ジルチアゼムのヒト口腔からの吸収と塩酸ジルチアゼム速溶錠の調製ならびにその基礎的検討

概要

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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℃). 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 53〜106 μm and 250〜355 μm. 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 0.1M 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 106〜250 μm and tribasic sodium phosphate is suitable for the oral cavity dosage form as the fast-release and fast-effect tablet.
日本医療薬学会の論文
1995-10-10