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Characterization of recrystallized itraconazole prepared by cooling and anti-solvent crystallization

Asian Journal of Pharmaceutical Sciences 2015年第3期10卷 230-238页

作者： Pornsak Sriamornsak kanokporn burapapadh Department of Pharmaceutical Technology Faculty of PharmacySilpakorn UniversityNakhon Pathom 73000Thailand Pharmaceutical Biopolymer Group(PBiG) Faculty of PharmacySilpakorn UniversityNakhon Pathom 73000Thailand Faculty of Pharmacy Rangsit UniversityPathum Thani 12000Thailand.

The objective of the present study was to alter the crystal habit of itraconazole(ITZ)by cooling and anti-solvent crystallization and characterize its *** was recrystallized in different solvents and the effects of each solvent on morphology of crystals,dissolution behavior and solid state of recrystallized drug particles were *** results revealed that ITZ crystals recrystallized by cooling and anti-solvent crystallization showed the different crystal habits from the untreated *** cooling crystallization tended to provide needle-shaped crystals while the crystals obtained from anti-solvent crystallization showed more flaky,plate *** indicated the importance of preparation method on nucleation and crystal *** change in drug polymorphism was observed,according to determination of thermal property and crystalline state by differential scanning calorimetry and powder X-ray diffractometry,*** recrystallized ITZ showed higher drug dissolution than untreated ITZ and the highest drug dissolution was observed from the samples recrystallized in the presence of PEG 200,which provided the small plate-shaped crystals with tremendously increased in surface ***,the increasing of drug dissolution is relatively small,therefore,further development may be required.

关键词： Itraconazole Poorly water-soluble drug Cooling crystallization Anti-solvent crystallization

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Development of pectin nanoparticles through mechanical homogenization for dissolution enhancement of itraconazole

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Asian Journal of Pharmaceutical Sciences 2016年第3期11卷 365-375页

作者： kanokporn burapapadh Hirofumi Takeuchi Pornsak Sriamornsak Department of Pharmaceutical Technology Faculty of Pharmacy Silpakorn University Pharmaceutical Biopolymer Group (PBiG) Faculty of Pharmacy Silpakorn University Laboratory of Pharmaceutical Engineering Gifu Pharmaceutical University

A simple method to fabricate itraconazole(ITZ)-loaded pectin nanoparticles prepared from nanoemulsion templates is described in this study. Nanoemulsions containing ITZ were prepared by a mechanical homogenization using pectin as emulsifier. After freeze-drying, the morphology, crystallinity state, thermal properties, drug dissolution and stability of the obtained pectin nanoparticles were characterized. The results demonstrated that the morphology of freeze-dried products was different, depending on the type of internal phase; the nanoparticles prepared from chloroform-based nanoemulsions were completely dried and provided a fragile characteristic. The pectin nanoparticles also demonstrated good properties in terms of redispersibility, thermal properties, drug crystallinity and dissolution. The ITZ-loaded pectin nanoparticles showed high percentage of drug dissolved(about 60–80%within 2 h), and maintained their good dissolution properties even after 1-year storage. The results suggested that freeze-dried pectin nanoparticles prepared from nanoemulsions could be used as an effective carrier for enhancement of ITZ dissolution.

关键词： Itraconazole Nanoparticles Pectin Poorly water-soluble drug Stability

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