Ohshima T, Johno I, Kitazawa S
Department of Hospital Pharmacy, School of Medicine, Nagoya University, Japan.
Ther Drug Monit. 1988;10(3):310-5. doi: 10.1097/00007691-198803000-00013.
The free fraction of drugs was determined comparatively with new microultrafiltration devices, Molcut II (Catalogue No. SJGC type) (MLII) and (Catalogue No. PLGC type) (NML; a device derived by changing the membrane component of MLII), which were developed by Nihon Millipore Ltd., Tokyo, Japan. The results obtained with the device are compared with those of MPS-1 (MPS), which is commercially available from Amicon Co., Danvers, MA, U.S.A. Drugs tested are phenytoin, carbamazepine, valproic acid, theophylline, phenobarbital, and gliclazide. In five of six drugs the free fraction by MLII shows lower values, although that by NML is in good agreement with MPS. The lower values of free fraction of drugs obtained with MLII may be caused by adsorption to the device. The adsorption increase is relatively correlated to increasing lipophilicity of drugs. The results suggest that physicochemical properties of each drug, especially hydrophobicity, should be taken into account, when a new device is used to examine protein binding of drugs. The NML, which is less expensive and is convenient because no special instrument is needed, is a reliable and satisfactory device for routine therapeutic free drug monitoring.
使用日本东京日东电工株式会社研发的新型微超滤装置Molcut II（产品编号SJGC型）（MLII）和（产品编号PLGC型）（NML，一种通过改变MLII膜组件衍生而来的装置）对药物的游离分数进行了比较测定。将该装置获得的结果与美国马萨诸塞州丹弗斯市密理博公司商业化提供的MPS - 1（MPS）的结果进行了比较。所测试的药物有苯妥英、卡马西平、丙戊酸、茶碱、苯巴比妥和格列齐特。在六种药物中的五种中，MLII测得的游离分数显示较低值，尽管NML测得的结果与MPS相当。MLII测得的药物游离分数较低值可能是由于药物吸附到该装置上所致。吸附增加与药物亲脂性的增加相对相关。结果表明，当使用新装置检测药物的蛋白结合时，应考虑每种药物的物理化学性质，尤其是疏水性。NML价格较低且使用方便，因为无需特殊仪器，是用于常规治疗性游离药物监测的可靠且令人满意的装置。
