Taubøll E, Lindström S, Klem W, Gjerstad L
Dept. of Neurology, Rikshospitalet, University of Oslo, Norway.
Epilepsy Res. 1990 Sep-Oct;7(1):59-64. doi: 10.1016/0920-1211(90)90054-y.
Carbamazepine (CBZ) could be dissolved in Glycofurol (polyethylene glycol monotetra-hydrofurfuryl ether) with concentrations up to 100 mg/ml, and the solutions were stable for at least 14 days. Ethanol or benzyl alcohol was added without loss in solubility, while water, human serum albumin or Intralipid always led to immediate precipitation. The effect of a CBZ/Glycofurol solution on focal seizure threshold in the visual cortex in cats was investigated using a cerveau isolé preparation. Fourteen experiments were performed using i.v. injections of CBZ with concentrations ranging from 0.2 to 20 mg/kg. In all experiments with doses greater than 1 mg/kg the CBZ/Glycofurol injections exerted a pronounced and immediate effect on the seizure threshold, while Glycofurol alone was ineffective. On average, seizure threshold increased more than 5-fold with doses in the range of 5-20 mg/kg. Investigating the effect of CBZ/Glycofurol on picrotoxin-induced seizure activity in cats, 2 injections of 5 mg/ml of CBZ immediately stopped the seizure activity as evaluated by electrocorticography, while interictal activity remained.
卡马西平（CBZ）可溶解于聚乙二醇单四氢糠基醚（Glycofurol）中，浓度高达100毫克/毫升，且溶液至少可稳定保存14天。添加乙醇或苄醇不会降低溶解度，而添加水、人血清白蛋白或脂肪乳剂总会立即导致沉淀。使用孤立脑制备法研究了卡马西平/聚乙二醇单四氢糠基醚溶液对猫视觉皮层局灶性癫痫阈值的影响。通过静脉注射浓度范围为0.2至20毫克/千克的卡马西平进行了14次实验。在所有剂量大于1毫克/千克的实验中，卡马西平/聚乙二醇单四氢糠基醚注射对癫痫阈值产生了显著且即时的影响，而单独使用聚乙二醇单四氢糠基醚则无效。平均而言，剂量在5至20毫克/千克范围内时，癫痫阈值增加了5倍以上。在研究卡马西平/聚乙二醇单四氢糠基醚对猫匹鲁卡品诱导的癫痫活动的影响时，通过皮层脑电图评估，注射两次5毫克/毫升的卡马西平可立即停止癫痫活动，但发作间期活动仍存在。
