Zinc-leuprolide complex:: preparation, physicochemical characterization and release behaviour from in situ forming implant
Zinc-leuprolide complex:: preparation, physicochemical characterization and release behaviour from in situ forming implant
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DOI：
10.1002/psc.894
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发表时间：
2007-10-01
影响因子：
2.1
通讯作者：
Erfan, Mohammad
中科院分区：
文献类型：
--
作者：
Astaneh, Reyhaneh;Nafissi-Varcheh, Nastaran;Erfan, Mohammad
醋酸亮丙瑞林 (LA) 已被接受作为前列腺癌的治疗方法，目前也在治疗阿尔茨海默病的 II 期临床试验中进行评估。本研究制备了亮丙瑞林的锌配合物，并通过傅里叶变换红外（FTIR）、差示扫描量热（DSC）、紫外、X射线衍射（XRD）、原子吸收光谱、元素分析测定了其结构，并与醋酸亮丙瑞林的这些参数进行了比较。此外，还研究了亮丙瑞林及其复合形式原位形成植入物 (ISFI) 与商业制剂 (Eligard) 的体外释放曲线。这些研究表明，在 LA 从 ISFI 爆发释放后，锌络合物可以有效合成并影响三相模式，并将这种趋势转变为连续释放曲线。非线性回归测试也证实了这种转变是零阶释放曲线。版权所有 (C) 2007 欧洲肽协会和 John Wiley & Sons, Ltd.
Leuprolide acetate (LA) has been accepted as treatment for prostatic cancer and is currently also being evaluated in phase II clinical trials for the treatment of Alzheimer's disease. In this study, the zinc complex of leuprolide was prepared and its structure determined by Fourier-transform infrared (FTIR), differential scanning calorimetry (DSC), UV, X-ray diffraction (XRD), atomic absorption spectroscopy, elemental analysis, and compared with these parameters for leuorolide acetate. Also, the in vitro release profile of leuprolide and its complex form in situ forming implant (ISFI) in comparison to a commercial formulation (Eligard) was investigated. These studies indicate that the zinc complex can be effectively synthesized and influenced on tri-phasic pattern after burst release of LA from the ISFI and shifts this trend to a continuous release profile. Non-linear regression test confirmed this transformation as a zero-order release profile as well. Copyright (C) 2007 European Peptide Society and John Wiley & Sons, Ltd.