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以 PVP、PVA 为辅料制备了一种能漂浮在胃液上的地尔硫草(简称 D)漂浮片(HBS),测定了该片的体内外释药情况。D 能在人工胃液中缓慢持久地释放,药物系通过凝胶层扩散溶出,释药过程接近零级。家犬口服给药试验表明 D-HBS 片较 D 普通胶丸维持平稳而持久的血药浓度,其生物利用度也大致相同。
Diltiaulfuron (referred to as D) floating tablets (HBS) floating on the gastric juice were prepared by using PVP and PVA as excipients, and the in vitro and in vivo release properties of the tablets were measured. D can be slowly and permanently released in artificial gastric juice. Drugs diffuse and diffuse through the gel layer, and the drug release process approaches zero order. Dog oral administration test showed that D-HBS tablets than D ordinary capsules to maintain stable and long-lasting plasma concentration, its bioavailability is also roughly the same.