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1.
Vestn Ross Akad Med Nauk ; (3): 366-71, 2015.
Artigo em Russo | MEDLINE | ID: mdl-26495727

RESUMO

BACKGROUND: One way to increase drug efficacy is to provide a drug delivery transport system to the target organ. A widely used method is to incorporate the drug in a biodegradable polymer composition with forming nanosized drug's transport forms. Objective: Our aim was to investigate the tissue biodistribution of antibiotic rifabutin transport system based on lactic and glycolic acids copolymer, and to compare it with the pure substance of rifabutin. METHODS: These substances were administered to two groups of rats intragastrically in the doses of 10 mg/kg. After a certain period of time, the animals were sacrificed by cervical dislocation. Samples preparation for analysis was carried out of the liquid-liquid extraction. Active substance's concentrations were measured by high performance liquid chromatography method. RESULTS: The study included 8-week-aged Wistar rats of both sexes weighing 0.22 ± 0.02 kg. Animals were divided into 2 groups. The study group received polymer form of antibiotic, and the comparison group received substance of rifabutin. In intervals of 10 min, 30 min, 1 h, 2 h, 4 h, 7h, 15 h, 24 h after drug administration liver, lung, spleen, kidney, intestines, stomach, heart and brain were resected respectively. Organs were measured by their weight. The drug was not detected in the brain. Rifabutin was determined in other examined tissues within 10 minutes and the maximum drug concentration in organs was fixed in 1.5-3.5 hours after administration. The rifabutin concentrations defined in the lungs were significantly higher in polymerform (p < 0.05). The polymer form's distribution coefficient was higher in the liver and lungs (15.83 and 10.14 µg/g respectively) in comparison with the substance one. The minimum amount of the active ingredient was observed in the heart (0.02 µg/g). CONCLUSION: It is shown that the inclusion of the drug in a polymeric form substantially alters its localization in organs and tissues. Extensive biodistribution nanorifabutin in lung tissue, liver and spleen is established.


Assuntos
Sistemas de Liberação de Medicamentos/métodos , Ácido Láctico/farmacologia , Fígado , Pulmão , Ácido Poliglicólico/farmacologia , Rifabutina , Baço , Animais , Antibacterianos/administração & dosagem , Antibacterianos/farmacocinética , Materiais Biocompatíveis/farmacologia , Cromatografia Líquida de Alta Pressão , Portadores de Fármacos/farmacologia , Fígado/metabolismo , Fígado/patologia , Pulmão/metabolismo , Pulmão/patologia , Nanoconjugados , Copolímero de Ácido Poliláctico e Ácido Poliglicólico , Ratos , Ratos Wistar , Rifabutina/administração & dosagem , Rifabutina/farmacocinética , Baço/metabolismo , Baço/patologia , Distribuição Tecidual
2.
Bull Exp Biol Med ; 131(4): 312-4, 2001 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-11550012

RESUMO

We evaluated the efficiency of perfusion with olifen in preventing oxidative stress at the early stage of acute pancreatitis. Transaortic perfusion with olifen prevented clinical and biochemical symptoms of acute pancreatitis, attenuated oxidative stress, reduced peritoneal exudation, and restricts the area of pancreatic necrosis to 6% tissue.


Assuntos
Antioxidantes/farmacologia , Pancreatite Necrosante Aguda/prevenção & controle , Éteres Fenílicos/farmacologia , Amilases/sangue , Animais , Gatos , Modelos Animais de Doenças , Ácido Láctico/sangue , Estresse Oxidativo , Pancreatite Necrosante Aguda/sangue , Pancreatite Necrosante Aguda/patologia
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