Effect of grinding of beta-cyclodextrin and glibenclamide on tablet properties .1. In vitro

Physical properties including dissolution characteristics of glibenclamide (CB) tablets were studied. Directly compressed and wet-granulated GB tablets gave only 35% and 40% drug dissolved, respectively. Physical mixing, kneading, and grinding of beta-cyclodextrin (CD) with GB were investigated. It was found that the grinding method could markedly enhance the release of drug from the tablets. The physical properties of these tablets were unchanged after they had been stored at 40 degrees C and 75% RH for at least 3 months. The GB/CD mixture at a ratio of 1 to 4, ground for 24 or 48 hr, exhibited superior dissolution and chemical stability. Differential scanning calorimetry indicated that an inclusion complex was produced. Decreasing grinding time or CD concentration could result in incomplete formation of the inclusion complex. It was concluded that pretreatment of the drug with CD by the grinding method could significantly improve the dissolution and stability of GB tablets.