Use of porous aluminosilicate pellets for drug delivery
Use of porous aluminosilicate pellets for drug delivery
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DOI：
10.1080/02652040500100196
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发表时间：
2005-06-01
影响因子：
3.9
通讯作者：
Deasy, PB
中科院分区：
文献类型：
--
作者：
Byrne, RS;Deasy, PB
制备了三种多孔硅铝陶瓷球团，并对其作为缓释给药系统的潜力进行了评价。采用真空浸渍技术装药。载药液的浓度、陶瓷的孔隙度和容重等因素影响载药效果。由于药物被包裹在多孔的内部，药物从颗粒中释放的时间延长了。释药速度受微丸的孔隙结构和药物的理化性质的影响。采用挤压滚圆法制备类似多孔陶瓷的微球。颗粒配方包含铝硅酸盐粘土矿物（高岭土或高岭土），乙基纤维素100 cps，乙醇和不同数量的蔗糖。后两种成分起成孔剂的作用。将盐酸地尔硫卓装入微丸中，并延长其释放时间。释放速度可以通过改变初始配方中蔗糖的量来改变，因为蔗糖的量会影响颗粒的多孔微观结构。在以高岭土为基础的产品中，由于药物在高岭土微管中被包裹，释放进一步延长。采用低温球化法制备多孔高岭土基球团。这涉及到含有高岭土、硅酸钠溶液和十二烷基硫酸钠的水悬浮液的冷冻液滴。最终得到的颗粒被冷冻干燥，从而去除其中的冰，留下孔隙。微丸具有较长的释药时间，释药速度受微丸的孔隙结构和微气候pH的影响。
Three pelletized porous aluminosilicate ceramics were obtained commercially and their potential to act as extended release drug delivery systems was assessed. The pellets were drug loaded using a vacuum impregnation technique. Factors such as the concentration of the loading solution and the porosity and bulk density of the ceramic influenced the drug loading. The release of drug from the pellets was extended as the drug was entrapped within their porous interior. The rate of release was influenced by the porous microstructure of the pellets and the physicochemical properties of the drug. Extrusion-spheronization was used to prepare pellets similar to the porous ceramics. The pellet formulations contained an aluminosilicate clay mineral (kaolin or halloysite), ethylcellulose 100 cps, ethanol and varying quantities of sucrose. The latter two components acted as pore forming agents. Diltiazem HCl was loaded into the pellets and its release was extended. The release rate could be modified by changing the quantity of sucrose included in the initial formulation, as this influenced the porous microstructure of the pellets. In halloysite-based products the release was further extended due to entrapment of the drug within the halloysite microtubules. Porous kaolin-based pellets were also prepared by cryopelletization. This involved freezing droplets of an aqueous suspension containing kaolin, sodium silicate solution and sodium lauryl sulphate. The resulting pellets were freeze-dried, which removed ice from them to leave pores behind. The pellets gave extended drug release with the release rate being influenced by the porous microstructure of the pellets and their microclimate pH.