binding to the leucocytes may be a saturable process, however it is of minor importance in terms of the overall binding capacity in the blood.
通过在聚蔗糖-泛影葡胺和葡聚糖中沉降的方法，在体外研究了环孢素A在血浆、白细胞和红细胞之间的分布。发现红细胞的摄取量约为50%，与白细胞结合的环孢素A部分占15%。通过超速离心对血浆进行分级分离也表明，三分之二的药物与脂蛋白相关，而对分离的脂蛋白和血浆进行的结合研究也表明，脂蛋白是血浆中环孢素A的主要络合成分。环孢素A与红细胞和脂蛋白的结合似乎是一个线性过程。与白细胞的结合可能是一个可饱和的过程，然而就血液中的总体结合能力而言，它的重要性较小。
