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Utilization of diethyl-beta-cyclodextrin as a sustained-release carrier for isosorbide dinitrate
F Hirayama1, N Hirashima, K Abe
1Faculty of Pharmaceutical Sciences, Kumamoto University, Japan.
Journal of Pharmaceutical Sciences
|March 1, 1988
Summary
Heptakis(2,6-di-O-ethyl)-beta-cyclodextrin (2) shows potential as a sustained-release drug carrier. Complexation with this cyclodextrin derivative significantly retards drug release, offering prolonged therapeutic effects.
Area of Science:
- Pharmaceutical Sciences
- Supramolecular Chemistry
- Drug Delivery Systems
Background:
- Cyclodextrins are widely used in drug formulation due to their ability to form inclusion complexes.
- Modifications of cyclodextrins can alter their physicochemical properties, influencing drug interactions and release profiles.
- Heptakis(2,6-di-O-ethyl)-beta-cyclodextrin (2) is a modified cyclodextrin with potential applications in drug delivery.
Purpose of the Study:
- To synthesize and characterize heptakis(2,6-di-O-ethyl)-beta-cyclodextrin (2).
- To compare the physicochemical properties of cyclodextrin (2) with beta-cyclodextrin (1) and heptakis(2,6-di-O-methyl)-beta-cyclodextrin (3).
- To evaluate the utility of cyclodextrin (2) as a sustained-release drug carrier for isosorbide dinitrate.
Main Methods:
- Synthesis and characterization of heptakis(2,6-di-O-ethyl)-beta-cyclodextrin (2).
- Comparative analysis of aqueous solubility and surface activity of cyclodextrins (1), (2), and (3).
- In vitro dissolution and release studies of isosorbide dinitrate from capsule and tablet formulations containing cyclodextrin (2).
- In vivo pharmacokinetic evaluation in rats following oral administration of drug-cyclodextrin complexes.
Main Results:
- Heptakis(2,6-di-O-ethyl)-beta-cyclodextrin (2) was successfully prepared.
- Complexation with cyclodextrin (2) significantly retarded the dissolution and release rates of isosorbide dinitrate.
- Oral administration of isosorbide dinitrate complexed with cyclodextrin (2) in rats demonstrated a sustained-release pattern over an extended period.
Conclusions:
- Heptakis(2,6-di-O-ethyl)-beta-cyclodextrin (2) exhibits favorable physicochemical properties for drug complexation.
- Cyclodextrin (2) effectively acts as a sustained-release matrix for the model drug isosorbide dinitrate.
- The modified cyclodextrin (2) shows promise as a hydrophobic drug carrier for achieving prolonged drug release.