Exenatide（synthetic exendin-4）, which has been approved by the Food and Drug Administration（FDA） for the adjunctive treatment of patients with type 2 diabetes, is an incretin mimetic agent. The development and val...Exenatide（synthetic exendin-4）, which has been approved by the Food and Drug Administration（FDA） for the adjunctive treatment of patients with type 2 diabetes, is an incretin mimetic agent. The development and validation of a RP-HPLC method for the quantification of the exenatide in poly（lactic-co-glycolic acid）（PLGA） microspheres is described. Separation was performed on a C4 column via a mobile phase consisting of ACN：KH2PO4（0.02 tool/L, pH=2.5） gradient elution from 30：70 to 45：55（volume ratio） in 30 min. Multi-diode array detection（DAD） appears to be most appropriate to evaluate the spectral purity of exenatide. The limits of detection and quantification of exenatide were 0.4 and 1.2 μg/mL, respectively. The calibration curve of exenatide was linear in a range of 0.025--0.2 mg/mL with a correlation coefficient of 0.9995. The results of validation study show that this method is specific, accurate（recovery〉95%）, precise（RSD〈2.0%） and robust.展开更多
目的运用美国FDA不良事件报告系统(FAERS)挖掘艾塞那肽微球使用中不良事件(ADE)风险信号,为临床合理用药和保障用药安全提供参考。方法以“艾塞那肽微球”为目标药物,检索关键词为“exenatide microspheres for injection”“LY05006”...目的运用美国FDA不良事件报告系统(FAERS)挖掘艾塞那肽微球使用中不良事件(ADE)风险信号,为临床合理用药和保障用药安全提供参考。方法以“艾塞那肽微球”为目标药物,检索关键词为“exenatide microspheres for injection”“LY05006”“AC 2993 LAR”及“bydureon”,利用SAS软件提取FAERS数据库中2012年1月2日至2023年3月31日的ADE报告数据并去重,采用报告比值比法与综合标准法对艾塞那肽微球相关ADE报告进行数据挖掘。结果共检索到艾塞那肽微球ADE报告27248份,涉及27个系统器官分类,其中严重ADE报告4719份。上报人员以消费者为主(18435例,占67.66%),上报国家以美国为主(26295例,占96.50%)。采用报告比值比法(ROR)与综合标准法(MHRA)共获得163个ADE风险信号,包括血胆固醇异常、脂肪酶升高及混合型高脂血症等新发不良反应。结论基于FAERS数据库对艾塞那肽微球上市后的ADE进行挖掘分析,可对临床用药安全和提高患者用药依从性提供参考。展开更多
The present study establishes a visualization method for the measurement of the distribution and localization of protein/peptide constituents within a single poly-lactide-co-glycolide (PLGA) microsphere using synchrot...The present study establishes a visualization method for the measurement of the distribution and localization of protein/peptide constituents within a single poly-lactide-co-glycolide (PLGA) microsphere using synchrotron radiation based Fourier-transform infrared speciiomlcroscopy (SR-FTIR). The representative infrared wavenumbers specific for protein/peptide (Exenatide) and excipient (PLGA) were identified and chemical maps at the single microsphere level were generated by measuring and plotting the intensity of these specific bands. For quantitative analysis of the distribution within microspheres, Matlab soft are was used to transform the map file into a 3D matrix and the matiix values specific for the drug and excipient were extracted. Comparison of the normalized SR- FM maps of PLGA and Exenatide indicated that PLGA was unit-on-lily distributed, while Exenatide was relatively non-uniformly distributed in the microspheres. In conclusion, SR-FTIR is a rapid, nondestructive and sensitive detection technology to provide the distribution of chemical constituents and functional groups in microparticles and microspheres. (C) 2015 Chinese Pharmaceutical Association and Institute of Materia 'Medico, Chinese Academy of 'Medical Sciences. Production and hosting by Elsevier B.V.展开更多
基金Supported by the Key Projects in the National Science & Technology Pillar Program in the Eleventh Five-year Plan Period,China(No.2008ZX10001-012)
文摘Exenatide（synthetic exendin-4）, which has been approved by the Food and Drug Administration（FDA） for the adjunctive treatment of patients with type 2 diabetes, is an incretin mimetic agent. The development and validation of a RP-HPLC method for the quantification of the exenatide in poly（lactic-co-glycolic acid）（PLGA） microspheres is described. Separation was performed on a C4 column via a mobile phase consisting of ACN：KH2PO4（0.02 tool/L, pH=2.5） gradient elution from 30：70 to 45：55（volume ratio） in 30 min. Multi-diode array detection（DAD） appears to be most appropriate to evaluate the spectral purity of exenatide. The limits of detection and quantification of exenatide were 0.4 and 1.2 μg/mL, respectively. The calibration curve of exenatide was linear in a range of 0.025--0.2 mg/mL with a correlation coefficient of 0.9995. The results of validation study show that this method is specific, accurate（recovery〉95%）, precise（RSD〈2.0%） and robust.
基金financial support from the National Natural Science Foundation of China (Nos.81273453 and 81430087)
文摘The present study establishes a visualization method for the measurement of the distribution and localization of protein/peptide constituents within a single poly-lactide-co-glycolide (PLGA) microsphere using synchrotron radiation based Fourier-transform infrared speciiomlcroscopy (SR-FTIR). The representative infrared wavenumbers specific for protein/peptide (Exenatide) and excipient (PLGA) were identified and chemical maps at the single microsphere level were generated by measuring and plotting the intensity of these specific bands. For quantitative analysis of the distribution within microspheres, Matlab soft are was used to transform the map file into a 3D matrix and the matiix values specific for the drug and excipient were extracted. Comparison of the normalized SR- FM maps of PLGA and Exenatide indicated that PLGA was unit-on-lily distributed, while Exenatide was relatively non-uniformly distributed in the microspheres. In conclusion, SR-FTIR is a rapid, nondestructive and sensitive detection technology to provide the distribution of chemical constituents and functional groups in microparticles and microspheres. (C) 2015 Chinese Pharmaceutical Association and Institute of Materia 'Medico, Chinese Academy of 'Medical Sciences. Production and hosting by Elsevier B.V.
