脂质和液体药物制剂多孔二氧化硅载体的比较评价

Y. Choudhari, U. Reddy, F. Monsuur, T. Pauly, H. Hoefer, W. McCarthy
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引用次数: 26

摘要

将液体和半固体脂质转化为自由流动的粉末是一种有利的技术,因为这种载体具有比表面积大、吸附能力强、易于加工、能够生成载脂的自由流动粉末的能力,这些粉末可以转化为片剂和胶囊等固体剂型。在选择合适的吸附剂时,密度、吸附能力和解吸能力三者的结合是很重要的。采用汞侵入法对镁铝硅酸盐(MAS)、气相颗粒二氧化硅(GFS)和介孔硅胶(MSG)等吸附剂的流动性能、粒径、扫描电镜(SEM)和孔隙结构进行了表征。扫描电镜结果显示了吸附剂的形态,而侵入-挤压研究显示了孔径分布。采用常规方法制备了载油吸附剂片剂和胶囊剂。评价了载油吸附剂将油转化为粉末的能力,易加工成片剂和胶囊,以及载油(维生素E)或活性(格列本脲)的释放。所有吸附剂均具有良好的流动性能,其中MSG的密度高于GFS和MAS。这有助于提供每单位容量的最大活动。与MSG和GFS相比,MAS的孔径分布更宽。MAS在粉末及其配方中表现出较差的油脂释放,而GFS则表现出与MSG非常相似的释放。味精的含油量最高可达70%,以片剂形式给药,而味精的高密度使其在有限体积的胶囊中给药量最高。因此,MAS较低的密度和较差的油脂释放限制了其在固体口服给药中的应用,而MSG和GFS被证明是合适的。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Comparative evaluation of porous silica based carriers for lipids and liquid drug formulations
Abstract Conversion of liquid and semisolid lipids into free flowing powders is an advantageous technique, as the carriers display high surface area, strong adsorption capacity, ease of processing, and ability to generate lipid loaded free flowing powders which can be converted to solid dosage forms like tablets and capsules. A combination of density, adsorption capacity and desorption is found to be of importance in the selection of the right adsorbent. Adsorbents like magnesium aluminium silicates (MAS), granulated fumed silica (GFS) and mesoporous silica gel (MSG) were characterized by flow property measurements, particle size, scanning electron microscopy (SEM) and pore structure by mercury (Hg) intrusion study. SEM results reveal adsorbent morphology, whereas an intrusion-extrusion study reveal pore size distributions. Tablets and capsules of oil loaded adsorbents were prepared by conventional methods. Oil loaded adsorbents were evaluated for the ability to convert oil into powder, easy of processing into tablets and capsules, and release of the loaded oil (Vitamin E) or active (Glyburide). All adsorbents possess good flow property while MSG has higher density than GFS and MAS. This helps to deliver maximum active per unit volume. A wider pore size distribution of MAS was observed in comparison to MSG and GFS. MAS exhibited poor oil release from powder and its formulations, whereas GFS demonstrated closely similar release to MSG. Maximum 70% oil loaded MSG can be delivered in tablet dosage form andMSG can deliver the highest amount in limited volume capsules due to its high density. Hence, lower density and poor oil release from MAS limit its applications in solid oral drug delivery,while both MSG and GFS proved to be suitable.
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