Chan K, Davison S C, Dehghan A, Hyman N
Methods Find Exp Clin Pharmacol. 1981 Sep-Oct;3(5):291-6.
Plasma levels of pyridostigmine and/or neostigmine were monitored in 8 myasthenic patients who were stabilised on oral pyridostigmine bromide only (60-540 mg per day), and in 9 patients who were stabilised on both neostigmine bromide (15-480 mg per day) and pyridostigmine bromide (240-1080 mg per day), over a period of 12 hr (8.00 a.m. - 8.00 p.m.). Maximum plasma concentrations of pyridostigmine in the first and second groups of patients ranged from 12.4 to 64.5 ng per ml and 15.3 to 144.0 ng per ml respectively. Despite this general intersubject variation in bioavailability of pyridostigmine, there was a direct relationship between the area under plasma concentration-time curves (AUC) and total daily dose in the first group of myasthenic patients (r = 0.95). However, no such observation was noticed neither in all 17 patients nor in the 9 patients who were treated with both drugs. Neostigmine was detected in only one of the second group of patients. It was suggested that neostigmine might interfere with the bioavailability of pyridostigmine when both drugs are concurrently administered orally.
对8例仅口服溴吡斯的明(每日60 - 540毫克)病情稳定的重症肌无力患者,以及9例同时口服溴新斯的明(每日15 - 480毫克)和溴吡斯的明(每日240 - 1080毫克)病情稳定的患者,在12小时内(上午8点至晚上8点)监测血浆中吡斯的明和/或新斯的明水平。第一组和第二组患者中吡斯的明的最大血浆浓度分别为每毫升12.4至64.5纳克和每毫升15.3至144.0纳克。尽管吡斯的明的生物利用度存在这种个体间的普遍差异,但在第一组重症肌无力患者中,血浆浓度-时间曲线下面积(AUC)与每日总剂量之间存在直接关系(r = 0.95)。然而,在所有17例患者中以及在同时接受两种药物治疗的9例患者中均未观察到这种情况。仅在第二组的1例患者中检测到新斯的明。有人提出,当两种药物同时口服给药时,新斯的明可能会干扰吡斯的明的生物利用度。