کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
2010916 1066991 2014 5 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
The pharmacokinetics and hypoglycaemic effect of sunitinib in the diabetic rabbits
ترجمه فارسی عنوان
فارماکوکینتیک و اثر هیپوگلیسمی سولیتینیب در خرگوشهای دیابتی
موضوعات مرتبط
علوم زیستی و بیوفناوری بیوشیمی، ژنتیک و زیست شناسی مولکولی زیست شیمی
چکیده انگلیسی

BackgroundDiabetes is one of the most common metabolic diseases in the world, which may influence changes in the pharmacokinetics and pharmacodynamics of drugs. Sunitinib is a tyrosine kinase inhibitor (TKI) broadly used for treatment of numerous cancers, which exhibits the side hypoglycaemic effect. The aim of the study was a comparison of concentrations and pharmacokinetics of sunitinib after a single administration in rabbits with hyperglycaemia and normoglycaemia (control group). Additionally, the effect of sunitinib on glucose levels was investigated.MethodsThe research was carried out on a control group (n = 6) and a group of rabbits with diabetes (n = 6). The rabbits were treated with sunitinib in the oral dose of 25 mg. Plasma concentrations of sunitinib and its metabolite (SU12662) were measured with validated HPLC method with UV detection.ResultsThe comparison of the sunitinib Cmax and AUC0–∞ in the diabetic group with the control group gave the ratios of 1.63 [90% confidence interval (CI) [1.59; 1.66] and 2.03 [1.97; 2.09], respectively. Statistically significant differences between the analyzed groups were revealed for Cmax (p = 0.006), AUC0–∞ (p = 0.0088), and AUCkel (p = 0.009). The maximum glycaemia drop of 14.4–69.6% and 15.4–33.5% was observed in the diabetic animals and in the control group, respectively. The glycaemia values returned to the initial values in 24 h after the administration of the drug.ConclusionsThe research proved the significant influence of diabetes on the pharmacokinetics of sunitinib and it confirmed the hypoglycaemic effect of the TKI in diabetic rabbits and in normoglycaemia.

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Pharmacological Reports - Volume 66, Issue 5, October 2014, Pages 892–896
نویسندگان
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