Blagodatskikh S V, Martsevich S Iu, Metelitsa V I, Kutishenko N P, Kozyreva M P, Simkhaev L S, Slastinkova I D, Vakulovskaia M K
Eksp Klin Farmakol. 1995 May-Jun;58(3):25-7.
Isosorbide-5-mononitrate (IMN) concentration-antianginal effect relationships were studied in 14 coronary heart diseases patients with stable exertion-induced angina after administration of Efox (Schwarz-Pharma) as two dosage forms: routinely acting tablets (20 mg) and long-acting capsules (50 mg). The antianginal effect index was an increase of treadmill exercise duration (sec) as compared with placebo, the concentration and effect were measured in points 0, 1, 3, and 7 hours after administration, in some patients, investigations were conducted 12 and 24 hours. The two formulations were found to be highly effective drugs whose action lasted 7 hours, by that time the effect of the tablets substantially decreased, which was associated with decreases in drug concentrations. The efficiency of the capsules at this point was significantly higher than that of the tablets. The use of the capsules resulted in tachyphylaxis--rapid decreasing responses to IMN. Following 7 hours of their administration there is a significant decrease in their effect with an increase in IMN concentrations.
对14例稳定型劳力性心绞痛冠心病患者服用依福(施瓦茨制药公司)的两种剂型后,研究了单硝酸异山梨酯(IMN)浓度与抗心绞痛效应的关系,这两种剂型为常规作用片剂(20毫克)和长效胶囊(50毫克)。抗心绞痛效应指标是与安慰剂相比跑步机运动持续时间(秒)的增加,在给药后0、1、3和7小时测量浓度和效应,在一些患者中,在12和24小时进行了研究。发现这两种制剂都是高效药物,其作用持续7小时,到那时片剂的效应大幅下降,这与药物浓度降低有关。此时胶囊的疗效明显高于片剂。胶囊的使用导致快速耐受性——对IMN的反应迅速降低。给药7小时后,随着IMN浓度的增加,其效应显著降低。