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        Preparation and Characterization of a Novel pH-Sensitive Coated Microsphere for Duodenum-Specific Drug Delivery

        Dan Zhou,Yuan Huang,Xi Zhu,Yang Wang,Yun Jin,Xuefan Xu,Tingting Fan,Yan Liu,Zhirong Zhang 대한약학회 2012 Archives of Pharmacal Research Vol.35 No.5

        The aim of this study is to develop a duodenum-specific drug delivery system on the basis of a pH-sensitive coating and a mucoadhesive inner core for eradication of Helicobacter pylori (H. pylori) in the ulcer duodenum. Hydroxypropyl methylcellulose acetate maleate (HPMCAM) was used as the pH-sensitive material, which dissolves around pH 3.0. The mucoadhesive microspheres loaded with furazolidone (FZD-ad-MS) were prepared by the emulsification-solvent evaporation method using Carbopol 971NP as the mucoadhesive polymer. The prepared pH-sensitive coated mucoadhesive microspheres (AM-coated-MS) were characterized in regards to particle size, drug loading efficiency, morphological change, drug stability, drug release and in vitro anti-H. pylori activity. The particle size was 160.97 ± 47.24 μm and 336.44 ± 129.34 μm, and the drug content was 42.33 ± 3.43% and 10.96 ± 1.29% for FZD-ad-MS and AM-coated-MS, respectively. The morphological changes in different pH media were characterized by scanning electron microscopy (SEM). HPMCAM coating improved the stability of the FZD-ad-MS and these particles were expected to remain intact until their arrival in the duodenum. The drug release was extremely suppressed at pH 1.2 for AM-coated-MS, but increased at pH 4.0 after regeneration of FZD-ad-MS. In addition, FZD-ad-MS exhibited excellent anti-H. pylori activity in vitro. Thus, the HPMCAM-coated microspheres developed in this study hold great promise for use as a duodenum-specific drug delivery system for H. pylori clearance.

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        Five new anthraquinones from the seed of Cassia obtusifolia

        Yi-Long Xu,Li-Ying Tang,Xi-Dan Zhou,Guo-Hong Zhou,Zhu-Ju Wang 대한약학회 2015 Archives of Pharmacal Research Vol.38 No.6

        A phytochemical investigation on the seeds ofCassia obtusifolia led to the isolation of five new anthraquinones,including one aglycon and four glycosides. Thestructures were elucidated by analysis of extensive spectroscopicdata and the results of acid hydrolysis. All theseisolates were evaluated for their inhibitory effects againsta-glucosidase, and 1 showed potent activity with IC50value of 185 ± 15 lM.

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