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Preparation of injectable auto-forming alginate gel containing simvastatin with amorphous calcium phosphate as a controlled release medium and their therapeutic effect in osteoporosis model rat

机译:以无定形磷酸钙为控释介质的含辛伐他汀的可注射自动形成藻酸盐凝胶的制备及其对骨质疏松模型大鼠的治疗作用

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摘要

Highly soluble amorphous calcium phosphate powder (ACP) was added to the alginate gel as a buffering agent, in an attempt to enable widely controlled release while avoiding an acidification of the gel-environment. Therapeutic effects of the ACP-containing alginate gel which slowly releases a drug, simvastatin, on osteoporosis model rats were examined. A model drug, simvastatin, incorporated in the alginate gel with ACP up to 0.5%, was continuously released for a long time under the acidic condition. The release rate was controlled by the amount of ACP, serving as a buffer to suppress acidity. When the alginate solution intramuscularly injected in the rat, a soft gel was formed in the injected site. Simvastatin released from the gel containing 0.5% of ACP showed high therapeutic effect on osteoporosis rat. Thus, the present injectable long-sustained release system is expected to be a novel drug delivery controlling device.
机译:将高可溶性无定形磷酸钙粉末(ACP)作为缓冲剂添加到藻酸盐凝胶中,以试图实现广泛控制的释放,同时避免凝胶环境酸化。研究了含ACP的藻酸盐凝胶(它缓慢释放一种药物辛伐他汀)对骨质疏松模型大鼠的治疗作用。在酸性条件下,模型药物辛伐他汀与ACP含量高达0.5%的藻酸盐凝胶混合,可长时间连续释放。释放速率由ACP的量控制,ACP用作抑制酸度的缓冲剂。当将藻酸盐溶液肌肉内注射到大鼠中时,在注射部位形成了软凝胶。从含有0.5%ACP的凝胶中释放的辛伐他汀对骨质疏松症大鼠具有很高的治疗作用。因此,本发明的可注射的长效释放系统有望成为一种新颖的药物输送控制装置。

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  • 来源
    《Journal of materials science》 |2012年第5期|p.1291-1297|共7页
  • 作者单位

    Research Institute of Pharmaceutical Sciences,Musashino University, Tokyo, Japan;

    Faculty of Pharmaceutical Sciences, Musashino University,Tokyo. Japan;

    Research Institute of Pharmaceutical Sciences,Musashino University, Tokyo, Japan,College of Engineering, Nihon University, Fukushima, Japan;

    Research Institute of Pharmaceutical Sciences,Musashino University, Tokyo, Japan,RIKEN Innovation Center, Saitama, Japan;

    Dipartimento di Scienze Mediche, Universita del Piemonte Orientale, Novara, Italy,Dipartimento di Chimica "G. Ciamician", Alma Mater Studiorum, Universita di Bologna, Bologna, Italy;

    Dipartimento di Scienze Mediche, Universita del Piemonte Orientale, Novara, Italy;

    Dipartimento di Scienze Mediche, Universita del Piemonte Orientale, Novara, Italy;

    Research Institute of Pharmaceutical Sciences,Musashino University, Tokyo, Japan,Faculty of Pharmaceutical Sciences, Musashino University,Tokyo. Japan;

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