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首页> 外文期刊>International Journal of Pharmaceutics >Preparation of silymarin proliposome: a new way to increase oral bioavailability of silymarin in beagle dogs.
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Preparation of silymarin proliposome: a new way to increase oral bioavailability of silymarin in beagle dogs.

机译:水飞蓟素脂质体的制备:增加水飞蓟素在比格犬中口服生物利用度的新方法。

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The aim of the present study was to find a method to increase oral bioavailability of silymarin, that is to say, by the preparation of silymarin proliposome and to compare the pharmacokinetic characteristics and bioavailability after oral administration of silymarin proliposome and silymarin in beagle dogs. Silymarin proliposome was prepared by the film-deposition on carriers. After the proliposome was contacted with water, the silymarin liposome suspensions formed automatically. The tests of physicochemical properties including SEM, TEM, encapsulation efficiency, dissolution studies, particle size of the reconstituted liposome and stability of the silymarin proliposome were determined by laser-particle-sizer, HPLC, etc. The concentrations of silymarin in plasma of beagle dogs and its pharmacokinetic behaviors after oral administration of silymarin liposome suspensions and silymarin were studied by RP-HPLC. The pharmacokinetic parameters were computed by software program 3p97. The encapsulation efficiency of silymarin liposome could be more than 90%, with an average particle size of about 196.4 nm and the proliposome appeared a very stability at 40 degrees C during 3 months. It was found that mean plasma concentration-time curves of silymarin after oral administration of liposome suspensions and silymarin in beagle dogs were both in accordance with open two-compartments model and first-order absorption. Pharmacokinetic parameters of silymarin proliposome and silymarin in beagle dogs were Tmax both 30 min; Cmax 472.62 and 89.78 ng mL(-1); and AUC0-infinity 2606.21 and 697 ng mL(-1)h, respectively. The high bioavailability of silymarin proliposome could be obtained by oral administration. Silymarin proliposome was stable and did enchance the gastrointestinal absorption of silymarin.
机译:本研究的目的是找到一种提高水飞蓟素口服生物利用度的方法,也就是说,通过制备水飞蓟素前脂质体,并比较水飞蓟素脂质体和水飞蓟素在比格犬中口服后的药代动力学特征和生物利用度。水飞蓟素脂质体通过在载体上的膜沉积来制备。前脂质体与水接触后,水飞蓟素脂质体悬浮液会自动形成。通过激光粒度仪,HPLC等方法测定了SEM,TEM,包封效率,溶出度研究,重构脂质体的粒径和水飞蓟素原脂质体的稳定性等理化性质测试。比格犬血浆中水飞蓟素的浓度RP-HPLC研究了水飞蓟素脂质体悬浮液和水飞蓟素口服后的药代动力学行为。通过软件程序3p97计算药代动力学参数。水飞蓟素脂质体的包封率可能超过90%,平均粒径约为196.4 nm,并且前脂质体在40℃下3个月内表现出非常稳定的稳定性。结果发现,比格犬口服脂质体悬浮液和水飞蓟素后,水飞蓟素的平均血浆浓度-时间曲线均符合开放式二室模型和一级吸收。水飞蓟素脂质体和水飞蓟素在比格犬中的药代动力学参数均为Tmax均为30分钟。 Cmax 472.62和89.78 ng mL(-1);和AUC0-infinity 2606.21和697 ng mL(-1)h。水飞蓟素脂质体的高生物利用度可通过口服给药获得。水飞蓟素脂质体稳定并且确实增强了水飞蓟素在胃肠道的吸收。

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