The Metastable Form of Tolbutamide Crystals obtained by Using Sulfobutyl ether β-cyclodextrin

• Main Authors: WIE-JHIH SHIH, 石惟之
• Other Authors: C.L. Liu
• Format: Others
• Language: zh-TW
• Published: 2009
• Online Access: http://ndltd.ncl.edu.tw/handle/52597705765941860658

碩士 === 國立東華大學 === 生物技術研究所 === 97 === Polymorphic drugs exhibit difference in physicochemical properties, such as melting point, dissolution rate, density, stability, and crystal shape, although they have the same chemical structure. Therefore it is important to purify and analyze these polymorphic drugs. Tolbutamide is hard to dissolve in water; nevertheless, it has four kinds of crystal forms: form I, form II, form III and form IV Form I is stable crystal form, but Form II, Form III, Form IV are not. In this experiment we used Sulfobutyl ether β-cyclodextrin (SBE-β-cyclodextrin) a circle glucose compound with polar outside and non-polar inside, to enhance the solubility of Tolbutamide and purified the metastable crystals. We adjusted 0.01M PBS buffer to pH:11.5 by 0.1M NaOH and 0.1M HCl. After Tolbutamide was completely dissolved in the buffer containing SBE-β-cyclodextrin, the increase in the solubility of Tolbutamide was analyzed by UV-Vis spectrophotometer. The pH value of the solution was adjusted to pH:6 by titration. Then the pH:6 solution was stored in 4℃ for 12 hrs until Tolbutamide crystalline totally formed. These crystals analyzed by powder X-ray diffractometry (PXRD), differential scanning calorimetry (DSC), and FT/IR. Moreover, the solubility and dissolution rate for the appeared crystals were also analyzed.