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Transport Properties of Ibuprofen Encapsulated in Cyclodextrin Nanosponge Hydrogels: A Proton HR-MAS NMR Spectroscopy Study
Published on: August 15, 2016
Preformulation study of the inclusion complex irbesartan-beta-cyclodextrin.
Rajashree Hirlekar1, Vilasrao Kadam
1Department of Pharmaceutics, Bharati Vidyapeeth's College of Pharmacy,CBD Belapur, Navi Mumbai, Maharashtra, India. rshirlekar@rediffmail.com
AAPS Pharmscitech
|March 14, 2009
Summary
Improving irbesartan (IRB) solubility was achieved by forming an inclusion complex with beta-cyclodextrin (betaCD). The coevaporation method yielded the best results, significantly enhancing IRB
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Physical Chemistry
Background:
- Irbesartan (IRB) is a poorly water-soluble antihypertensive drug.
- Low solubility limits its bioavailability and therapeutic efficacy.
- Cyclodextrin complexation is a promising strategy to enhance drug solubility.
Purpose of the Study:
- To improve the solubility and dissolution profile of irbesartan (IRB).
- To prepare and characterize inclusion complexes of IRB with beta-cyclodextrin (betaCD).
- To evaluate different methods for inclusion complex formation.
Main Methods:
- Phase solubility studies were conducted to determine drug-solubility relationships.
- Inclusion complexes were prepared using cogrinding, kneading, and coevaporation methods.
- Characterization involved DSC, FTIR, SEM, XRD, and 1H NMR spectroscopy.
- Dissolution profiles were assessed and compared to pure IRB and physical mixtures.
Main Results:
- Phase solubility studies indicated a 1:1 stoichiometry inclusion complex formation with a stability constant (K(s)) of 104.39 M(-1).
- All preparation methods enhanced IRB solubility and dissolution.
- The coevaporation method demonstrated the most significant improvement in solubility and dissolution rate.
- Characterization confirmed the formation of IRB-betaCD inclusion complexes.
Conclusions:
- Beta-cyclodextrin complexation effectively enhances the solubility and dissolution of irbesartan.
- The coevaporation method is superior for preparing IRB-betaCD inclusion complexes.
- Cyclodextrin technology offers a viable approach to overcome the poor water solubility of irbesartan.
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