本文選題：阿維拉霉素 + 自微乳化　； 參考：《中國(guó)藥學(xué)雜志》2017年20期

【摘要】：目的采用星點(diǎn)設(shè)計(jì)-效應(yīng)面法優(yōu)化阿維拉霉素自微乳化給藥系統(tǒng)(SMEDDS),并進(jìn)行質(zhì)量評(píng)定。方法測(cè)定阿維拉霉素在各輔料中的溶解度,通過(guò)三相配伍實(shí)驗(yàn)篩選自微乳化基質(zhì);以微乳粒徑、Zeta電位和分散系數(shù)(PDI)作為效應(yīng)值,應(yīng)用Design Expert進(jìn)行處方優(yōu)化,并對(duì)阿維拉霉素自微乳制劑進(jìn)行穩(wěn)定性、釋放度及抑菌活性考察。結(jié)果通過(guò)星點(diǎn)效應(yīng)面優(yōu)化獲得阿維拉霉素自微乳的處方:丙二醇月桂酸酯(36.67%)、聚氧乙烯氫化蓖麻油(42.83%)、二乙二醇乙醚(20.50%),載藥量為2%。將自微乳濃縮液加水乳化后粒徑為(28.34±0.06)nm,Zeta電位為(-1.98±0.24)mV,PDI為(0.15±0.005),并具有較好的體外抑菌活性。結(jié)論成功制備了阿維拉霉素SMEDDS,質(zhì)量穩(wěn)定,可顯著改善阿維拉霉素的溶出度,有望提高阿維拉霉素動(dòng)物體內(nèi)口服生物利用度。
[Abstract]:Objective to optimize the self-emulsifying drug delivery system (SMEDs) of Avila mycin by star design-effect surface method and evaluate its quality. Methods the solubility of Avila in various excipients was determined, the self-emulsified matrix was selected by three-phase compatibility experiment, and the formulation was optimized by using the particle size, Zeta potential and dispersion coefficient of microemulsion as effect values. The stability, release and bacteriostatic activity of Avila-mycin self-emulsion were investigated. Results the formulation of Avila mycin self-microemulsion was obtained by star effect surface optimization: propanediol lauric acid ester (36.67%), polyoxyethylene hydrogenated castor oil (42.83%), diethylene glycol ether (20.50%). The particle size of self-microemulsion concentrate was (28.34 鹵0.06) nm Zeta potential (-1.98 鹵0.24) MV, PDI was (0.15 鹵0.005), and it had better bacteriostatic activity in vitro. Conclusion the Avila mycin SMEDDSs were prepared successfully, and the quality was stable, the dissolution of Avila was improved significantly, and the bioavailability of Avila mycin was expected to be increased in vivo.
【作者單位】： 浙江工商大學(xué)食品與生物工程學(xué)院;
【基金】：浙江省新苗人才計(jì)劃資助項(xiàng)目(2014R408085)
【分類(lèi)號(hào)】：R943

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