Suzuki Nobuyuki, Kawasaki Takao
Analytical and Quality Evaluation Research Laboratories, Sankyo Co. Ltd., 1-12-1 Shinomiya, Hiratsuka, Kanagawa 254-0014, Japan.
J Pharm Biomed Anal. 2005 Feb 7;37(1):177-81. doi: 10.1016/j.jpba.2004.09.035.
The solid state forms of troglitazone drug substance and diastereomers were characterized using solid state nuclear magnetic resonance (SSNMR) spectroscopic method. The SSNMR spectroscopy could distinguish the hydrated and the non-hydrated RR/SS forms more clearly than powder X-ray diffractometry (PXRD). The SSNMR result supported that troglitazone drug substance consists of diastereomers as a simple physical mixture. SSNMR spectroscopy was also able to characterize the solid state forms of troglitazone in tablets while PXRD was unable to because of interference from the pharmaceutical additives. Troglitazone was proved to exist in amorphous form in tablets, and keep its solid state form amorphous against heat and humidity. SSNMR spectroscopy thus provides very important information for the development of the pharmaceutical formulation of troglitazone.
采用固体核磁共振（SSNMR）光谱法对曲格列酮原料药及其非对映异构体的固态形式进行了表征。与粉末X射线衍射法（PXRD）相比，SSNMR光谱法能够更清晰地区分水合和非水合RR/SS形式。SSNMR结果支持曲格列酮原料药由非对映异构体组成，是一种简单的物理混合物。SSNMR光谱法还能够对片剂中曲格列酮的固态形式进行表征，而PXRD由于受到药物添加剂的干扰而无法做到这一点。事实证明，曲格列酮在片剂中以无定形形式存在，并且在加热和潮湿条件下保持其无定形固态形式。因此，SSNMR光谱法为曲格列酮药物制剂的开发提供了非常重要的信息。
