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目的制备硫酸长春新碱(vincristine,VCR)热敏脂质体,测定其粒径及体外释药热敏特性,建立脂质体含量、包封率及有关物质的测定方法。方法 pH梯度主动载药法制备长春新碱热敏脂质体,激光粒度分析仪测定脂质体粒径;以水为释放介质,分别考察脂质体在37和42℃的释放特性;超滤离心法测定脂质体包封率;HPLC测定脂质体中长春新碱的含量及有关物质。结果长春新碱热敏脂质体的平均粒径为(86±6)nm,37℃几乎不释放,42℃30 min内释放约90%;3批样品包封率均高于95%;含量为1.92 mg·mL-1,有关物质符合药典要求。结论长春新碱长循环热敏脂质体的制备工艺简单稳定,所制备的脂质体粒径均一,具有明显的热敏特性,包封率高,适于-20℃长期储存。脂质体含量、包封率及有关物质测定方法简便、快速、准确。
OBJECTIVE: To prepare vincristine sulfate (VCR) thermosensitive liposomes, determine its particle size and in vitro thermal release characteristics, and to establish a method for the determination of liposome content, entrapment efficiency and related substances. Methods Vincristine thermosensitive liposomes were prepared by pH gradient active drug loading method. The particle size of liposomes was determined by laser particle size analyzer. The release characteristics of liposomes at 37 and 42 ℃ were investigated with water as the release medium. The entrapment efficiency of liposomes was determined by centrifugation. The contents of vincristine in liposomes and related substances were determined by HPLC. Results The average particle size of vincristine thermosensitive liposomes was (86 ± 6) nm, almost not released at 37 ℃ and 90% at 42 ℃ for 30 min. The entrapment efficiencies of vincristine were higher than 95% 1.92 mg · mL-1, the relevant substances meet the pharmacopoeia requirements. Conclusion The preparation method of vincristine long-circulating thermosensitive liposomes is simple and stable. The prepared liposomes have uniform particle size, obvious thermal sensitivity and high entrapment efficiency, suitable for long-term storage at -20 ℃. Determination of liposome content, entrapment efficiency and related substances is simple, rapid and accurate.