|
|||||
|
|
| 不同磷脂组成的莪术油包合物脂质体的药剂学性质与急性毒性研究 | |
| 引用本文： | 陈军,程娜娜,陆兔林,陈志鹏,严书霞,蔡宝昌.不同磷脂组成的莪术油包合物脂质体的药剂学性质与急性毒性研究[J].中成药,2012,34(4):645-650. |
| 作者姓名： | 陈军 程娜娜 陆兔林 陈志鹏 严书霞 蔡宝昌 |
| 作者单位： | 1. 南京中医药大学药学院,江苏南京210046;江苏省中药炮制重点实验室,江苏南京210029 2. 南京中医药大学药学院,江苏南京,210046 3. 江苏省中药炮制重点实验室,江苏南京,210029 |
| 基金项目： | 江苏省青蓝工程资助(2010);南京中医药大学引进人才启动项目(200802) |
| 摘 要： | 目的 比较不同磷脂组成对莪术油包合物脂质体药剂学性质以及急性毒性的影响.方法 采用饱和水溶液法制备莪术油-羟丙基-β-环糊精包合物并且冷冻干燥得到固体,乙醇注入法制备莪术油包合物脂质体.比较了使用大豆磷脂(SPC)或使用复合磷脂组成氢化大豆磷脂(HSPC)+大豆磷脂(SPC)]对制得的莪术油包合物脂质体的药剂学性质(包封率、粒径、电位、释放度、泄漏率等)的影响.并且进一步比较了莪术油溶液、莪术油包合物以及两种不同磷脂组成莪术油包合物脂质体的急性毒性.结果 添加10％ HSPC对莪术油包合物脂质体的包封率、粒径、电位等没有影响,但释放度和泄漏率实验结果表明莪术油HSPC+ SPC包合物脂质体的稳定性显著高于莪术油包合物SPC脂质体.莪术油溶液、莪术油环包合物,莪术油包合物SPC脂质体和莪术油包合物HSPC+ SPC脂质体静脉注射后的LD50分别为207.87、153.31、269.13和327.30 mg/kg.结论 应用复合磷脂组成(HSPC+ SPC)可以显著提高莪术油包合物脂质体的稳定性和安全性. |
| 关 键 词： | 莪术油 包合物脂质体 稳定性 氢化大豆磷脂 大豆磷脂 急性毒性 |
Effect of phospholipid composition on pharmaceutical property and acute toxicity of liposomes entrapped zedoary turmeric oil and its inclusion |
|
| CHEN Jun , CHENG Na-na , LU Tu-lin , CHEN Zhi-peng , YAN Shu-xia , CAI Bao-chang.Effect of phospholipid composition on pharmaceutical property and acute toxicity of liposomes entrapped zedoary turmeric oil and its inclusion[J].Chinese Traditional Patent Medicine,2012,34(4):645-650. | |
| Authors: | CHEN Jun CHENG Na-na LU Tu-lin CHEN Zhi-peng YAN Shu-xia CAI Bao-chang |
| Institution: | 1.College of Pharmacy,Nanjing University of Chinese Medicine,Nanjing 210046,China;2.Jiangsu Provincial Key Laboratory of Chinese Medicine Processing,Nanjing 210029,China) |
| Abstract: | AIM To compare the effect of phospholipid composition on pharmaceutical characteristics and acute toxicity of liposomes containing zedoary turmeric oil(ZTO) and ZTO hydroxypropyl-β-cyclodextrin inclusion complex(ZTO-CD).METHODS ZTO-CD was prepared by saturated water solution method and obtained by freeze-drying technique.The liposomes were prepared by ethanol injection method and used to encapsulate ZTO-CD into liposomes.Pharmaceutical characteristics such as entrapment efficiency,size,zeta potential,release profiles and stability were determined and compared between ZTO-CD-loaded liposomes with different phospholipid composition(SPC or HSPC+SPC).Acute toxicity of ZTO solution,ZTO-CD and ZTO-CD-loaded liposomes with different phospholipid composition was also compared.RESULTS ZTO-CD-loaded HSPC+SPC liposomes had the similar entrapment efficiency,size and zeta potential compared with the corresponding SPC liposomes.But the results of release profiles and leakage experiments revealed that the stability of ZTO-CD-loaded HSPC+SPC liposomes was significantly higher than that of SPC lipsomes.The LD50 values of ZTO solution,ZTO-CD,ZTO-CD-loaded SPC liposomes and ZTO-CD-loaded HSPC+SPC liposomes were 207.87,153.31,269.13 and 327.30 mg/kg following intravenous administration,respectively.CONCLUSION As to the carrier of ZTO,liposomes composed of both HSPC and SPC possess good stability and safety compared with conventional SPC liposomes. |
| Keywords: | zedoary turmeric oil inclusion complex-in-liposome stability hydrogenated soybean phosphatidylcholine soybean phosphatidylcholine acute toxicity |
| 本文献已被 CNKI 万方数据 等数据库收录！ | |