کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
2484900 | 1114339 | 2012 | 16 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Application of Modelâbased Methods to Characterize Exenatideâloaded Doubleâwalled Microspheres: In vivo Release, Pharmacokinetic/Pharmacodynamic Model, and In Vitro and In Vivo Correlation
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موضوعات مرتبط
علوم پزشکی و سلامت
داروسازی، سم شناسی و علوم دارویی
اکتشاف دارویی
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چکیده انگلیسی
The objective of this study was to characterize exenatide doubleâwalled microspheres (DWMS) using modelâbased methods. Exenatide DWMS were prepared using oilâinâoilâinâwater method, and physicochemical characterization and in vitro release and degradation of DWMS were evaluated. The pharmacokinetics (PK) and pharmacodynamics (PD) were investigated after subcutaneous injection to diabetic rats. Transit compartment model was used to describe the in vivo release of exenatide from DWMS successfully. On the basis of the insulinotropic effects of exenatide and hypoglycemic effects of insulin, PK/PD model was developed and nicely described the concentration-effect relationship of exenatide. Moreover, on the basis of the transit compartment model, a simulation method was applied to predict in vivo release, and in vitro and in vivo correlation was established. In conclusion, DWMS was a promising vehicle for delivery of exenatide, and the proposed PK/PD model allowed a better understanding of the pharmacological properties of exenatide DWMS. Transit compartment modelâbased modeling and simulation methods provided more options for the description and prediction of the in vivo exenatide release from DWMS.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Journal of Pharmaceutical Sciences - Volume 101, Issue 10, October 2012, Pages 3946-3961
Journal: Journal of Pharmaceutical Sciences - Volume 101, Issue 10, October 2012, Pages 3946-3961
نویسندگان
Xingang Li, Liang Li, Xipei Wang, Yupeng Ren, Tianyan Zhou, Wei Lu,