Preparation and evaluation of novel directly-compressed fast-disintegrating furosemide tablets with sucrose stearic acid ester.
Fast-disintegrating tablets of furosemide (FS) were prepared by the novel direct compression method. FS, microcrystalline cellulose (MC), croscarmellose sodium (CC), xylitol (XL) and sucrose stearic acid esters (SSEs) with an hydrophilic-lipophilic balance (HLB) of 16, 15 and 11, named S1670, S1570 and S1170, were used. An FS/SSE/MC mixed powder was obtained by solvent evaporation of a suspension of MC in ethanol solution containing FS and SSE, and the resultant mixed powder was mixed with CC and XL, and directly compressed. The tablets with hardness of more than 40 N and disintegration time of less than 20 s were obtained at the addition of SSE at 0--0.5% (w/w). A tablet with S1670 at 0.1% (w/w), named TA2, dissolved faster than a commercial FS tablet, Lasix. TA2 tended to show higher plasma concentration than Lasix after intragastric administration to rats. It was demonstrated that the present direct compression using homogeneous FS/S1670/MC powder mixture could give an excellent fast-disintegrating tablet of FS.
Koseki
Takuma
T
Department of Drug Delivery Research, Hoshi University, Tokyo, Japan.
Onishi
Hiraku
H
Takahashi
Yuri
Y
Uchida
Minoru
M
Machida
Yoshiharu
Y
D000818:Animals; D004339:Drug Compounding / Q000379:methods*; D004952:Esters / Q000737:chemistry; D005079:Excipients / Q000737:chemistry*; D005665:Furosemide / Q000097:blood / Q000737:chemistry*; D008297:Male; D008855:Microscopy, Electron, Scanning; D051381:Rats; D017207:Rats, Sprague-Dawley; D012995:Solubility; D013395:Sucrose / Q000031:analogs & derivatives* / Q000737:chemistry; D013499:Surface Properties; D013607:Tablets; D013997:Time Factors
D004952:Esters; D005079:Excipients; D013607:Tablets; C018153:sucrose monostearate; D013395:Sucrose; D005665:Furosemide