Kaminskaia G O, Firsova V A, Gubkina M F, Efimova L N
Central NII of Tuberculosis RAMN, Moscow.
Probl Tuberk. 1997(2):45-7.
Isoniazid concentrations were measured in the serum, liver, and lungs of the animals 1, 3, 6, and 24 hours after administration of isoniazid in a dose of 10 mg/kg via various routes (orally, intramuscularly, and lymphotropically--into the pretracheal cellular space) guinea-pig blood and organs in the experiment on 36 guinea-pigs. Within the first 1-3 hours after intramuscular injection of isoniazid, its concentrations in the serum and lungs were higher than those with other routes of administration. With lymphotropic and oral routes, the levels of the drug were very similar in all the studied media in the first 6 hours, but later its hepatic accumulation after lymphotropic administration proved to be considerably lower than via other routes. The lymphotropic injection of isoniazid provides its therapeutic concentrations in the blood and in the lung and simultaneously creates prerequisites for reducing the incidence and severity of hepatotoxic adverse reactions.
在一项对36只豚鼠进行的实验中,以10毫克/千克的剂量通过不同途径(口服、肌肉注射以及向淋巴组织——气管前细胞间隙)给豚鼠注射异烟肼后,在给药后1小时、3小时、6小时和24小时测量动物血清、肝脏和肺部中的异烟肼浓度。肌肉注射异烟肼后的最初1 - 3小时内,其在血清和肺部中的浓度高于其他给药途径。采用向淋巴组织给药和口服途径时,在最初6小时内所有研究介质中的药物水平非常相似,但后来向淋巴组织给药后其在肝脏中的蓄积量明显低于其他途径。向淋巴组织注射异烟肼可在血液和肺部中提供治疗浓度,同时为降低肝毒性不良反应的发生率和严重程度创造了条件。