Design and Preparation of Ethyl Cellulose Microcapsules of Gadopentetate Dimeglumine for Neutron-Capture Therapy Using the Wurster Process

概要

論文の詳細を見る
Microcapsules of hygroscopic, hyghly water-soluble gadopentetate dimeglumine (Gd-DTPA-DM) for use in preliminary in vivo experiments for neutron-capture therapy were designed. They were prepared with such properties as a particle size small enough to be suspended and injected through a syringe, a negligible release of Gd-DTPA-DM, and a high drug content by means of the Wurster process, a spray coating method using a spouted bed with a draft tube. They were composed of lactose cores of 53-63 μm, an undercoat of ethyl cellulose (EC) and polyvinylpyrrolidone (PVP), a drug-layer of Gd-DTPA-DM, EC and PVP, a waterproof coat and a release-sustaining overcoat of EC and cholesterol (1 : 1), and a surface treated with hydrogenated egg lecithin. By curing at 110℃ for 30 min after mixing with 20% pulverized mannitol powder, the 20% overcoating suppressed the release of Gd-DTPA-DM from 75-106 μm microcapsules to less than 10% for the first 20 min, which was the period required to prepare a suspension, inject it and irradiate the neutron. The microcapsules could be used to confirm that the intracellular presence of Gd is not critical in gadolinium neutron-capture therapy.
公益社団法人日本薬学会の論文
1993-06-15