کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
8527335 | 1557997 | 2017 | 8 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
A lipophilic prodrug of Danshensu: preparation, characterization, and in vitro and in vivo evaluation
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کلمات کلیدی
موضوعات مرتبط
علوم پزشکی و سلامت
پزشکی و دندانپزشکی
طب مکمل و جایگزین
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چکیده انگلیسی
Danshensu [3-(3, 4-dihydroxyphenyl) lactic acid, DSS], one of the significant cardioprotective components, is extracted from the root of Salvia miltiorrhiza. In the present study, an ester prodrug of Danshensu (DSS), palmitoyl Danshensu (PDSS), was synthesized with the aim to improve its oral bioavailability and prolong its half-life. The in vitro experiments were carried out to evaluate the physicochemical properties and stability of PDSS. Although the solubility of PDSS in water was only 0.055 mg·mLâ1, its solubility in FaSSIF and FeSSIF reached 4.68 and 9.08 mg·mLâ1, respectively. Octanol-water partition coefficient (log P) was increased from â2.48 of DSS to 1.90 of PDSS. PDSS was relatively stable in the aqueous solution in pH range from 5.6 to 7.4. Furthermore, the pharmacokinetics in rats was evaluated after oral administration of PDSS and DSS. AUC and t1/2 of PDSS were enhanced up to 9.8-fold and 2.2-fold, respectively, compared to that of DSS. Cmax was 1.67 ± 0.11 μg·mLâ1 for PDSS and 0.81 ± 0.06 μg·mLâ1 for DSS. Thus, these results demonstrated that PDSS had much higher oral bioavailability and longer circulation time than its parent drug.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Chinese Journal of Natural Medicines - Volume 15, Issue 5, May 2017, Pages 355-362
Journal: Chinese Journal of Natural Medicines - Volume 15, Issue 5, May 2017, Pages 355-362
نویسندگان
Xue-Jiao GUO, Xue-Jiao FAN, Bin QIAO, Zhi-Qiang GE,