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穿心莲内酯磷脂复合物的制备及表征
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| 篇名： | 穿心莲内酯磷脂复合物的制备及表征 |
| TITLE： | |
| 摘要： | 目的：制备穿心莲内酯磷脂复合物，优化其处方工艺并进行表征。方法：采用溶剂法制备穿心莲内酯磷脂复合物，以复合率为评价指标，考察反应溶剂、反应时间、反应温度、药物质量浓度、投料比例等单因素对复合率的影响，再结合正交试验优化投料比、反应温度和药物浓度，并进行验证。采用紫外分光光度法（UV）及差示扫描量热分析（DSC）进行表征。比较穿心莲内酯、穿心莲内酯磷脂物理混合物和穿心莲内酯磷脂复合物在水、大豆油、丙二醇单月桂酸甘油酯（Lauroglycol FCC）中的溶解性能。结果：复合物的最佳制备工艺为以四氢呋喃为反应溶剂，反应时间为4 h，反应温度为50 ℃，药物质量浓度为10 mg/ml，穿心莲内酯与磷脂的摩尔比为1 ∶ 3。所制穿心莲内酯磷脂复合物的复合率为83.2％（n＝3） ，UV与DSC分析结果均表明复合物已形成。与原料药及物理混合物比较，磷脂复合物明显提高了穿心莲内酯在水、大豆油、Lauroglycol FCC中的溶解性能。结论：成功制得穿心莲内酯磷脂复合物。 |
| ABSTRACT： | OBJECTIVE： To prepare andrographolide phospholipid compound， optimize its formulation technology and characterizeit. METHODS： Andrographolide phospholipid compound was prepared with solvent method. Using compound rate as index， the effects of reaction solvent， reaction time， reaction temperature， drug concentration， the ratio of reactants and other single factors on compound rate were investigated. The ratio of reactants， reaction temperature and drug concentration were optimized by orthogonal test and validated. The dissolubilities of andrographolide， andrographolide phospholipid physical mixture and andrographolide phospholipid compound in water， soybean oil and Lauroglycol FCC were compared and characterized with UV and DSC. RESULTS： The optimal preparation technology was tetrahydrofuran as reaction solvent， reaction time of 4 h， reaction temperature of 50 ℃， drug concentration of 10 mg/ml， ratio of andrographolide to phospholipid 1 ∶ 3. The compound rate of andrographolide phospholipid compound was 83.2％ （n＝3）. Compared with raw material and physical mixture， phospholipid compound significantly improved the dissolubility of andrographolide in water， soybean oil and Lauroglycol FCC. UV and DSC showed that compound had been prepared. CONCLUSIONS： Andrographolide phospholipid compound is prepared successfully. |
| 期刊： | 2016年第27卷第10期 |
| 作者： | 余凤玮，聂绩，袁野 |
| AUTHORS： | YU Fengwei，NIE Ji，YUAN Ye |
| 关键字： | 穿心莲内酯；磷脂复合物；制备；正交试验；表征 |
| KEYWORDS： | Andrographolide； Phospholipid compound； Preparation； Orthogonal test； Characterization |
| 阅读数： | 519 次 |
| 本月下载数： | 4 次 |
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