黑龙江医药
黑龍江醫藥
흑룡강의약
HEILONGJIANG MEDICAL JOURNAL
2015年
2期
275-277
,共3页
依托泊苷%前体脂质体%长循环热敏脂质体
依託泊苷%前體脂質體%長循環熱敏脂質體
의탁박감%전체지질체%장순배열민지질체
Etoposide%long-circulating thermosensitive liposomes%proliposomes
目的：对依托泊苷（Etoposide，VP-16）长循环热敏前体脂质体的制备工艺进行研究，并对该制备工艺进行方法学及制剂质量考察。方法：应用薄膜分散法制成VP-16长循环热敏脂质体，进一步借助冷冻干燥技术进行依托泊苷长循环热敏前体脂质体的制备；采用zeta电势测定仪及HPLC等技术进行方法学考察，主要包括脂质体的包封率、粒径、载药量、电位、释放度、稳定性。结果：VP-16长循环热敏前体脂质体水合形成长循环热敏脂质体，粒径为(105.2±3.4) nm，Zeta电位为(-11.9±1.7)mV，包封率可达96.8%；该脂质体在相变温度42℃下药物释放达到96%以上。结论：VP-16长循环热敏前体脂质体的制备工艺稳定，脂质体载药量大，包封率高；药物含量及包封率的测定方法简单、快速而准确，因而，该研究可为VP-16开发成静脉注射用新制剂提供数据支持。
目的：對依託泊苷（Etoposide，VP-16）長循環熱敏前體脂質體的製備工藝進行研究，併對該製備工藝進行方法學及製劑質量攷察。方法：應用薄膜分散法製成VP-16長循環熱敏脂質體，進一步藉助冷凍榦燥技術進行依託泊苷長循環熱敏前體脂質體的製備；採用zeta電勢測定儀及HPLC等技術進行方法學攷察，主要包括脂質體的包封率、粒徑、載藥量、電位、釋放度、穩定性。結果：VP-16長循環熱敏前體脂質體水閤形成長循環熱敏脂質體，粒徑為(105.2±3.4) nm，Zeta電位為(-11.9±1.7)mV，包封率可達96.8%；該脂質體在相變溫度42℃下藥物釋放達到96%以上。結論：VP-16長循環熱敏前體脂質體的製備工藝穩定，脂質體載藥量大，包封率高；藥物含量及包封率的測定方法簡單、快速而準確，因而，該研究可為VP-16開髮成靜脈註射用新製劑提供數據支持。
목적：대의탁박감（Etoposide，VP-16）장순배열민전체지질체적제비공예진행연구，병대해제비공예진행방법학급제제질량고찰。방법：응용박막분산법제성VP-16장순배열민지질체，진일보차조냉동간조기술진행의탁박감장순배열민전체지질체적제비；채용zeta전세측정의급HPLC등기술진행방법학고찰，주요포괄지질체적포봉솔、립경、재약량、전위、석방도、은정성。결과：VP-16장순배열민전체지질체수합형성장순배열민지질체，립경위(105.2±3.4) nm，Zeta전위위(-11.9±1.7)mV，포봉솔가체96.8%；해지질체재상변온도42℃하약물석방체도96%이상。결론：VP-16장순배열민전체지질체적제비공예은정，지질체재약량대，포봉솔고；약물함량급포봉솔적측정방법간단、쾌속이준학，인이，해연구가위VP-16개발성정맥주사용신제제제공수거지지。
Objective:Study on the preparation technology of Etoposide (VP-16) long-circulating thermo-sensitive proliposomes and investigate its methodology. Methods:Film dispersion method was used to prepare VP-16 long-circulating thermo-sensitive li-posomes which were further prepared as VP-16 long-circulating proliposomes by vacuum freeze-drying technique. The shape and size distribution of proliposomes were detected by transmission electron Zetasizer, and the content of VP-16 was determined by HPLC. The encapsulation efficiency (EE) and the release rate of liposome were computed as well. Results:The VP-16 long-circulating ther-mo-sensitive liposomes aquated as the Etoposide long-circulating proliposomes, the appearance of liposomes was whole round, distri-bution uniform, the mean particle size were (105.2±3.4) nm, and zeta potential were (-11.9±1.7) mV. The liposome 42℃tempera-ture under the drug release above 96%. Conclusion:The preparation technology of Etoposide long-circulating thermo-sensitive proli-posomes was stable, drug loading and entrapping capacity of liposomes were well. The methods for determination of Etoposide content and entrapment efficiency were simple, rapid and accurate. These studies can provide bases for further developing VP-16 as ther-mo-sensitive liposomes intravenous injection.
