Atta-Politou J, Macheras P E, Koupparis M A
University of Athens, Panepistimiopolis, Greece.
J Toxicol Clin Toxicol. 1996;34(3):307-16. doi: 10.3109/15563659609013795.
This investigation was undertaken to study: a) the adsorption characteristics of chlorpromazine to activated charcoal and its formulations Carbomix powder and Ultracarbon tablets at gastric pH; b) the effect on chlorpromazine adsorption of polyethylene glycol and its combination with electrolyte lavage solution; c) the effect of the order of addition of polyethylene glycol-electrolyte lavage solution.
Ion selective electrode potentiometry, based on the selective, direct and continuous response of a chlorpromazine-ion selective electrode to the concentration of the free drug, was used. Successive additions of microvolumes of a chlorpromazine solution were made into a charcoal slurry in acidic medium of pH 1.2 with measurement of the chlorpromazine-ion selective electrode potential at equilibrium.
The maximum adsorption capacity values of activated charcoal, Carbomix and Ultracarbon, were 297, 563, and 382 mg/g respectively, while the affinity constant values were 40.2, 70.4, and 40.5 L/g, respectively. The adsorption of chlorpromazine to each of the Ultracarbon and Carbomix components was compared to the total adsorption of the formulations. The addition of polyethylene glycol-electrolyte lavage solution causes a slight desorption of chlorpromazine from activated charcoal at gastric pH, more pronounced when polyethylene glycol-electrolyte lavage solution follows the addition of activated charcoal, suggesting the possibility of a nonspecific binding of chlorpromazine to polyethylene glycol. The amount of chlorpromazine absorbed to Carbomix and Ultracarbon was not significantly affected at gastric pH by the presence of polyethylene glycol or polyethylene glycol-electrolyte lavage solution added either concurrently or sequentially to these formulations.
本研究旨在探讨：a）在胃内pH值条件下，氯丙嗪对活性炭及其制剂Carbomix粉末和Ultracarbon片剂的吸附特性；b）聚乙二醇及其与电解质灌洗液联合使用对氯丙嗪吸附的影响；c）聚乙二醇-电解质灌洗液添加顺序的影响。
采用离子选择性电极电位分析法，该方法基于氯丙嗪离子选择性电极对游离药物浓度的选择性、直接和连续响应。在pH为1.2的酸性介质中，向活性炭浆液中连续微量添加氯丙嗪溶液，并在平衡时测量氯丙嗪离子选择性电极电位。
活性炭、Carbomix和Ultracarbon的最大吸附容量值分别为297、563和382 mg/g，而亲和常数值分别为40.2、70.4和40.5 L/g。将Ultracarbon和Carbomix各成分对氯丙嗪的吸附与制剂的总吸附进行了比较。添加聚乙二醇-电解质灌洗液会导致在胃内pH值条件下氯丙嗪从活性炭上有轻微解吸，当聚乙二醇-电解质灌洗液在添加活性炭之后添加时更为明显，这表明氯丙嗪可能与聚乙二醇存在非特异性结合。在胃内pH值条件下，同时或先后向Carbomix和Ultracarbon中添加聚乙二醇或聚乙二醇-电解质灌洗液，对氯丙嗪在其上的吸附量没有显著影响。
