Vladimirskiĭ M A, Ladygina G A, Stepanov V M
Antibiotiki. 1984 Apr;29(4):282-5.
Distribution of 3H-dihydrostreptomycin ( DHS ) in the blood serum and organs of intact mice and mice with generalized tuberculosis was studied. The antibiotic was administered in the form of a liposomal preparation and solution. It was shown that the distribution pattern of DHS administered in the form of a liposomal preparation corresponded to that of liposomes, which were the drug carriers. The serum levels of DHS injected intravenously in the form of a liposomal drug in a dose of 1 mg per mouse in the intact animals were 19 and 17 times higher 1 and 3 hours after injection, respectively as compared to those provided by the solution. In animals with generalized tuberculosis, the respective figures were 5 and 1.9 times. The levels of DHS in the liver provided by the liposomes were 4-6 times higher at all the time intervals in both the groups of animals. The antibiotic levels in the spleen of intact and infected animals were 2.5-3 and 8-12 times higher, respectively. In the lungs of intact animals, the antibiotic levels were 2 times higher 1 hour after administration. In infected animals, the levels of the antibiotic in the lung tissue were 3 times higher in 1 and 3 hours. The DHS levels in the kidneys of infected and intact animals were similar after drug administration in the form of a solution and liposomal preparation. The extremely high difference in the DHS levels in the spleen tissues of the mice with generalized tuberculosis after drug administration in the form of a solution and liposomal preparation may be of a significant importance for sanation of the organ lymphoid system affected with tuberculosis.
研究了3H-二氢链霉素(DHS)在正常小鼠和全身性结核病小鼠血清及器官中的分布情况。抗生素以脂质体制剂和溶液的形式给药。结果表明,以脂质体制剂形式给药的DHS的分布模式与作为药物载体的脂质体的分布模式相对应。在正常动物中,以脂质体药物形式静脉注射剂量为每只小鼠1mg的DHS后,血清水平在注射后1小时和3小时分别比溶液给药时高19倍和17倍。在全身性结核病动物中,相应的数字分别为5倍和1.9倍。在两组动物的所有时间间隔内,脂质体提供的肝脏中DHS水平均高4 - 6倍。正常和感染动物脾脏中的抗生素水平分别高2.5 - 3倍和8 - 12倍。在正常动物的肺部,给药1小时后抗生素水平高2倍。在感染动物中,肺组织中的抗生素水平在1小时和3小时高3倍。以溶液和脂质体制剂形式给药后,感染和正常动物肾脏中的DHS水平相似。以溶液和脂质体制剂形式给药后,全身性结核病小鼠脾脏组织中DHS水平的极高差异可能对受结核病影响的器官淋巴系统的净化具有重要意义。