کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
9917619 | 1556304 | 2005 | 10 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
A three step supercritical process to improve the dissolution rate of Eflucimibe
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کلمات کلیدی
DSCγ-cyclodextrinSASGPCSDSnuclear magnetic resonance - رزونانس مغناطیسی هستهایAUC - AUCDMSO - DMSONMR - تشدید مغناطیسی هستهای Room temperature - دمای اتاقDimethylsulfoxide - دیمتیل سولفواکسیدsodium dodecyl sulfate - سدیم دودسیل سولفاتSupercritical fluid - سیال فوق بحرانیCyclodextrin - سیکلودکسترینSupercritical antisolvent - ضد حلال فوق بحرانیInclusion complex - مجتمع گنجاندنarea under the curve - منطقه تحت منحنیSolid dispersion - پراکندگی جامدDifferential scanning calorimetry - کالریمتری روبشی افتراقیgas phase chromatography - کروماتوگرافی فاز گازhigh performance liquid chromatography - کروماتوگرافی مایع با کارایی بالاHPLC - کروماتوگرافی مایعی کارا
موضوعات مرتبط
علوم پزشکی و سلامت
داروسازی، سم شناسی و علوم دارویی
اکتشاف دارویی
پیش نمایش صفحه اول مقاله

چکیده انگلیسی
The aim of this study is to improve the dissolution properties of a poorly-soluble active substance, Eflucimibe by associating it with γ-cyclodextrin. To achieve this objective, a new three-step process based on supercritical fluid technology has been proposed. First, Eflucimibe and cyclodextrin are co-crystallized using an anti-solvent process, dimethylsulfoxide being the solvent and supercritical carbon dioxide being the anti-solvent. Second, the co-crystallized powder is held in a static mode under supercritical conditions for several hours. This is the maturing step. Third, in a final stripping step, supercritical CO2 is flowed through the matured powder to extract the residual solvent. The coupling of the first two steps brings about a significant synergistic effect to improve the dissolution rate of the drug. The nature of the entity obtained at the end of each step is discussed and some suggestions are made as to what happens in these operations. It is shown the co-crystallization ensures a good dispersion of both compounds and is rather insensitive to the operating parameters tested. The maturing step allows some dissolution-recrystallization to occur thus intensifying the intimate contact between the two compounds. Addition of water is necessary to make maturing effective as this is governed by the transfer properties of the medium. The stripping step allows extraction of the residual solvent but also removes some of the Eflucimibe which is the main drawback of this final stage.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: European Journal of Pharmaceutical Sciences - Volume 26, Issue 2, October 2005, Pages 184-193
Journal: European Journal of Pharmaceutical Sciences - Volume 26, Issue 2, October 2005, Pages 184-193
نویسندگان
Elisabeth Rodier, Hubert Lochard, Martial Sauceau, Jean-Jacques Letourneau, Bernard Freiss, Jacques Fages,