Telmisartan (TEL) was entrapped into β-cyclodextrin aiming the improvement of its biopharmaceutical properties of low solubility. A solid state grinding process was used to prepare the molecular inclusion complex (MIC) for up to 30min. The inclusion ratio of drug and β-cyclodextrin was established as 1:2 and 1:3 (mol/mol) by phase solubility study and Job Plot. DSC, XRPD and FTIR confirmed the molecular interactions between TEL and β-cyclodextrin. Computer molecular modeling supports the presence of hydrogen bonds between guest and host and demonstrated the most probable complexes configuration. MIC_1:2_30 and MIC_1:3_30 enhanced the dissolution rate of the drug achieving a delivery rate comparable with the reference medicine available in the market (81
作者:Paola Aline Amarante, Borba;Marihá, Pinotti;George Ricardo Santana, Andrade;Nivan Bezerra, da Costa;Luiz Renato, Olchanheski Junior;Daniel, Fernandes;Carlos Eduardo Maduro, de Campos;Hellen Karine, Stulzer
来源:Carbohydrate polymers 2015 年 133卷