کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
8513911 | 1556502 | 2008 | 39 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Origin of Nanodroplet Formation Upon Dissolution of an Amorphous Solid Dispersion: A Mechanistic Isotope Scrambling Study
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کلمات کلیدی
LLPSPVPVAPVPAAPsCD3ODD2ONTAnuclear magnetic resonance - رزونانس مغناطیسی هستهایDeuterium Oxide - اکسید دوتریمDrug loading - بارگیری مواد مخدرNanoparticle tracking analysis - تجزیه و تحلیل ردیابی نانو ذراتNMR - تشدید مغناطیسی هستهای Liquid-liquid phase separation - جداسازی فاز مایع مایعglass transition temperature - دمای انتقال شیشهRelative humidity - رطوبت نسبیDeuterated methanol - متانول ماتهDissolution mechanism - مکانیزم انحلالASD - نقص سپتوم یا دیوارهی دهلیزیAmorphous solid dispersion - پراکندگی جامد AmorphousAmorphous solid dispersions - پراکندگی جامد amorphouspolyvinylpyrrolidone - پلی وینیل پیرولیدون
موضوعات مرتبط
علوم پزشکی و سلامت
داروسازی، سم شناسی و علوم دارویی
اکتشاف دارویی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Origin of Nanodroplet Formation Upon Dissolution of an Amorphous Solid Dispersion: A Mechanistic Isotope Scrambling Study Origin of Nanodroplet Formation Upon Dissolution of an Amorphous Solid Dispersion: A Mechanistic Isotope Scrambling Study](/preview/png/8513911.png)
چکیده انگلیسی
It has been observed that certain amorphous solid dispersions (ASDs), upon dissolution, generate drug-rich amorphous nanodroplets. These nanodroplets, present as a dispersed phase, can potentially enhance oral bioavailability of poorly soluble drugs by serving as a drug reservoir that efficiently feeds the continuous aqueous solution phase following absorption of drug. The purpose of this study is to probe the formation mechanism of the nanodroplets. The model system studied was nifedipine (NFD) formulated as an ASD with hydroxypropyl methylcellulose E5 Premium LV or polyvinylpyrrolidone/vinyl acetate. Dissolution of ASDs prepared with proteated nifedipine (H-NFD) was carried out in a medium saturated with deuterated nifedipine (D-NFD) at the amorphous solubility. Upon dissolution, the H/D composition of NFD aqueous solution was determined using nuclear magnetic resonance spectroscopy. The results suggested that isotopic scrambling (equilibrium in the distribution of deuterated and proteated form of the drug) had occurred. Thus, as the H-NFD was brought into the aqueous solution via ASD dissolution, the drug concentration in solution exceeded the amorphous solubility. Subsequent precipitation of the drug, a process which does not differentiate H-NFD from D-NFD, generated NFD nanodroplets and resulted in redistribution of the isotopes. Thus, nanodroplets of NFD are formed due to dissolution of these homogenous ASDs followed by precipitation of the drug from aqueous solutions.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Journal of Pharmaceutical Sciences - Volume 106, Issue 8, August 2017, Pages 1998-2008
Journal: Journal of Pharmaceutical Sciences - Volume 106, Issue 8, August 2017, Pages 1998-2008
نویسندگان
Anura S. Indulkar, Jan E. Waters, Huaping Mo, Yi Gao, Shweta A. Raina, Geoff G.Z. Zhang, Lynne S. Taylor,