Document Detail

Development of eye drops containing antihypertensive drugs: formulation of aqueous irbesartan/γCD eye drops.
MedLine Citation:
PMID:  24754413     Owner:  NLM     Status:  Publisher    
Abstract Aqueous nanoparticulated eye drop formulations based on γ-cyclodextrin (γCD) complexes were developed and tested in vitro. Three antihypertensive drugs, i.e. enalapril maleate, irbesartan and verapamil HCl, that have been shown to possess IOP-lowering activity were selected for this study. All three drugs displayed Bs-type phase-solubility diagrams in aqueous γCD solutions and had relatively low affinity for γCD. Irbesartan was selected for further formulation development. The drug was relatively stable at pH 4.5 but somewhat less stable at physiologic pH. However, presence of γCD in the aqueous media enhanced the chemical stability of irbesartan. Aqueous γCD-based eye drop formulations containing 1% and 2% (w/v) irbesartan were prepared and the effect of pH on the particles size distribution and drug release investigated. Only ∼2% of the drug was in solution in the pH 4.5 formulations but up to 45% in the pH 7 formulations. The pH 7 formulations, where larger fraction of the drug was in solution, displayed somewhat greater drug permeation flux but much lower drug permeation coefficients than the pH 4.5 formulations. Dynamic light scattering studies indicated the faster permeation was due to formation of smaller particles in presence tyloxapol.
Phatsawee Jansook; Chutimon Muankaew; Einar Stefánsson; Thorsteinn Loftsson
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Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2014-4-23
Journal Detail:
Title:  Pharmaceutical development and technology     Volume:  -     ISSN:  1097-9867     ISO Abbreviation:  Pharm Dev Technol     Publication Date:  2014 Apr 
Date Detail:
Created Date:  2014-4-23     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9610932     Medline TA:  Pharm Dev Technol     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
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From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

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