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KMID : 0369820150450030271
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Jorunal of Korean Pharmaceutical Sciences
2015 Volume.45 No. 3 p.271 ~ p.283
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Development of self emulsifying drug delivery system of itraconazole for oral delivery: formulation and pharmacokinetic consideration
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Chudasama Arpan
Shah Brijesh
Patel Vineetkumar
Nivsarkar Manish
Vasu Kamala
Shishoo Chamanlal
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Abstract
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Poorly water-soluble drug, itraconazole (ITZ) offers a challenge in developing a drug product with adequate bioavailability. The potential for lipidic self-emulsifying drug delivery system to improve the oral bioavailability of ITZ was investigated in fasted rats. A series of ITZ SEDDS were prepared in three groups based on oil:S/CoS mixture ratios (1:9, 1:6 and 1:4) using Capryol 90 (oil), a mixture of Labrasol and Tween 20 (surfactants) and Transcutol P (co-surfactant). The multi-component delivery systems were optimized by evaluating their ability to self-emulsify when introduced in simulated gastric fluid, without pepsin, under gentle agitation and by determination of droplet size and visual observation. Three formulations (F5, F21 and F27), one from each group were selected based on droplet size and visual observation. The effect of oil and surfactants content on mean globule size of resulting emulsions was studied. It was clear that oil to surfactant and co-surfactant ratio has the main impact on the droplet size of the emulsion formed after dilution. However, the relation between droplet size and in vivo absorption of ITZ was futile. The order of AUC was 1:4 > 1:6 > 1.9 for oil:S/CoS mixture ratios. Following an oral administration of developed SEDDS and marketed capsule to rats, a 1.7, 2.0 and 2.33-fold increase in bioavailability was observed for F5, F21 and F27 respectively, compared with marketed capsule. The results from this study demonstrate the potential use of SEDDS to provide an effective way of improving oral absorption of lipophilic drugs.
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KEYWORD
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Itraconazole, Lipid-based formulation, Antifungal, Triglycerides, Pseudo-ternary phase diagram, Bioavailability
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