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China Pharmacist ; (12): 977-981, 2018.
Article in Chinese | WPRIM | ID: wpr-705642


Objective: To establish an accurate and selective UPLC-MS/MS) method for the determination of afatinib in rat plas-ma. Methods: Protein precipitating by acetonitrile was used to prepare the samples. A CORTECS BEH C18column ( 50 mm × 2. 1 mm, 1. 6 μm) was used to separate the analytes at 40℃. The mobile phase consisted of acetonitrile and water (0. 1% formic acid) with the flow rate of 0. 4 ml·min-1. The analytes were quantified by multiple reaction monitoring ( MRM) mode with positive electrospray ionization, while the target fragment ions were m/z 486. 19→112. 1 for afatinib and m/z 557. 3→112. 15 for neratinib (IS). Results: The calibration curve obtained good linearity for afatinib within the range of 1–200 ng·ml-1(r=0. 998 1), and the LLOQ in rat plasma was 1. 0 ng/ml. The intra-and inter-day precisions were both≤9. 51% . The recovery of afatinib from plasma was above 77. 1% . After intragastric administration and intravenous administration of afatinib in rats, the t1/2was 7. 19 h and 2. 69 h, Cmax was 97. 78 ng·ml-1and 123. 37 ng·ml-1,and AUC(0-∞)was 1 505. 4 ng·ml-1·h and 405. 55 ng·ml-1·h, respectively. Con-clusion: The validated method can be applied in the pharmacokinetic study of afatinib at the intragastric and intravenous dosage of 10 and 2 mg·kg-1, respectively.

Chinese Journal of Clinical and Experimental Pathology ; (12): 623-628, 2017.
Article in Chinese | WPRIM | ID: wpr-609042


To investigate the effect of MMP-26 on human glioma angiogenesis and the possible mechanism.Methods The MMP-26 plasmid and empty plasmid pcDNA3.1 were stably transfected into U251 cells to establish a nude mice xenograft model,and then an in vitro human tumor tissue-based three-dimensional angiagenic model.Tissue disks were visually assessed over time to determine the percentage of wells that developed an angiogenic response(I%) and the density and length of neovessel growth were graded at intervals using a semiquantitative visual growth-rating scheme (angiogenic index,AI,0-16scale) in groups of MMP-26 transfected U251 cells (U251-MMP-26),pcDNA3.1 vector-transfected U251 cells (U251-pcDNA3.1) and non-transfected U251 cells (U251).RT-PCR and immunohistochemistry were used to detect the expression of mRNA and protein of MMP-26 and VEGF in groups of U251-MMP-26,U251-pcDNA3.1 and U251.Immunohistochemical localization of CD31 was determined in the endothelial tubes invading the fibrin-thrombin clot matrix.Results Immunohistochemical endothelial cell markers CD31 was positive in the vascular tubes invading the fibrin-thrombin clot matrix,confirming their endothelial origin.The angiogenesis results showed that difference of length of micro capillaries,density of branches,and the area occupied between U251-MMP-26 groups and control groups were significant.The percentage of tumor implants that developed invasion (I%) and the angiogenic index AI in U251-MMP-26 group on day 14 were higher than those of U251-pcDNA3.1 group and U251 group (P < 0.05).The trends of I% and AI in 14 days were significant compared with those in control groups.The expression of mRNA and protein of MMP-26and VEGF in U251-MMP-26 group was significantly higher in U251-MMP-26 group than those in U251-pcDNA3.1 group and U251 group(P <0.01).Conclusion The effect of MMP-26 on promoting glioma angiogenesis may be related to the increased expression of VEGF,which can be used as targets for anti-tumor therapy.