| 水飞蓟素磷脂复合物的制备及体外溶出行为评价 |
| 投稿时间：2022-06-13 修订日期：2022-11-20 点此下载全文 |
| 引用本文：曾棋平,刘建清,杨丽娜,刘志宏,宋洪涛.水飞蓟素磷脂复合物的制备及体外溶出行为评价[J].药学实践杂志,2024,42(3):101~107 |
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| 基金项目:国家自然科学基金面上项目（81073064）；福建省自然科学基金（2015J01491） |
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| 中文摘要:目的 将水飞蓟素和磷脂复合以研制水飞蓟素磷脂复合物（silymarin phospholipids complex，SM-PC），并考察其基本理化性质。 方法 采用溶剂挥发法制备SM-PC。通过前期的单因素考察，选择脂药比、药物浓度以及反应温度作为星点设计-效应面法的考察因素，以SM-PC的复合率为衡量指标筛选最佳研制工艺，并测定SM-PC的体外溶出度。结果 SM-PC的最优制备条件如下：以丙酮为反应溶剂，水飞蓟素与大豆卵磷脂的比例为1∶1.8，反应温度56 ℃，反应物的浓度8.0 mg/ml。在此条件下制备3批样品得到SM-PC的复合率为（95.15±1.55）%，偏差<3%。体外溶出试验表明，SM-PC各组分在60 min的溶出接近90 %，主要成分水飞蓟宾的溶出行为与市售水飞蓟素胶囊相似，远高于原料药。结论 采用星点设计-效应面法成功制备SM-PC，明显提高了溶出度，为后续制剂的研究奠定基础。 |
| 中文关键词:水飞蓟素 磷脂复合物 溶剂挥发法 星点设计-效应面法 溶出 |
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| Preparation and in vitro dissolution behaviors evaluation of silymarin phospholipid complex |
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| Abstract:Objective To prepare silymarin phospholipids complex（SM-PC） and investigate its physicochemical properties. Methods On the basis of single-factor tests, the drug-lipid ratio, drug concentration and reaction temperature were selected as the factors of the central composite design and response surface methodology in the preparation of SM-PC by solvent volatilization, and the best process was optimized with the compound rate as the index. And its in vitro dissolution was measured. Results The optimum preparation technology of SM-PC was as follows: acetone was used as compound solvent, the concentration of SM was 8.0 mg/ml, the mass ratio of SM to phospholipid was 1∶1.8, the reaction temperature was 56 ℃ and the recombination rate was（95.15±1.55）% with deviation of less than 3%. The in vitro dissolution test showed that the dissolution of SM-PC was close to 90% in 60 min. The dissolution behavior of main component of silybin was similar to that of silymarin capsules（Legalon ®）, which was higher than SM-API. Conclusion SM-PC was successfully prepared by central composite design response surface method, which significantly improved the dissolution and laid a foundation for the study of subsequent preparations. |
| keywords:silymarin phospholipid complex solvent volatilization method central composite design and response surface methodology dissolution |
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