Kohei Matsumoto

Design and drug release properties of time-controlled release granule containing metominostrobin

A novel controlled drug release system on agrochemicals, time-controlled release granule (TCRG). which is characterized as an active ingredient release with a lag time, has been developed. This TCRG has a five-layered structure composed of core, active ingredient, swelling agent and two water-insoluble polymer membranes. The release profile of TCRG showed that lag time and release rate were optionally controlled by the coated amount of a water-insoluble polymer membrane, polyvinylidene chloride (PVC) and/or by the amount of a swelling agent, acrylate starch.

EFFECTS OF COATING CONDITIONS ON RELEASE PROFILES OF CONTROLLED RELEASE GRANULES COATED WITH WATER INSOLUBLE POLYMER

モデル薬物としてメトミノストロビンを用い, 粒剤表面を疎水性高分子で被覆した徐放性粒剤からの溶出挙動におよぼす被覆方法 (高分子液の滴下または流動層造粒機による被覆) と被覆液中の高分子濃度 (5および50%) の影響を調べた. その結果, 1) 高分子濃度50%の被覆液を用いて滴下または流動層造粒機で被覆した場合, 薬物の放出速度は滴下による被覆法>流動層造粒機による被覆法であったが, 溶出機構は同一であった. 2) 流動層造粒機による被覆の場合, 薬物の放出速度は高分子濃度5%<50%で, 溶出機構が異なった. これらの原因は, 粒剤表面の被覆膜における細孔の大きさや数の違いによることが示唆された.