کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
5820958 | 1557408 | 2012 | 11 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Solid dispersions of itraconazole for inhalation with enhanced dissolution, solubility and dispersion properties
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کلمات کلیدی
NGIHSMMDTTPGSDPIXRPDFPDHPLC-UVGRASAPIITZpMDIMSLIMTDSCFPFModulated Temperature Differential Scanning Calorimetry - Calorimetry اسکن دیفرانسیل درجه حرارت مدولاسیونPulmonary aspergillosis - آسپرژیلوز ریویAmorphous - آمورفItraconazole - ایتراکونازولgenerally recognized as safe - به طور کلی به عنوان امن شناخته شده استSpray-drying - خشک کردن افشانه ای یا اسپری درایینگ Dae - دلمfine particle dose - دوز ذرات خوبNext generation impactor - ضربه گیر نسل بعدیPressurised metered dose inhaler - فشار انسداد دز انسدادAerodynamic diameter - قطر آیرودینامیکیMean dissolution time - متوسط زمان انحلالSEM - مدل معادلات ساختاری / میکروسکوپ الکترونی روبشیActive Pharmaceutical Ingredient - مواد اولیه دارویی فعالScanning electron microscopy - میکروسکوپ الکترونی روبشیHot stage microscopy - میکروسکوپ مرحله داغX-ray powder diffraction - پراش پودر اشعه ایکسSolid dispersion - پراکندگی جامدDry powder for inhalation - پودر خشک برای استنشاقFine particle fraction - کسر ذرات جامد
موضوعات مرتبط
علوم پزشکی و سلامت
داروسازی، سم شناسی و علوم دارویی
علوم دارویی
پیش نمایش صفحه اول مقاله

چکیده انگلیسی
The purpose of this study was to produce a dry powder for inhalation (DPI) of a poorly soluble active ingredient (itraconazole: ITZ) that would present an improved dissolution rate and enhanced solubility with good aerosolization properties. Solid dispersions of amorphous ITZ, mannitol and, when applicable, d-α-tocopherol polyethylene glycol 1000 succinate (TPGS) were produced by spray-drying hydro-alcoholic solutions in which all agents were dissolved. These dry formulations were characterized in terms of their aerosol performances and their dissolution, solubility and physical properties. Modulate differential scanning calorimetry and X-ray powder diffraction analyses showed that ITZ recovered from the different spray-dried solutions was in an amorphous state and that mannitol was crystalline. The inlet drying temperature and, indirectly, the outlet temperature selected during the spray-drying were critical parameters. The outlet temperature should be below the ITZ glass transition temperature to avoid severe particle agglomeration. The formation of a solid dispersion between amorphous ITZ and mannitol allowed the dry powder to be produced with an improved dissolution rate, greater saturation solubility than bulk ITZ and good aerosol properties. The use of a polymeric surfactant (such as TPGS) was beneficial in terms of dissolution rate acceleration and solubility enhancement, but it also reduced aerosol performance. For example, significant dissolution rate acceleration (f2 < 50) and greater saturation solubility were obtained when introducing 1% (w/w) TPGS (mean dissolution time dropped from 50.4 min to 36.9 min and saturation solubility increased from 20 ± 3 ng/ml to 46 ± 2 ng/ml). However, the fine particle fraction dropped from 47 ± 2% to 37.2 ± 0.4%. This study showed that mannitol solid dispersions may provide an effective formulation type for producing DPIs of poorly soluble active ingredients, as exemplified by ITZ.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: International Journal of Pharmaceutics - Volume 428, Issues 1â2, 30 May 2012, Pages 103-113
Journal: International Journal of Pharmaceutics - Volume 428, Issues 1â2, 30 May 2012, Pages 103-113
نویسندگان
Christophe Duret, Nathalie Wauthoz, Thami Sebti, Francis Vanderbist, Karim Amighi,