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Characterization and pharmacokinetic study of itraconazole solid dispersions prepared by solvent-controlled precipitation and spray-dry methods

Title
Characterization and pharmacokinetic study of itraconazole solid dispersions prepared by solvent-controlled precipitation and spray-dry methods
Author
최한곤
Keywords
biological evaluation of dosage forms; controlled- and sustained-release systems; dosage form design and characterization; pharmaceutics and drug delivery
Issue Date
2017-12
Publisher
WILEY-BLACKWELL
Citation
JOURNAL OF PHARMACY AND PHARMACOLOGY, v. 69, No. 12, Page. 1707-1715
Abstract
Objectives : Solid dispersion formulations have attracted attention to improve solubility and bioavailability of water-insoluble drugs. In this study, the variation of solubility and bioavailability by different preparation methods were studied using itraconazole (ITZ) solid dispersions. Methods : Itraconazole solid dispersions were prepared by a solvent-controlled precipitation method (SCPM) using HPMCAS-LF, HCl antisolvent or a spray-drying method (SDM) for comparison. Dissolution tests by pH transition and pharmacokinetic study using male Sprague Dawley rats were conducted. Key findings : Itraconazole solid dispersion dissolution tests by pH transition exhibited better dissolution compared to naive ITZ, limited dissolution in acidic conditions and a burst release at neutral pH. The ITZ solid dispersions by SCPM indicated a smaller-sized particle dispersion, limited dissolution at acidic pH and a higher release at neutral pH compared to those by SDM, suggesting that the increased protonation of anionic polymers and HPMCAS-LF by acidic antisolvent could form a tighter hydrophobic aggregation with ITZ in solid dispersions. ITZ solid dispersion prepared by SCPM also showed improved ITZ absorption in male Sprague Dawley rats compared to SDM and naive ITZ. Conclusions : This study suggests that the SCPM method can be widely used for solid dispersion preparations due to improved dissolution and PK profile.
URI
https://onlinelibrary.wiley.com/doi/abs/10.1111/jphp.12805http://repository.hanyang.ac.kr/handle/20.500.11754/103857
ISSN
0022-3573; 2042-7158
DOI
10.1111/jphp.12805
Appears in Collections:
COLLEGE OF PHARMACY[E](약학대학) > PHARMACY(약학과) > Articles
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