کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1986069 1540237 2016 6 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Improved oral absorption of tacrolimus by a solid dispersion with hypromellose and sodium lauryl sulfate
ترجمه فارسی عنوان
جذب دهانی جذب تاکرولیموس توسط پراکندگی جامد با هیپرومولوز و سدیم لوریل سولفات بهبود یافته است
کلمات کلیدی
تاکرولیموس، پراکندگی جامد، هیدروکسی پروپیل متیل سلولز، سدیم لوریل سولفات، انحلال، قابلیت دسترسی به بی
موضوعات مرتبط
علوم زیستی و بیوفناوری بیوشیمی، ژنتیک و زیست شناسی مولکولی زیست شیمی
چکیده انگلیسی

A novel surfactant-incorporated hydroxypropyl methylcellulose (HPMC) solid dispersion (SD) system was constructed in order to facilitate the release rate and oral absorption of tacrolimus (FK506), a poorly water-soluble immunosuppressant. Several emulsifiers including sodium lauryl sulfate (SLS), as drug release promotors, were employed with HPMC to fabricate SD using the solvent wetting method. The solid state characteristics using differential scanning calorimetry and X-ray powder diffraction, revealed that FK506 was molecularly distributed within all dispersions in amorphous form. The dissolution rates of FK506 in SLS-incorporated SDs were much higher than those in SDs prepared with HPMC alone, and even with stearoyl polyoxyl-32 glycerides or tocopheryl polyethylene glycol 1000 succinate. In particular, the greatest dissolution enhancement was obtained from the SD consisting of the drug, HPMC, and SLS in a weight ratio of 1:1:3, providing a 50-fold higher drug concentration within 15 min, compared with HPMC SD. In vivo absorption study in rats demonstrates that the optimized formula remarkably increased the oral absorption of FK506, providing about 4.0-fold greater bioavailability (p < 0.05) compared with the marketed product (Prograf®, Astellas Pharma). These data suggest that a novel SLS/HPMC SD may be an advantageous dosage form of FK506, boosting the dissolution and absorption in gastrointestinal tract.

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: International Journal of Biological Macromolecules - Volume 83, February 2016, Pages 282–287
نویسندگان
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