抄録
We attempted to prepare diltiazem fast-release and fast-effect tablets using cellulose derivatives such as low-substituted hydroxypropylcellulose (LH-30 type L-HPC), hydroxyethylcelluose (CF-X type HEC, CF-G type HEC) and hydroxypropylmethylcellulose (TC-5E type HPMC) which are known as disintegrants and binders. The tablets were evaluated by in vitro dissolution test using the paddle method in JP XII second fluid (100 rpm, 37.0±0.5°C). The dissolution profiles showed that diltiazem was most rapidly dissolved from the tablet prepared with CF-G type HEC having four polymers. Moreover, the dissolution rate of diltiazem from the tablet prepared with CF-G type HEC was greater in the particle size of 106-250μm than in those of 53-106μm and 250-355μm. The effect of pH on absorption of diltiazem from the oral cavity was studied in six healthy volunteers. When diltiazem was administered to healthy volunteers with 0.1 M phosphate buffer solution, pH 7.0, the percent (25.5% of the dose) eliminated from the oral cavity was greater than that (6.9% of the dose) with 0.1 M phosphate buffer solution, pH 6.0 (p<0.01). From these results, it may be concluded that the formulation composed of diltiazem-HCl, CF-G type HEC with a particle size of 106-250μm and tribasic sodium phosphate is suitable for the oral cavity dosage form as the fast-release and fast-effect tablet.
