奧沙利鉑脂質(zhì)體的制備及體外釋藥研究
發(fā)布時(shí)間：2018-08-02 14:54
【摘要】：目的制備一種包封率較高的奧沙利鉑脂質(zhì)體,并考察該脂質(zhì)體的體外性質(zhì)。方法采用多種方法制備奧沙利鉑脂質(zhì)體,通過(guò)單因素試驗(yàn)和正交試驗(yàn)最終確定脂質(zhì)體處方。采用高效液相色譜法檢測(cè)脂質(zhì)體包封率,Zeta Plus激光粒度分析儀測(cè)定脂質(zhì)體粒徑。同時(shí),采用高效液相色譜法、原子吸收光譜法兩種方法考察了該脂質(zhì)體的體外釋放情況。結(jié)果與薄膜分散法和p H梯度法相比,通過(guò)逆相蒸發(fā)法制備得到的了奧沙利鉑脂質(zhì)體包封率更高;在此基礎(chǔ)上進(jìn)行的處方篩選試驗(yàn)確定了最優(yōu)處方工藝為藥脂比1∶7.5,膽磷比1∶2,超聲功率195 W,超聲時(shí)間3 min;體外釋放試驗(yàn)結(jié)果表明,通過(guò)高效液相色譜法和原子吸收光譜法測(cè)定的奧沙利鉑脂質(zhì)體24 h的累計(jì)釋放率分別為25.0%和33.6%。結(jié)論通過(guò)逆相蒸發(fā)法制備得到的奧沙利鉑脂質(zhì)體包封率高,且具有較高的穩(wěn)定性和一定的緩釋作用。
[Abstract]:Aim to prepare oxaliplatin liposome with high entrapment efficiency and investigate its in vitro properties. Methods oxaliplatin liposomes were prepared by various methods. The formulation of oxaliplatin liposomes was determined by single factor test and orthogonal test. The particle size of liposome was determined by high performance liquid chromatography (HPLC) with Zeta Plus laser particle size analyzer. At the same time, the in vitro release of the liposome was investigated by high performance liquid chromatography (HPLC) and atomic absorption spectrometry (AAS). Results compared with thin film dispersion method and pH gradient method, the encapsulation efficiency of oxaliplatin liposomes prepared by inverse phase evaporation method was higher than that of thin film dispersion method and pH gradient method. On the basis of this, the optimum prescription conditions were determined as follows: ratio of drug to lipid 1: 7.5, ratio of bile to phosphorus 1: 2, ultrasonic power 195 W, ultrasonic time 3 min. The results of in vitro release test showed that: 1: 7. The cumulative release rates of oxaliplatin liposomes determined by HPLC and atomic absorption spectrometry for 24 h were 25.0% and 33.6%, respectively. Conclusion Oxaliplatin liposomes prepared by reverse phase evaporation have high entrapment efficiency, high stability and sustained release.
【作者單位】： 中國(guó)藥科大學(xué)藥學(xué)院藥劑學(xué)教研室;
【基金】：國(guó)家自然科學(xué)基金(No.81501579) 江蘇省自然科學(xué)基金(No.BK20150702) 江蘇高校優(yōu)勢(shì)學(xué)科建設(shè)工程資助項(xiàng)目
【分類(lèi)號(hào)】：R943
[Abstract]:Aim to prepare oxaliplatin liposome with high entrapment efficiency and investigate its in vitro properties. Methods oxaliplatin liposomes were prepared by various methods. The formulation of oxaliplatin liposomes was determined by single factor test and orthogonal test. The particle size of liposome was determined by high performance liquid chromatography (HPLC) with Zeta Plus laser particle size analyzer. At the same time, the in vitro release of the liposome was investigated by high performance liquid chromatography (HPLC) and atomic absorption spectrometry (AAS). Results compared with thin film dispersion method and pH gradient method, the encapsulation efficiency of oxaliplatin liposomes prepared by inverse phase evaporation method was higher than that of thin film dispersion method and pH gradient method. On the basis of this, the optimum prescription conditions were determined as follows: ratio of drug to lipid 1: 7.5, ratio of bile to phosphorus 1: 2, ultrasonic power 195 W, ultrasonic time 3 min. The results of in vitro release test showed that: 1: 7. The cumulative release rates of oxaliplatin liposomes determined by HPLC and atomic absorption spectrometry for 24 h were 25.0% and 33.6%, respectively. Conclusion Oxaliplatin liposomes prepared by reverse phase evaporation have high entrapment efficiency, high stability and sustained release.
【作者單位】： 中國(guó)藥科大學(xué)藥學(xué)院藥劑學(xué)教研室;
【基金】：國(guó)家自然科學(xué)基金(No.81501579) 江蘇省自然科學(xué)基金(No.BK20150702) 江蘇高校優(yōu)勢(shì)學(xué)科建設(shè)工程資助項(xiàng)目
【分類(lèi)號(hào)】：R943
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