汤丽娟, 翁帼英. 三尖杉酯碱脂质体的制剂研究J. 药学学报, 1985, 20(6): 463-469.
引用本文: 汤丽娟, 翁帼英. 三尖杉酯碱脂质体的制剂研究J. 药学学报, 1985, 20(6): 463-469.
TANG Li-Juan, WENG Guo-Ying. PREPARATION AND STABILITY OF LIPOSOME-ASSOCIATED HARRINGTONINEJ. Acta Pharmaceutica Sinica, 1985, 20(6): 463-469.
Citation: TANG Li-Juan, WENG Guo-Ying. PREPARATION AND STABILITY OF LIPOSOME-ASSOCIATED HARRINGTONINEJ. Acta Pharmaceutica Sinica, 1985, 20(6): 463-469.

三尖杉酯碱脂质体的制剂研究

PREPARATION AND STABILITY OF LIPOSOME-ASSOCIATED HARRINGTONINE

  • 摘要: 本文探讨三尖杉酯碱脂质体的较佳制备方法。表明用转相蒸发法(REV)制备时影响三尖杉酯碱脂质体包裹率的因素与大多数水溶性药物脂质体的影响因素相同。提出并经实验证实,以稠厚型脂质体贮存可减少内包三尖杉酯碱的渗漏。实验还表明脂质体100℃30分钟灭菌和10℃以下贮存五个月,制品的结构、粒度和包裹率均无明显改变,溶血试验合格。但在40℃加速实验1至3个月制品产生溶血,此溶血与卵磷脂的氧化有明显相关性。

     

    Abstract: Harringtonine was incorporated into positively charged liposomes by using the REV (Reverse-phase-evaporation) method. It was shown that the percentage encapsulation of harringtonine in liposomes was greatly affected by ionic strength, evaporation temperature, lipid concentration and the amount of cholesterol. A thick harringtonine liposomal suspension with higher encapsulation and stability has been screened and devised. Its structure, size, percentage of encapsulation, degree of lipid oxidation and tendency to cause haemolysis were examined at 10℃ and 40℃. The suspension showed no change when stored at 10℃ for five months; after storage at 40℃ for one month a tendency to cause haemolysis was observed. After two months of storage some changes in size and structure were found. The results indicate that thick harringtonine liposomes are stable in physical and chemical properties under appropriate conditions (eg at 10℃ and under N2) in a limited time (five months).

     

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