Inclusion complex of trimethoprim with beta-cyclodextrin.
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.
Li
Ning
N
College of Pharmaceuticals and Biotechnology, Tianjin University, Tianjin 300072, PR China.
Zhang
Yun-Hui
YH
Wu
Ya-Nan
YN
Xiong
Xiao-Li
XL
Zhang
Ya-Hui
YH
D019342:Acetic Acid / Q000032:analysis / Q000737:chemistry; D002152:Calorimetry, Differential Scanning; D002626:Chemistry, Pharmaceutical / Q000379:methods; D012995:Solubility; D013053:Spectrophotometry; D013056:Spectrophotometry, Ultraviolet; D013678:Technology, Pharmaceutical / Q000379:methods; D013696:Temperature; D013818:Thermogravimetry; D013997:Time Factors; D014295:Trimethoprim / Q000032:analysis* / Q000737:chemistry*; D014867:Water / Q000737:chemistry; D014961:X-Ray Diffraction; D047392:beta-Cyclodextrins / Q000032:analysis* / Q000737:chemistry*
D047392:beta-Cyclodextrins; D014867:Water; D014295:Trimethoprim; C031215:betadex; D019342:Acetic Acid