錠劑是藥物劑型的其中之一。是由有效成分和賦型劑粉末混合壓製而成的。賦型劑包含了崩散劑、稀釋劑、潤滑劑等。崩散劑因吸水膨脹作用,產生膨脹力,使得錠劑裂解成小碎片,進而增進藥物溶離的速率。目前有關崩散劑所產生膨脹力的研究,很少有稀釋劑探討。
因此本研究目的,是想藉由物性測定儀,探討稀釋劑對於膨脹力的影響。本研究使用氫氯苯嗪做為模型藥物。欲探討的賦型劑有磷酸二鈣、微晶纖維素及甘露醇三種。崩散劑則為羧甲基澱粉鈉、交聯聚乙烯吡咯烷酮及交聯羧甲基纖維素鈉。將所製備之藥錠以物性測定儀測定膨脹力,並分別放入pH 1.2 的鹽酸緩衝溶液或pH 6.8磷酸緩衝溶液,進行崩散和溶離試驗。 研究結果顯示含有磷酸二鈣和崩散劑的錠劑,崩散和溶離效果最佳。雖然含有微晶纖維素和崩散劑的錠劑,膨脹力較大。 The tablet dosage form is the most popular pharmaceutical dosage form. It comprises a mixture of active substances and excipients compacted into a solid. The direct compression method is the most convenient method. The excipients usually include diluents and disintegrants. A disintegrant is commonly included in an immediate release tablet to enhance the disintegration of the tablet. The efficiency of a disintegrant is usually ascribed to its water uptake and swelling ability. The water-induced swelling force plays an important role in the disintegration of tablets.
However, the effect of diluents on the swelling force has not been studied. The purpose of this study is to investigate the effect of excipients on the swelling force. Dicalcium phosphate dihydrate, microcrystalline cellulose, and mannitol were chosen as model diluents. Hydrochlorothiazide was chosen as a model drug. The disintegration test and the dissolution test were also conducted in the pH 1.2 HCl buffer and the pH 6.8 phosphate buffer to discuss the mutual relationships.
The results show that the tablet containing a disintegrant and dicalcium phosphate dihydrate has the best disintegration and dissolution although the tablet containing a disintegrant and microcrystalline cellulose has higher swelling force.