李红桥, 易涛. 膜乳化法制备盐酸小檗碱自乳化微球及其体外表征J. 药学学报, 2013,48(4): 554-559.
引用本文: 李红桥, 易涛. 膜乳化法制备盐酸小檗碱自乳化微球及其体外表征J. 药学学报, 2013,48(4): 554-559.
LI Hong-qiao, YI Tao. Preparation and in vitro characterization of berberine hydrochloride — self-emulsifying microsphere by membrane emulsification technologyJ. 药学学报, 2013,48(4): 554-559.
Citation: LI Hong-qiao, YI Tao. Preparation and in vitro characterization of berberine hydrochloride — self-emulsifying microsphere by membrane emulsification technologyJ. 药学学报, 2013,48(4): 554-559.

膜乳化法制备盐酸小檗碱自乳化微球及其体外表征

Preparation and in vitro characterization of berberine hydrochloride — self-emulsifying microsphere by membrane emulsification technology

  • 摘要:

    本文以难溶性药物盐酸小檗碱为模型药, 采用膜乳化法制备一种新型固体自乳化给药系统——自乳化微球。以溶解度和伪三元相图法, 筛选与优化液体自乳化给药系统处方。以海藻酸钠和氯化钙形成的凝胶为固体载体, 采用膜乳化法制备自乳化微球, 并对其进行体外表征。结果显示, 液体自乳化给药系统处方为: Capmul MCM/辛酸癸酸聚乙二醇甘油酯/聚氧乙烯醚-40氢化蓖麻油/1-2丙二醇为20323216。自乳化微球的平均粒径为10.92 μm, 包封率为32.57%; 遇水重分散后形成微乳的粒径为156.5 nm; 盐酸小檗碱在自乳化微球中为无定形态; 体外释药具有pH响应特性以上结果表明, 膜乳化法制备的自乳化微球为难溶性药物的口服给药提供了一种可能的新剂型。

     

    Abstract:

    This paper reports a new solid self-emulsifying drug delivery system self-emulsifying microsphere prepared by membrane emulsification technology with the hydrophobic berberine hydrochloride as a model drug.  Solubility test and pseudo-ternary phase diagram were employed to select the optimal prescription of liquid self-emulsifying drug delivery system.  The self-emulsifying microsphere was prepared by membrane emulsification technology with the solid carrier in a gel formed by sodium alginate and calcium chloride.  The results showed that the optimal prescription of liquid self-emulsifying drug delivery system was Capmul MCM/Cremophor RH40/Labrasol/1-2propanediol = 20323216.  The solid self-emulsifying microsphere had average diameter of 10.92 μm, encapsulation efficiency of 32.57% and the droplet size of reconstituted micromulsion of 156.5 nm.  Berberine hydrochloride was dispersed in microsphere in non-crystalline form.  In vitro release of the self-emulsifying microsphere showed pH response characteristics.  These results indicated that the self-emulsifying microsphere prepared by membrane emulsification technology might become a new dosage form for poorly water soluble drugs.

     

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