Study on Itraconazole Self-Emulsifying Drug Delivery System

CHEN Ying;ZHENG Qing-ling;LIU Hong;XIN Hu-wen

Chinese Pharmaceutical Journal ›› 2008, Vol. 43 ›› Issue (22) : 1714-1718.

Chinese Pharmaceutical Journal ›› 2008, Vol. 43 ›› Issue (22) : 1714-1718.
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Study on Itraconazole Self-Emulsifying Drug Delivery System

  • CHEN Ying,ZHENG Qing-ling,LIU Hong,XIN Hua-wen
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Abstract

OBJECTIVE To develop the formulation of self-emulsifying drug delivery system for itraconazole(ITZ-SEDDS).METHODS The optimum formulations of ITZ-SEDDS were screened by solubility experiments,compatibility tests and pseudo-ternary phase diagrams,with the time of formulating emulsion,the consequence of visual examination and particle size as parameters.And the physic-chemical characters and dissolution in vitro of ITZ-SEDDS were also determined.RESULTS The optimum self-emulsifying drug delivery system was composed of Maisine 35-1(25%),Cremophor EL(30%) and Transcutol P(45%).The particle diameter was 162.5 nm,the time of self-microemulsifying was less than 1 min.The percent of accumulated dissolution of itraconazole in SEDDS in simulated intenstinal fluid was up to 90.9% at 2 h,which was 174.8 times as much as that of ITZ crude powder,and 9.0 times as much as that of ITZ capsules.CONCLUSION The formulation of ITZ-SEDDS prepared achieved the requirement of design.It could provide reference for the new dosage form of itraconazole.

Key words

itraconazole / self-emulsifying drug delivery system / formulation design / dissolution in vitro

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CHEN Ying;ZHENG Qing-ling;LIU Hong;XIN Hu-wen. Study on Itraconazole Self-Emulsifying Drug Delivery System [J]. Chinese Pharmaceutical Journal, 2008, 43(22): 1714-1718

References

[1] BARONE J A,KOH J G,BIERMAN R H,et al. Food interaction and steady-state pharmacokinetics of itraconazole capsules in healthy male volunteers[J] .Antimicrob Agents Chemother,1993,37(4):778-784. [2] HASSAN H A,AL-MARZOUQI A H,JOBE B,et al. Enhan- cement of dissolution amount and in vivo bioavailability of itraconazole by complexation with beta-cyclodextrin using supercritical carbon dioxide[J] . J Pharm Biomed Anal,2007,45(2):243-250. [3] BARONE J A,MOSKOVITZ B L,GUARNIERI J,et al. Enhan- ced bioavailability of itraconazole in hydroxypropyl- beta- cyclodextrin solution versus capsules in healthy volunteers[J] . Antimicrob Agents Chemother,1998 ,42(7):1862-1865. [4] GURSOY R N,BENITA S. Self-emulsifying drug delivery systems (SEDDS) for improved oral delivery of lipophilic drugs[J] . Biomed Pharmacother,2004,58(3):173-182. [5] KONG B B,WANG S L,SU D S,et al. Studies on preparation and properties of itraconazole emulsion for intravenous administration[J] . Chin J Pharm (中国药剂学杂志),2006,4(1):7-11. [6] ZIMMERMANN T,YEATES R A,LAUFEN H,et al. Influence of concomitant food intake on the oral absorption of two triazole antifungal agents,itraconazole and fluconazole[J] . Eur J Clin Pharmacol,1994,46(2):147-150. [7] CHEN Y, LI G, WU X G, et al. Self-microemulsifying drug delivery system(SMEDDS) of vinpocetine: formulation development and in vivo assessment[J] . Bio Pharm Bull,2008,31(1):118-125. [8] SONG Y,CHANG D,WANG D K,et al. Formulation selection and study of dissolution in vitro on liquid hard capsules of daidzein[J] . J Shenyang Pharm Univ(沈阳药科大学学报),2008,2(2):96-100.

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