Preparation and Evaluation of Berberine Alginate Beads for Stomach-Specific Delivery 英文参考文献.docVIP

Molecules 2011, 16, 10347-10356; doi:10.3390/molecules161210347 OPEN ACCESS molecules ISSN 1420-3049 /journal/molecules Article Preparation and Evaluation of Berberine Alginate Beads for Stomach-Specific Delivery Zhen-Hai Zhang 1,?, Yong-Shun Sun 2,?, Hui Pang 3, Were L.L. Munyendo 4, Hui-Xia Lv 4,* and Sheng-Liang Zhu 2,* 1 Jiangsu Province Academy of Traditional Chinese Medicine, No. 100 shizhijie, Nanjing 210028, China; E-Mail: davidpharm@ (Z.-H.Z.) 2 Yueyang Hospital of Integrated Traditional Chinese and Western Medicine, Shanghai University of Traditional Chinese Medicine, No. 110 ganhelu, Shanghai 200437, China; E-Mail: yongshunsun@ (Y.-S.S.) 3 Jiangsu Institute for Food and Drug Control, No. 6 beijingxilu, Nanjing 210024, China; E-Mail: yupang77@ (H.P.) 4 Department of Pharmaceutics, China Pharmaceutical University, No. 24 tongjiaxiang, Nanjing 210009, China ? These authors contributed equally to this work. * Authors to whom correspondence should be addressed; E-Mails: lvhuixia@163.com (H.-X.L.); zhushengliang999@163.com (S.-L.Z.); Tel.: +86-25-8530-9785 (H.-X.L.); +86-21-6516-1782-2512 (S.-L.Z.). Received: 10 November 2011; in revised form: 25 November 2011 / Accepted: 5 December 2011 / Published: 14 December 2011 Abstract: The purpose of this research was to prepare floating calcium alginate beads of berberine for targeting the gastric mucosa and prolonging their gastric residence time. The floating beads were prepared by suspending octodecanol and berberine in sodium alginate (SA) solution. The suspension was then dripped into a solution of calcium chloride. The hydrophobic and low-density octodecanol enhanced the sustained-release properties and floating ability of the beads. The bead formulation was optimized for different weight ratios of octodecanol and SA and evaluated in terms of diameter, floating ability and drug loading, entrapment and release. In vitro release studies showed that the floating