کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
2084318 1545375 2010 7 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Transglycosylated stevia and hesperidin as pharmaceutical excipients: Dramatic improvement in drug dissolution and bioavailability
موضوعات مرتبط
علوم زیستی و بیوفناوری بیوشیمی، ژنتیک و زیست شناسی مولکولی بیوتکنولوژی یا زیست‌فناوری
پیش نمایش صفحه اول مقاله
Transglycosylated stevia and hesperidin as pharmaceutical excipients: Dramatic improvement in drug dissolution and bioavailability
چکیده انگلیسی

The capability of transglycosylated materials, α-glycosyltransferase-treated stevia (Stevia-G) and α-glycosyl hesperidin (Hsp-G), to enhance the bioavailability of poorly water-soluble drugs was investigated. Spray-dried particles (SDPs) of drug/transglycosylated material, such as, flurbiprofen (FP)/Stevia-G, probucol (PRO)/Stevia-G, FP/Hsp-G, and PRO/Hsp-G were prepared. All SDPs showed pronounced improvement in both dissolution rate and apparent drug solubility. The amount of dissolved PRO was significantly improved to that of untreated PRO crystals when prepared as SDPs of PRO/Stevia-G or PRO/Hsp-G. There was no cytotoxicity to Caco-2 cells at levels of 10% Stevia-G or Hsp-G solution. Values for the area under the plasma concentration–time curve (AUC) of untreated PRO, SDPs of PRO/Hsp-G and PRO/Stevia-G after oral administration to rats were 4.94 ± 2.06, 26.08 ± 4.52 and 48.79 ± 9.97 μg h/mL, respectively. Interestingly, AUC values in cases of the FP system were in the order of untreated FP < SDPs of FP/Stevia-G < SDPs of FP/Hsp-G. The effect on drug absorption enhancement may depend on the type of transglycosylated materials used. Stevia-G, a newly investigated material for this purpose, was found to have good potential for use as a pharmaceutical excipient.

Plasma concentration–time profiles of probucol in rats after oral administration of untreated probucol and spray-dried particles of probucol and Stevia-G or Hsp-G.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: European Journal of Pharmaceutics and Biopharmaceutics - Volume 76, Issue 2, October 2010, Pages 238–244
نویسندگان
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