Li Ning, Zhang Yun-Hui, Wu Ya-Nan, Xiong Xiao-Li, Zhang Ya-Hui
College of Pharmaceuticals and Biotechnology, Tianjin University, Tianjin 300072, PR China.
J Pharm Biomed Anal. 2005 Sep 15;39(3-4):824-9. doi: 10.1016/j.jpba.2005.05.011.
The complexation of trimethoprim (TMP) with beta-cyclodextrin (beta-CD) was studied. UV-spectrophotometry and phase-solubility techniques were employed to investigate the complexation behaviour in liquid medium, and to demonstrate that the aqueous solubility of TMP increased 2.2-fold due to complexation with beta-CD. Solid samples prepared by co-evaporation (in 2 wt% acetic acid solution) have also been studied, using differential scanning calorimetry (DSC) and powder X-ray diffraction (XRD), to assess the formation of the inclusion complex. The water content of the complex and beta-CD was determined using thermo gravimetric analysis (TGA). In vitro dissolution analysis indicated that dissolution properties of TMP/beta-CD complex were superior compared to both pure TMP and the corresponding physical mixture of TMP and beta-CD.
研究了甲氧苄啶（TMP）与β-环糊精（β-CD）的络合作用。采用紫外分光光度法和相溶解度技术研究了其在液体介质中的络合行为，并证明由于与β-CD络合，TMP的水溶性提高了2.2倍。还研究了通过共蒸发（在2 wt%乙酸溶液中）制备的固体样品，使用差示扫描量热法（DSC）和粉末X射线衍射（XRD）来评估包合物的形成。使用热重分析（TGA）测定了络合物和β-CD的含水量。体外溶出度分析表明，TMP/β-CD络合物的溶出性能优于纯TMP以及TMP与β-CD的相应物理混合物。
