医药导报
醫藥導報
의약도보
HERALD OF MEDICINE
2014年
11期
1486-1490
,共5页
李志平%赵希青%赵诗情%张慧%刘燕%肖若蕾
李誌平%趙希青%趙詩情%張慧%劉燕%肖若蕾
리지평%조희청%조시정%장혜%류연%초약뢰
紫杉醇热敏脂质体%溶血性%色谱法,高效液相%质量控制
紫杉醇熱敏脂質體%溶血性%色譜法,高效液相%質量控製
자삼순열민지질체%용혈성%색보법,고효액상%질량공제
Thermo-sensitive liposomes with paclitaxel%Haemolysis%HPLC%Quantity control
目的：制备紫杉醇热敏脂质体，建立测定其含量、有关物质及溶血磷脂的方法，考察其含量、有关物质、溶血磷脂量以及体外溶血性。方法采用高效液相色谱（ HPLC）-紫外法检测制剂含量及有关物质，HPLC-电雾式检测器检测制剂中溶血磷脂单棕榈酰磷脂酰胆碱的量，并对检测方法进行验证；分光光度法测定体外溶血百分率。结果紫杉醇在60.39~181.17μg·mL-1范围内峰面积与浓度线性关系良好，回收率及精密度实验均符合要求；有关物质测定方法专属性、灵敏度和系统适用性均符合要求；溶血磷脂测定方法的专属性和灵敏度符合有关规定，在1.5~50.0μg·mL-1范围内峰面积与浓度线性关系良好，回收率、重复性均符合要求；3批自制紫杉醇热敏脂质体的含量在90.0%~110.0%之间，单个杂质含量均〈0.5%，总杂质含量均〈2.0%，体外基本不引起溶血。结论含量、有关物质及溶血磷脂检测方法均可用于紫杉醇热敏脂质体的质量评价，自制紫杉醇热敏脂质体各项指标均符合要求，且质量稳定。
目的：製備紫杉醇熱敏脂質體，建立測定其含量、有關物質及溶血燐脂的方法，攷察其含量、有關物質、溶血燐脂量以及體外溶血性。方法採用高效液相色譜（ HPLC）-紫外法檢測製劑含量及有關物質，HPLC-電霧式檢測器檢測製劑中溶血燐脂單棕櫚酰燐脂酰膽堿的量，併對檢測方法進行驗證；分光光度法測定體外溶血百分率。結果紫杉醇在60.39~181.17μg·mL-1範圍內峰麵積與濃度線性關繫良好，迴收率及精密度實驗均符閤要求；有關物質測定方法專屬性、靈敏度和繫統適用性均符閤要求；溶血燐脂測定方法的專屬性和靈敏度符閤有關規定，在1.5~50.0μg·mL-1範圍內峰麵積與濃度線性關繫良好，迴收率、重複性均符閤要求；3批自製紫杉醇熱敏脂質體的含量在90.0%~110.0%之間，單箇雜質含量均〈0.5%，總雜質含量均〈2.0%，體外基本不引起溶血。結論含量、有關物質及溶血燐脂檢測方法均可用于紫杉醇熱敏脂質體的質量評價，自製紫杉醇熱敏脂質體各項指標均符閤要求，且質量穩定。
목적：제비자삼순열민지질체，건립측정기함량、유관물질급용혈린지적방법，고찰기함량、유관물질、용혈린지량이급체외용혈성。방법채용고효액상색보（ HPLC）-자외법검측제제함량급유관물질，HPLC-전무식검측기검측제제중용혈린지단종려선린지선담감적량，병대검측방법진행험증；분광광도법측정체외용혈백분솔。결과자삼순재60.39~181.17μg·mL-1범위내봉면적여농도선성관계량호，회수솔급정밀도실험균부합요구；유관물질측정방법전속성、령민도화계통괄용성균부합요구；용혈린지측정방법적전속성화령민도부합유관규정，재1.5~50.0μg·mL-1범위내봉면적여농도선성관계량호，회수솔、중복성균부합요구；3비자제자삼순열민지질체적함량재90.0%~110.0%지간，단개잡질함량균〈0.5%，총잡질함량균〈2.0%，체외기본불인기용혈。결론함량、유관물질급용혈린지검측방법균가용우자삼순열민지질체적질량평개，자제자삼순열민지질체각항지표균부합요구，차질량은정。
Objective To prepare long-circulating temperature-sensitive liposomes with paclitaxel( LTSLP ),develop methods for determination of paclitaxel,related substances and monostearoyl phosphatidylcholine( MSPC ) in LTSLP,and the haemolysis of LTSLP in vitro. Methods HPLC-UV methods for paclitaxel content and related substances and HPLC-CAD method for MSPC in LTSLP were established and validated. Spectrophotometric method was used to determine hemolysis in vitro. Results There was a good linear relationship between peak area and concentration within the range of 60. 39-181. 17μg·mL-1 . Recovery and precision of the method for determination of paclitaxel content met the requirements. Specificity,sensitivity,and system suitability for related substances were consistent with requirements. There was a good linear relationship between peak area and concentration within the range of 1. 5-50. 0μg·mL-1 for the determination of MSPC with good specificity,sensitivity and recovery. Paclitaxel contents in three batches of self-prepared LTSLP were between 90. 0% and 110. 0%,single related substances were below 0. 5% and total impurities were below 2. 0%. There was almost no hemolysis in vitro. Conclusion The methods for determining paclitaxel content,related substances and haemolysis can be used to assess the quality of LTSLP. Self-produced LTSLP consistently meet the quality standards.
