本文關(guān)鍵詞： 糖酯 醇質(zhì)體 脂質(zhì)體 穩(wěn)定性 高速逆流色譜　出處：《浙江工商大學(xué)》2015年碩士論文　論文類型：學(xué)位論文

【摘要】：隨著納米技術(shù)和藥物控釋系統(tǒng)的發(fā)展,磷脂型納米載藥體系成為近年來研究的熱點。但該體系容易發(fā)生聚沉、氧化分解、藥物泄漏等,其穩(wěn)定性差一直是發(fā)展中亟待解決的問題。目前,應(yīng)用于磷脂型納米體系的穩(wěn)定劑主要有吐溫、聚乙二醇等系列,效果一般。糖酯類化合物作為綠色、安全的兩親性非離子型表面活性劑,已廣泛應(yīng)用于食品、化妝品和醫(yī)藥領(lǐng)域中。研究表明,糖酯還能影響藥物的溶解、吸收和滲透性能,大大提高藥物生物利用度。另外,某些糖酯類化合物本身具有保濕滋潤、消炎抗氧化等藥理學(xué)功效。 本文采用高速逆流色譜(HSCCC-D15000)和柱色譜聯(lián)用法成功地從南瓜粉提取物中分離制備了二半乳糖酯、三半乳糖酯和四半乳糖酯；通過進(jìn)行兩次高速逆流色譜(HSCCC-D1200)分別將商品蔗糖酯SE-13分離純化為蔗糖單酯、蔗糖二酯和蔗糖多酯。采用薄膜超聲法制備了醇質(zhì)體和脂質(zhì)體,將分離制備的糖酯類化合物作為穩(wěn)定劑加入醇質(zhì)體和脂質(zhì)體這兩種典型的磷脂型納米體系中,通過直接觀察法和透射電鏡(TEM)法觀察其宏、微觀形態(tài),馬爾文粒度電位儀測定其粒徑、多分散系數(shù)(PDI)和Zeta電位,高效液相色譜(HPLC)法測定其藥物包封率,以及在4℃下貯存1、3、6個月后觀察和測定各參數(shù)的變化,研究不同糖基數(shù)的半乳糖酯和不同酯化程度的蔗糖酯對磷脂型納米體系穩(wěn)定性的影響。結(jié)果表明：(1)蔗糖酯和半乳糖酯都能一定程度地提高醇質(zhì)體的穩(wěn)定性。另外,其穩(wěn)定性隨著蔗糖酯酯化程度的增加以及半乳糖酯糖基數(shù)目的增加而提高。綜合比較分析,蔗糖多酯提高醇質(zhì)體穩(wěn)定性的效果比半乳糖酯好。所制備的蔗糖多酯-醇質(zhì)體粒徑為62.0±4.3nm,Zeta電位為-72.3±4.5mV,在貯存6個月后體系依然澄清透明,各參數(shù)變化不大。(2)蔗糖酯同樣能夠提高脂質(zhì)體的穩(wěn)定性,其中蔗糖多酯提高脂質(zhì)體的穩(wěn)定性效果優(yōu)于其他蔗糖酯。所制備的蔗糖多酯-脂質(zhì)體粒徑為84.0±4.2nm,Zeta電位為-52.4±3.4mV,在貯存6個月后體系依然澄清透明,各參數(shù)變化不大。 綜上所述,糖酯是一種極具潛力的磷脂型納米體系穩(wěn)定劑。
[Abstract]:With the development of nanotechnology and drug controlled release system, phospholipid nano-drug delivery system has become a hot topic in recent years. However, the system is prone to coalescence, oxidative decomposition, drug leakage and so on. At present, the stabilizers used in phospholipid nanosystems are mainly Tween, polyethylene glycol and other series, the effect is general. Sugar and ester compounds as green. Safe amphiphilic Nonionic surfactants have been widely used in the fields of food, cosmetics and medicine. Studies have shown that carbohydrates can also affect the dissolution, absorption and permeability of drugs. In addition, some sugar and ester compounds themselves have moisturizing, anti-inflammatory, anti-oxidation and other pharmacological effects. In this paper, high speed countercurrent chromatography (HSCCC-D15000) and column chromatography were used to separate and prepare digalactyl ester, trigalactose ester and tetragalactose ester from pumpkin powder extract. The commercial sucrose ester (SE-13) was separated and purified to sucrose monoester by two high speed countercurrent chromatography (HSCCC-D1200). Sucrose diesters and sucrose polyesters were prepared by thin-film ultrasonic method. The glycosylates and liposomes were added to the two typical phospholipid nanosystems as stabilizers. The macroscopical and microscopic morphology were observed by means of direct observation and transmission electron microscopy (TEM). The particle size, polydispersity coefficient (PDI) and Zeta potential were measured by Ma Erwen particle size potentiometer. High performance liquid chromatography (HPLC) HPLC method was used to determine the drug encapsulation efficiency, and the changes of the parameters were observed and determined after storage at 4 鈩，

本文編號：1467325