采用正交实验优化诺氟沙星片剂的制备条件,获得最佳处方:淀粉为填充剂,质量分数为5%的羧甲基淀粉钠(CMS-Na)为崩解剂,1%的滑石粉为润滑剂,10%的淀粉浆为黏合剂.为增大诺氟沙星药物的溶出,采用研磨法制备β-环糊精诺氟沙星包合物,经湿法制粒压片工艺制备环糊精诺氟沙星片剂.环糊精诺氟沙星片的片重差异、脆碎度和崩解时限均符合2010版中国药典要求,其中诺氟沙星的溶出度得到有效改善,解决了诺氟沙星片剂对照组的主药溶出度低的问题.采用优化处方和制备工艺,制备环糊精诺氟沙星片,可改善难溶性诺氟沙星药物的溶出度且工艺简单易行.
[1] 罗昕, 平其能, 柯学, 宋云梅. 微粉化及包合技术对格列本脲溶出度的影响 [J]. 中国药学杂志 2003.doi:10.3321/j.issn:1001-2494.2003.03.012
[2] 吕娟丽, 王坚成, 张烜, 张强, Juan-Li Lu, Jian-Cheng Wang, Xuan Zhang, Qiang Zhang. 9-硝基喜树碱自微乳化注射液的研制及其体内药动学行为 [J]. 中国药学(英文版) 2007.
[3] 罗昕, 徐月红, 陈宝, 古练权, 黄民, 刘培庆, LUO Xin, XU Yue-hong, CHEN Bao, GU Lian-quan, HUANG Min, LIU Pei-qing. 隐丹参酮固体分散体的制备及性质研究 [J]. 中草药 2005.doi:10.3321/j.issn:0253-2670.2005.06.016
[4] 袁曦, 洪清, 林功舟, 林芳英. 氯化血红素-β环糊精包合物的研制 [J]. 中国药学杂志 2001.doi:10.3321/j.issn:1001-2494.2001.06.010
[5] 李海鹰, 杨文智, 刘静, 刘海燕, LI Hai-ying, YANG Wen-zhi, LIU Jing, LIU Hai-yan. 诺氟沙星胶囊含量及其溶出度的测定 [J]. 河北大学学报(自然科学版) 2005.doi:10.3969/j.issn.1000-1565.2005.05.014
[6] GUYOT M, FAWAZ F, BILDRT J. Physicochemical characterization and dissolution of norfloxacin-cyclodextrin inclusion compounds and PEG solid dispersions [J]. International Journal of Pharmaceutics 1995, 123(01).
[7] 中华人民共和国卫生部药典委员会. 2010版中华人民共和国药典 [M]. 北京:化学工业出版社 2010.
[8] 朱治本, 何海霞, 周远大. 几种诺氟沙星盐的药代动力学及相对生物利用度的比较 [J]. 中国抗生素杂志 1993, 18(05).
[9] Kang BK, Chon SK, Kim SH, Jeong SY, Kim MS, Cho SH, Lee HB, Khang G. Controlled release of paclitaxel from microemulsion containing PLGA and evaluation of anti-tumor activity in vitro and in vivo. [J]. International Journal of Pharmaceutics 2004, 1/2(1/2).
[10] Moneghini M, Kikic I, Voinovich D, Perissutti B, Filipovic-Grcic J. Processing of carbamazepine-PEG 4000 solid dispersions with supercritical carbon dioxide: preparation, characterisation, and in vitro dissolution. [J]. International Journal of Pharmaceutics 2001, 1(1).
[11] Mathot F, van Beijsterveldt L, Preat V, Brewster M, Arien A. Intestinal uptake and biodistribution of novel polymeric micelles after oral administration [J]. Journal of Controlled Release: Official Journal of the Controlled Release Society 2006, 1/2(1/2).
[12] Mathot F, Rieux AD, Arien A, Schneider YJ, Brewster M, Preat V. Transport mechanisms of mmePEG(750)P(CL-co-TMC) polymeric micelles across the intestinal barrier [J]. Journal of Controlled Release: Official Journal of the Controlled Release Society 2007, 3(3).
[13] Li-Juan Yang, Wen Chen, Shui-Xian Ma. Host-guest system of taxifolin and native cyclodextrin or its derivative: Preparation, characterization, inclusion mode, and solubilization [J]. Carbohydrate Polymers: Scientific and Technological Aspects of Industrially Important Polysaccharides 2011, 3(3).
[14] WANG Jing, CAO Yanping, SUN Baoguo. Characterisation of inclusion complex of trans-ferulic acid and hydroxypropyl-b-cyclodextrin [J]. Food Chemistry 2011, 124(03).
[15] LOFTSSON T, JARHO P, MASSON M. Cyclodextrins in drug delivery [J]. Expert Opinion Drug Delivery 2005, 2(02).
[16] TOSHIRO FUKAMI, TAKAYUKI FURUISHI, TOYOFUMI SUZUKI. Improvement in Solubility of Poorly Water Soluble Drug by Cogrinding with Highly Branched Cyclic Dextrin [J]. Journal of Inclusion Phenomena and Macrocyclic Chemistry 2006, 1/2(1/2).
[17] Riekes, M.K., Tagliari, M.P., Granada, A., Kuminek, G., Silva, M.A.S., Stulzer, H.K.. Enhanced solubility and dissolution rate of amiodarone by complexation with β-cyclodextrin through different methods [J]. Materials science & engineering, C. Biomimetic and supramolecular systems 2010, 7(7).