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Inclusion complexation of furosemide in cyclodextrins. Part 2: Implication on bioavailability
H O Ammar1, M Ghorab, L H Emara
1Department of Pharmaceutical Sciences, Faculty of Pharmacy, Cairo University, Egypt.
Die Pharmazie
|April 7, 1999
Summary
Formulating furosemide (a diuretic) with cyclodextrins (CyD) enhances its bioavailability. This inclusion complexation improves drug performance, increasing duration and overall biological availability.
Area of Science:
- Pharmacology
- Drug Delivery Systems
- Physical Chemistry
Background:
- Furosemide is a widely used diuretic with a rapid onset and short duration of action.
- Improving the bioavailability and pharmacokinetic profile of furosemide is crucial for optimizing therapeutic outcomes.
- Cyclodextrins (CyD) are known excipients that can form inclusion complexes to modify drug properties.
Purpose of the Study:
- To investigate the effect of furosemide inclusion complexation with cyclodextrins on its bioavailability.
- To evaluate the pharmacokinetic parameters of furosemide after administration of its cyclodextrin inclusion complexes.
- To determine if cyclodextrin complexation can enhance the biological performance of furosemide.
Main Methods:
- Human volunteers were administered furosemide in both free form and as cyclodextrin inclusion complexes.
- Drug excretion rates were monitored over 24 hours post-dosing using High-Performance Liquid Chromatography (HPLC).
- Key pharmacokinetic parameters including peak excretion rate, time to peak, half-peak time, elimination rate constant, and total excreted drug were calculated and analyzed.
Main Results:
- Inclusion complexation of furosemide with cyclodextrins, especially beta-cyclodextrin and its dimethyl derivative, demonstrated improved biological performance.
- Complexation led to a delay in the onset of action but significantly increased the duration of action.
- A significant augmentation in the overall biological availability of furosemide was observed with cyclodextrin complexation.
Conclusions:
- Furosemide inclusion complexes with cyclodextrins, particularly beta-CyD, can enhance its bioavailability and prolong its therapeutic effect.
- This formulation strategy offers a promising approach to improve the pharmacokinetic profile and efficacy of furosemide.
- Cyclodextrin complexation is an effective method for modulating the drug release and absorption characteristics of furosemide.