کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
8515034 | 1556513 | 2016 | 9 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Gastrointestinal and Systemic Monitoring of Posaconazole in Humans After Fasted and Fed State Administration of a Solid Dispersion
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کلمات کلیدی
supersaturation - فوق اشباع یا ابر سیرشده Amorphous - آمورفPrecipitation - بارندگیAbsorption - جذبOral absorption - جذب دهانیIntestinal absorption - جذب رودهGastrointestinal - دستگاه گوارشbiopharmaceutics classification system - سیستم طبقه بندی بیولوژیکی داروClinical pharmacokinetics - فارماکوکینتیک بالینیSolid dispersion - پراکندگی جامد
موضوعات مرتبط
علوم پزشکی و سلامت
داروسازی، سم شناسی و علوم دارویی
اکتشاف دارویی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Gastrointestinal and Systemic Monitoring of Posaconazole in Humans After Fasted and Fed State Administration of a Solid Dispersion Gastrointestinal and Systemic Monitoring of Posaconazole in Humans After Fasted and Fed State Administration of a Solid Dispersion](/preview/png/8515034.png)
چکیده انگلیسی
The purpose of this study was to explore the intraluminal behavior and systemic exposure of posaconazole in humans after oral intake of a novel delayed-release tablet (Noxafil®), containing posaconazole dispersed in a matrix of hydroxypropyl methylcellulose acetate succinate. Five healthy volunteers were asked to ingest the tablet in the fasted and fed state condition, after positioning one aspiration catheter in the stomach and one in the jejunum. Subsequently, gastric and jejunal fluids were aspirated and analyzed for posaconazole. In parallel, blood samples were collected. In gastric aspirates, dissolved concentrations were negligible regardless of the test condition, confirming the delayed-release properties of the tablet. In fasted state jejunal aspirates, sustained supersaturation was observed during an average period of time of 93 ± 78.2 min, with a mean maximum degree of supersaturation of 7.28 ± 8.81. In the fed state condition, supersaturation was negligible in the jejunum with a pronounced presence of solid posaconazole, suggesting the importance of more distal intestinal regions for posaconazole absorption.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Journal of Pharmaceutical Sciences - Volume 105, Issue 9, September 2016, Pages 2904-2912
Journal: Journal of Pharmaceutical Sciences - Volume 105, Issue 9, September 2016, Pages 2904-2912
نویسندگان
Bart Hens, Maura Corsetti, Joachim Brouwers, Patrick Augustijns,