Inclusion complexation of furosemide in cyclodextrins. Part 2: Implication on bioavailability.
The effect of inclusion complexation of furosemide in cyclodextrins (CyD) on the bioavailability of the drug was studied on normal human volunteers. The excretion rate of the drug was determined by HPLC for a period of 24 h. post dosing. Several pharmacokinetic parameters were calculated and statistically analyzed. viz., peak excretion rate, peak excretion time, half peak time, elimination rate constant, area under the excretion rate time-curve as well as the total amount of drug excreted. The obtained results show that on administration of furosemide in the form of an inclusion complex in CyDs particularly beta-CyD or its dimethyl derivative may improve its biological performance, taking into consideration that furosemide is characterized by a rapid onset and a short duration of action. Inclusion complexation of furosemide in CyDs leads to a more or less delay in its onset of action, a significant increase in its duration of action as well as significant augmentation in its overall biological availability.
Ammar
H O
HO
Department of Pharmaceutical Sciences, Faculty of Pharmacy, Cairo University, Egypt.
Ghorab
M
M
Emara
L H
LH
el-Nahhas
S A
SA
Makram
T S
TS
D000328:Adult; D019540:Area Under Curve; D001682:Biological Availability; D002851:Chromatography, High Pressure Liquid; D003505:Cyclodextrins; D004232:Diuretics / Q000008:administration & dosage / Q000737:chemistry* / Q000493:pharmacokinetics; D005665:Furosemide / Q000008:administration & dosage / Q000737:chemistry* / Q000493:pharmacokinetics; D006207:Half-Life; D006801:Humans
D003505:Cyclodextrins; D004232:Diuretics; D005665:Furosemide