Preparation and cyclodextrin assisted dissolution rate enhancement of itraconazolium dinitrate salt.
Summary of "Preparation and cyclodextrin assisted dissolution rate enhancement of itraconazolium dinitrate salt."
The poor solubility of itraconazole (ITR) results in its variable oral absorption and bioavailability and has also proven to be a major setback in developing an efficient oral delivery system. To improve its solubility and dissolution profile, itraconazolium dinitrate salt (ITRDNT) was prepared and characterized using various spectral and thermal techniques. The morphology of the salt was studied using optical and scanning electron microscopy (SEM). Broth microdilution assay demonstrated antifungal efficacy of ITRDNT similar to ITR against four different fungal strains namely, Asparagillus fumigatus, Microsporum canis, Microsporum gypsum and Trichophyton rubrum. The salt exhibited better solubility profile than ITR in water and a number of pharmaceutical solvents. Dissolution studies revealed the total amount of drug released from ITRDNT in 3 h was four times greater than that of ITR. To further improve dissolution characteristics, the physical mixtures of ITR and ITRDNT with two cyclodextrins, β-cyclodextrin (β-CD) and HP-β-cyclodextrin (HP-β-CD) were prepared and their molar ratios were optimized. It was observed that about 75% of drug was released in 30 min from 1:3 molar ratio of ITRDNT and HP-β-CD physical mixture, which was distinctly higher than ITR commercial capsules (70%). Owing to its facile and economical preparation and substantially better in vitro release profile, the ITRDNT and its CD physical mixtures could be better and cost effective alternatives to ITR and commercial ITR capsules.
Affiliation
University Institute of Pharmaceutical Sciences, UGC Centre of Advanced Study, Panjab University , Chandigarh , India.
Journal Details
This article was published in the following journal.
Name: Drug development and industrial pharmacy
ISSN: 1520-5762
Pages:
Links
- PubMed Source: http://www.ncbi.nlm.nih.gov/pubmed/22553909
- DOI: http://dx.doi.org/10.3109/03639045.2012.681382
Medical and Biotech [MESH] Definitions
Equine-assisted Therapy
Therapy assisted by the use of a horse and/or its movement, including equine-assisted psychotherapy, horseback riding, and hippotherapy.
Isosorbide Dinitrate
A vasodilator used in the treatment of ANGINA PECTORIS. Its actions are similar to NITROGLYCERIN but with a slower onset of action.
Numerical Analysis, Computer-assisted
Computer-assisted study of methods for obtaining useful quantitative solutions to problems that have been expressed mathematically.
Signal Processing, Computer-assisted
Computer-assisted processing of electric, ultrasonic, or electronic signals to interpret function and activity.
Radiotherapy Planning, Computer-assisted
Computer-assisted mathematical calculations of beam angles, intensities of radiation, and duration of irradiation in radiotherapy.
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