Maejima T, Osawa T, Nakajima K, Kobayashi M
Pharmaceutics Research Laboratory, Tanabe Seiyaku Co., Ltd., Osaka, Japan.
Chem Pharm Bull (Tokyo). 1998 Mar;46(3):531-3. doi: 10.1248/cpb.46.531.
A new coating method for use in preparing controlled-release beads was developed by modifying the tumbling melt granulation technique. The dissolution rate of the drug from the beads was controlled by coating the mixture of meltable and non-meltable materials by heating in a centrifugal fluidizing granulator without using any solvent. In experiments using talc as the non-meltable material, the resultant beads showed the sufficient ability to suppress the dissolution of the drug and no change in the dissolution characteristics by wetting agent and in a stability test at high temperature. Using functional polymer as the non-meltable material, the controlled-release beads with various dissolution characteristics could be prepared: entero-soluble-release beads using entero-soluble polymer, and zero-order-release beads using hydrophilic gel-forming agent and talc.
通过改进滚动熔融造粒技术，开发出一种用于制备控释微丸的新型包衣方法。在离心流化制粒机中加热，不使用任何溶剂，通过包衣可熔性和不可熔性材料的混合物，来控制药物从微丸中的溶出速率。在使用滑石粉作为不可熔性材料的实验中，所得微丸显示出足够的抑制药物溶出的能力，并且在加入湿润剂和高温稳定性试验中，其溶出特性没有变化。使用功能性聚合物作为不可熔性材料，可以制备具有各种溶出特性的控释微丸：使用肠溶聚合物的肠溶释放微丸，以及使用亲水性凝胶形成剂和滑石粉的零级释放微丸。
