中国药师
中國藥師
중국약사
CHINA PHARMACIST
2015年
8期
1290-1294
,共5页
辛伐他汀%纳米结构脂质载体%热熔乳化超声-低温固化法
辛伐他汀%納米結構脂質載體%熱鎔乳化超聲-低溫固化法
신벌타정%납미결구지질재체%열용유화초성-저온고화법
Simvastatin%Nanostructured lipid carriers%Melt-emulsion ultrasonication and low temperature-solidification method
目的：：制备辛伐他汀纳米结构脂质载体(辛伐他汀-NLCs )。方法：采用热熔乳化超声-低温固化法制备辛伐他汀-NLCs,以辛伐他汀-NLCs粒径分布、多聚分散系数( PdI)、包封率和载药量为评价指标,考察了制备辛伐他汀-NLCs的固体与液体脂质比例、脂质浓度、表面活性剂与助表面活性剂比例、乳化剂浓度、药物浓度等处方因素,并对制得的最优辛伐他汀-NLCs处方进行表征；考察辛伐他汀-NLCs的体外释药行为及稳定性。结果：辛伐他汀-NLCs的最优处方为：辛伐他汀浓度为0.5%,鲸蜡醇棕榈酸酯浓度为1.5%,辛酸/癸酸甘油酯浓度为4.5%,大豆卵磷脂浓度为2.5%,聚乙二醇-12-羟基硬脂酸酯浓度为1.5%；制得的3批辛伐他汀-NLCs平均粒径为(102.2±42.1)nm,PdI为(0.201±0.023),Zeta电位为(-33.1±4.1)mV,透射电镜显示成圆整、规则球形,24 h累计释放度为(59.1±4.8)%；稳定性研究显示,辛伐他汀-NLCs在5℃条件下放置3个月稳定。结论：该处方可用于辛伐他汀-NLCs的制备,工艺可行。
目的：：製備辛伐他汀納米結構脂質載體(辛伐他汀-NLCs )。方法：採用熱鎔乳化超聲-低溫固化法製備辛伐他汀-NLCs,以辛伐他汀-NLCs粒徑分佈、多聚分散繫數( PdI)、包封率和載藥量為評價指標,攷察瞭製備辛伐他汀-NLCs的固體與液體脂質比例、脂質濃度、錶麵活性劑與助錶麵活性劑比例、乳化劑濃度、藥物濃度等處方因素,併對製得的最優辛伐他汀-NLCs處方進行錶徵；攷察辛伐他汀-NLCs的體外釋藥行為及穩定性。結果：辛伐他汀-NLCs的最優處方為：辛伐他汀濃度為0.5%,鯨蠟醇棕櫚痠酯濃度為1.5%,辛痠/癸痠甘油酯濃度為4.5%,大豆卵燐脂濃度為2.5%,聚乙二醇-12-羥基硬脂痠酯濃度為1.5%；製得的3批辛伐他汀-NLCs平均粒徑為(102.2±42.1)nm,PdI為(0.201±0.023),Zeta電位為(-33.1±4.1)mV,透射電鏡顯示成圓整、規則毬形,24 h纍計釋放度為(59.1±4.8)%；穩定性研究顯示,辛伐他汀-NLCs在5℃條件下放置3箇月穩定。結論：該處方可用于辛伐他汀-NLCs的製備,工藝可行。
목적：：제비신벌타정납미결구지질재체(신벌타정-NLCs )。방법：채용열용유화초성-저온고화법제비신벌타정-NLCs,이신벌타정-NLCs립경분포、다취분산계수( PdI)、포봉솔화재약량위평개지표,고찰료제비신벌타정-NLCs적고체여액체지질비례、지질농도、표면활성제여조표면활성제비례、유화제농도、약물농도등처방인소,병대제득적최우신벌타정-NLCs처방진행표정；고찰신벌타정-NLCs적체외석약행위급은정성。결과：신벌타정-NLCs적최우처방위：신벌타정농도위0.5%,경사순종려산지농도위1.5%,신산/계산감유지농도위4.5%,대두란린지농도위2.5%,취을이순-12-간기경지산지농도위1.5%；제득적3비신벌타정-NLCs평균립경위(102.2±42.1)nm,PdI위(0.201±0.023),Zeta전위위(-33.1±4.1)mV,투사전경현시성원정、규칙구형,24 h루계석방도위(59.1±4.8)%；은정성연구현시,신벌타정-NLCs재5℃조건하방치3개월은정。결론：해처방가용우신벌타정-NLCs적제비,공예가행。
To prepare simvastatin nanostructured lipid carriers ( simvastatin-NLCs) . Methods:The simvastatin-NLCs were prepared by melt-emulsion ultrasonication and low temperature-solidification methods. Using the particle size, polydispersion in-dex, encapsulation efficiency and drug loading as the idices, the ratio of solid to liquid, lipid concentration, ratio of surfactant to cosur-factant, emulsifier concentration and drug concentration were optimized. The optimized simvastatin-NLCs were characterized for the en-capsulation efficiency, particle size, zeta potential and morphology. In vitro drug release behavior and stability of NLCs were also stud-ied. Results:The optimized simvastatin-NLCs formula was as follows:the concentration of simvastatin, cetyl palmitate, Miglyol? 812, soy lecithin and solutol HS15? was 0. 5%, 1. 5%, 4. 5%, 2. 5% and 1. 5%, respectively. The particle size and zeta potential of NLCs was (102. 2 ± 42. 1) nm and ( -33. 1 ± 4. 1) mV, respectively. The simvastatin-NLCs were found to be small and spherical with smooth surface under a transmission electron microscope. The in vitro release profile indicated that the accumulated release of sim-vastatin reached up to (59. 1 ± 4. 8) % in 24 h. The stability studies showed that simvastatin-NLCs were stable in 3 months after stored at 5℃. Conclusion:The formula of simvastatin-NLCs prepared by melt-emulsion ultrasonication and low temperature-solidifica-tion method is feasible.
