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
موضوعات مرتبط
علوم پزشکی و سلامت پزشکی و دندانپزشکی طب مکمل و جایگزین
پیش نمایش صفحه اول مقاله
A lipophilic prodrug of Danshensu: preparation, characterization, and in vitro and in vivo evaluation
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·mL−1, its solubility in FaSSIF and FeSSIF reached 4.68 and 9.08 mg·mL−1, respectively. Octanol-water partition coefficient (log P) was increased from −2.48 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·mL−1 for PDSS and 0.81 ± 0.06 μg·mL−1 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
نویسندگان
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