Cazzola E, Lattuada N, Zecca L, Radice D, Luzzana M, Imbimbo B P, Auteri A, Mosca A
Dipartimento di Scienze e Tecnologie Biomediche, Università degli Studi, Milano, Italy.
Chem Biol Interact. 1993 Jun;87(1-3):265-8. doi: 10.1016/0009-2797(93)90053-2.
Eptastigmine (MF 201) is a new physostigmine derivative with potent inhibitory activity on cholinesterases. Here we present a new potentiometric cholinesterase activity assay suitable for MF 201 monitoring. The analysis is performed on a differential pH system and has the following characteristics: (a) within-run precision: C.V. 2.0% (plasma cholinesterase), 1.8% (red cell cholinesterase); (b) between-run precision: C.V. 4.0% (plasma cholinesterase); (c) linearity: 1-10 kU/l (plasma cholinesterase), 6-70 U/g Hb (red cell cholinesterase); (d) comparison with a reference method (x, HITACHI 737 Boerhinger Mannheim, Italy): y = 0.785x - 0.07; n = 37; r = 0.998. The assay has been applied to the determination of plasma and red cell cholinesterase activity in volunteers over 60 years of age treated with a single oral dose of 30 mg eptastigmine. We found that red cell cholinesterase is selectively inhibited after MF 201 administration with the following kinetics (time, % of inhibition, mean +/- S.E., n = 6): 0 h, 0; 1 h, 17 +/- 4.6; 2 h, 24 +/- 4; 4 h, 23 +/- 4.4; 12 h, 14 +/- 3. Eptastigmine plasma levels were also determined by a HPLC method: maximum concentration was found one hour after drug administration.
依他斯的明（MF 201）是一种新的毒扁豆碱衍生物，对胆碱酯酶具有强大的抑制活性。在此，我们介绍一种适用于监测MF 201的新型电位胆碱酯酶活性测定法。该分析在差分pH系统上进行，具有以下特点：（a）批内精密度：变异系数（C.V.）为2.0%（血浆胆碱酯酶），1.8%（红细胞胆碱酯酶）；（b）批间精密度：C.V.为4.0%（血浆胆碱酯酶）；（c）线性范围：1 - 10 kU/l（血浆胆碱酯酶），6 - 70 U/g Hb（红细胞胆碱酯酶）；（d）与参考方法（x，意大利日立737勃林格殷格翰）比较：y = 0.785x - 0.07；n = 37；r = 0.998。该测定法已应用于60岁以上单次口服30 mg依他斯的明的志愿者血浆和红细胞胆碱酯酶活性的测定。我们发现，给予MF 201后红细胞胆碱酯酶被选择性抑制，其动力学如下（时间，抑制百分比，均值±标准误，n = 6）：0小时，0；1小时，17±4.6；2小时，24±4；4小时，23±4.4；12小时，14±3。依他斯的明血浆水平也通过高效液相色谱法测定：给药后1小时发现最大浓度。
