کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1222880 967873 2011 7 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Effect of cyclodextrins on the solubility and stability of candesartan cilexetil in solution and solid state
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آنالیزی یا شیمی تجزیه
پیش نمایش صفحه اول مقاله
Effect of cyclodextrins on the solubility and stability of candesartan cilexetil in solution and solid state
چکیده انگلیسی

Guest–host interactions of candesartan cilexetil (CAND) with cyclodextrins (CyDs) have been investigated using phase solubility diagrams (PSD), X-ray powder diffractometry (XRPD), differential scanning calorimetry (DSC) and molecular mechanical modelling (MM). Estimates of the complex formation constant (K11) show that the tendency of CAND (pKa = 6.0) to complex with CyDs follows the order: β-CyD > HP-β-CyD > γ-CyD > α-CyD. Complex formation of CAND with β-CyD (ΔG° = −31.5 kJ/mol) is largely driven by enthalpy change (ΔH° = −32.8 kJ/mol) and slightly retarded by entropy change (ΔS° = −4.6 J/mol K). The HPLC results indicate that complex prepared by freeze drying method is chemically not stable due to the formation of amorphous CAND. Also it may suggest formulating CAND with β-CyD by kneading (dispersion) or co-evaporation (real inclusion complex) methods into capsule rather than compressed in tablets, where the compression enhances the instability of CAND. DSC thermograms for CAND/β-CyD complexes proved the formation of inclusion complexes with new solid phase. MM studies indicate the partial penetration of CAND into the β-CyD cavity.

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Journal of Pharmaceutical and Biomedical Analysis - Volume 54, Issue 3, 20 February 2011, Pages 503–509
نویسندگان
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