Enhancement of Dissolution Rates of Furosemide Solvent Deposition Matrixes by Solvent Deposition Method and Diuretic Effects in Rats

Solvent Deposition Method를 이용(利用)한 Furosemide 제제(製劑)의 용출증대(溶出增大) Rat에서의 이용효과(利用效果)에 관한 연구(硏究)

The matrix affects the dissolution of furosemide, which is almost insoluble in the dissolution medium. In order to understand the effect of the matrix on the dissolution of furosemide, lactose, starch, $Avicel\;^{\circledR}pH\;101$, $Avicel\;^{\circledR}pH\;301$, $SiO_2$ and talc were used as the matrix and the solvent deposition method were used. The dissolution characteristics of four dissolution medium were compared to each other using various ratio of drug-to-matrix. The results are as follows: 1) Lactose was shown to be superior and talc was to be inferior to the other matrixes investigated. 2) A maximum dissolution rate and dissolution amount of furosemide were observed in 1 : 10 ratio of the drug-to-matrix. 3) $T_{80%}$ of 1 : 10 ratio of the drug-to-matrix in pH 7.2 was 1 min. from FM-lactose and 30 min. from FM-talc. $T_{50%}$ in pH 4.2 is 2 min. from furosemide-lactose and 150 min. from furosemide-talc. Total amount of furosemide in pH 1.2 at 30 min. were enhanced 13.3 fold in furosemide-lactose and 3.5 fold in furosemide-talc compared to the control. Diuretic action of those furosemide-lactose and furosemide-talc was also evaluated by monitoring changes in urinary excretion of sodium, potassium and urine volume in rat. The accumulated urine volume were enhanced 1.7 fold in furosemide-lactose (1.5) compared to the furosemide.