摘要
目的制备灯盏花素包合物冻干粉针并初步考察其安全性。方法以2-羟丙基-β-环糊精(HP-β-CD)为包合材料,采用冷冻干燥法制备灯盏花素包合物冻干粉针,摩尔连续递变法确定包合物的包合比例,红外光谱法、差示扫描量热法对包合物进行验证,高效液相色谱法测定包合物前后水溶液中药物的溶解度,并考察灯盏花素冻干粉针剂的溶血性和血管刺激性。结果包合物的包合比例为1∶2,红外光谱法和差示扫描量热法证明了包合物的形成,包合后药物的溶解度显著增加,且包合物冻干粉针无溶血性和血管刺激性。结论羟丙基-β-环糊精能够显著提高灯盏花素的溶解度,且制备的冻干粉针无溶血性和血管刺激性。
Abstract
OBJECTIVE To prepare brevescapine(BRE) inclusion complex freeze-dried powder injection and evaluate its safety.METHODS BRE-HP-β-CD inclusion complex was prepared by freeze-dried method using HP-β-CD as inclusion material.The molar ratio between host and guest was optimized by continuing variational method.The inclusion compound was identified by Infrared Spectra(IR) and Differential Scanning Calorimetry(DSC) methods.HPLC was used to determine the solubility of BRE in the inclusion complex.RESULTS The formulation was prepared and the conclusion molar ratio was 1∶2.The solubility was evidently increased and it had no hemolytic and irritant effect.CONCLUSION Brevescapine inclusion complex freeze-dried powder injection can be prepared by addition of HP-β-CD.The safety is eligible.
关键词
灯盏花素 /
2-羟丙基-β-环糊精 /
包合物 /
冷冻干燥
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Key words
brevescapine /
2-hydropropyl-β-cyclodextrin /
inclusion complex /
freeze-dried /
safety
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张慧颖;李学明;陈国广;韦萍.
灯盏花素包合物冻干粉针的制备及安全性初步考察[J]. 中国药学杂志, 2007, 42(06): 457-460
ZHNG Hui-ying;LI Xue-ming;CHEN Guo-gung;WEI Ping.
Preparation and Safety of Brevescapine Inclusion Complex Freeze-Dried Powder Injection [J]. Chinese Pharmaceutical Journal, 2007, 42(06): 457-460
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参考文献
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脚注
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