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溶剂中难溶性药物硝基安定与辅料的分子间相互作用
引用本文:溶剂中难溶性药物硝基安定与辅料的分子间相互作用[J]. 中国药科大学学报, 1998, (6): 408-412.
作者姓名:杨智钧 关宏子
作者单位:中国药科大学中药制剂教研室!南京210038(杨智钧),千叶大学分析中心(关宏子),千叶大学药学部!千叶市263,日本国(米持悦生,小口敏夫,山本惠司)
摘    要:用核磁共振(NMR)谱分析了难溶性药物硝基安定与聚乙烯吡咯烷酮(PVP)、聚氧乙烯60硬化蓖麻油(HCO-60)、羟丙基甲基纤维素(HPMC)等辅料的分子间相互作用。PVP等在氘代氯仿中可使硝基安定1位氢的核磁信号向低磁场方向位移。PVP与硝基安定的相互作用比HCO-60等要强。将HPMC分散于氘代氯仿也使硝基安定的第1位质子信号向低磁场方向位移。从而证明硝基安定分子的一位氢原子和辅料分子的氧原子的分子间发生了氢键作用。

关 键 词:分子间相互作用  核磁共振  辅料  难溶性药物  聚乙烯吡咯烷酮  氢键

Molecular Interaction in Solvents Between Water Insoluble Drug Nitrazepam and Pharmaceutical Excipients
Molecular Interaction in Solvents Between Water Insoluble Drug Nitrazepam and Pharmaceutical Excipients[J]. Journal of China Pharmaceutical University, 1998, (6): 408-412.
Authors:Yang Zhijun  Seki Hiroko  Yonemochi Etsuo  Oguchi Toshio  Yamamoto Keiji
Abstract:The molecular interaction of a water- insoluble drug, nitrazepam, with polyvinylpyrrolidone K25 (PVP) , hardening castor oil polyoxyethyline-60 (HCO-60) and hydroxypropylmethylcellulose 2910 (HPMC ) was investigated. When PVP or HCO-60 was added to a deuterated chloroform solution of nitrazepam, the 1H-NMR signals of N (1 )-H shifted to lower magnetic fields. From the comparison of the extene of change in UV and NMR spectra, PVP is considered to have a stronger interaction with nitrazepam than HCO-60 etc. Although HPMC was insoluble in CDC13, suspension of HPMC also induced a lower magnetic field shift of the protone signals. Thus the molecular interactions of nitrazepam with additives were certified to result from the hydrogen-bonding between the -N (1 )-H of nitrazepam and oxygen atoms of the additive molecules.
Keywords:Molecular interaction  NMR  Excipient  Insoluble drug  Polyvinylpyrrolidone  Hydrogen bond
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