注射用丹参酮ⅡA包合物的制备及性质考察

目的制备丹参酮ⅡA包合物,以期增加丹参酮ⅡA的溶解性及稳定性。方法以羟丙基-β-环糊精(HP--βCD)为包合材料,采用冷冻干燥法制备注射用丹参酮ⅡA包合物;用差示扫描量热法、红外光谱法及相溶解度法验证包合物的形成;考察注射用丹参酮ⅡA包合物复溶后的pH值、澄清度、渗透压、与稀释剂的配伍稳定性及溶血性等基本性质。结果差示扫描量热法、红外光谱法和相溶解度法充分显示包合物已形成;用注射用水、注射用生理盐水和质量分数为5%的葡萄糖注射液复溶后,溶液的pH值分别为5.31、4.94、4.01,渗透压分别为350、4013、82 mmol.kg-1,澄清度合格;注射用丹参酮ⅡA包合物与3种稀释剂配伍稳定,制剂无溶血。结论所制得的注射用丹参酮ⅡA包合物,制剂性质符合《中华人民共和国药典》(2005版)对注射用制剂的要求。

Preparation and characters studies of tanshinone ⅡA inclusion complex freeze-dried powder injection

study its characters. Methods tanshinone ⅡA-hydropropyl-β-cyclodextrin inclusion complex was prepared using hydropropyl-β-cyclodextrin as inclusion material. The inclusion compound was identified by dififerential scanning calorimetric, infrared spectra and phase solubility methods. The pH values, clarity, and osmotic pressure redissolved by distilled water, saline and glucose injection were determined. And the stability of compatibility with distilled water, saline and glucose injection and the hemolytic effect of the inclusion complex were investigated also. Results The inclusion was prepared and identified. After being redissolved by distilled water, saline and glucose injection, the pH values were 5.31, 4.94 and 4.01, respectively. The corresponding osmotic pressure values were 350, 401 and 382 mmol&;#8226;kg-1. The clarity was clear. It was steady diluted by the three solvents. No hemolytic effect was observed. Conclusions Tanshinone ⅡA inclusion complex freeze-dried powder injection is prepared successfully. And the characters were eligible.