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瑞舒伐他汀钙片溶出度研究 被引量:7

Research on the Dissolution Profiles of Rosuvastatin Calcium Tablets
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摘要 目的建立瑞舒伐他汀钙片溶出度研究方法。方法HPLC法,色谱柱:AgilentExtendC18(4.6×250mm,5μm);流动相:以乙腈为流动相A,以0.02%三氟乙酸溶液为流动相B,0~13min,A:37%,13—27min,A:37%--90%;检测波长:242nm;流速:1.0mL·min-1;发生降解行为的溶出度样品经碱中和前处理后以瑞舒伐他汀钙与瑞舒伐他汀非对映异构体峰面积之和计算累积溶出量(%)。结果瑞舒伐他汀钙在pH1.0盐酸溶液不稳定,降解生成瑞舒伐他汀非对映异构体,瑞舒伐他汀-5S-内酯和瑞舒伐他汀-5R-内酯,后两者经碱中和处理后重新生成瑞舒伐他汀及瑞舒伐他汀非对映异构体,且瑞舒伐他汀钙片在pH1.0盐酸溶液中溶出速率最慢。结论瑞舒伐他汀钙在pH1.0盐酸溶液中溶出曲线可作为处方筛选的依据。 Objective To establish the dissolution method of rosuvastatin calcium tablets. Methods Column: Agilent Extend C18 (4.6×250 mm, 5 μm), eluted with acetonitrile and 0.02% TFA in gradient mode. The ratio ofacetonitrile kept 37% in 13 rain and increased to 90% from 13--27 min at a flow rate of 1.0 mL·min-1 when the detective wavelength was set at 242 nm, plus the rosuvastatin and (3S, 5S)-rosuvastatin calcium peak area to calculate the cumulative release amount (%). Results Rosuvastatin calcium was instabile in pH 1.0 hydrochloric acid solution and degraded to (3S, 5S) -rosuvastatin calcium, rosuvastatin-5S-lactone and rosuvastatin-5R-lactone, when treated with alkali and regenerated to rosuvastatin and (3S, 5S)-Rosuvastatin calcium, also the dissolution profile of rosuvastatin calcium tablets in pH1.0 hydrochloric acid solution was the slowest one. Conclusion The dissolution profile of rosuvastatin calcium tablets in pH 1.0 hydrochloric acid solution can be used as the basis for formulation screening.
出处 《中国药物警戒》 2014年第10期596-600,共5页 Chinese Journal of Pharmacovigilance
关键词 瑞舒伐他汀钙 瑞舒伐他汀钙非对映异构体 溶出度 累积溶出量(%) 校正因子 rosuvastafin calcium (3S, 5S)-rosuvastafiaa calcium dissolution cumulative release amount (%) correction factor
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  • 1蔡伟,赵文镜,罗永慧.高效液相色谱法测定瑞舒伐他汀钙及其片剂的含量[J].江苏药学与临床研究,2006,14(2):97-100. 被引量:4
  • 2Steven PJ, Michael FG, David MR. Direct vascular and cardioprotective effects of rosuvastatin, a new HMG-CoA reductase inhibitor[J]. JACC, 2002,40(6): 1172.
  • 3Kathalijne AO, Timothy SI, Elizabeth T, etal. Application of micro- bore HPLC in combination with tandem MS for the quantification of rosuvastatin in human plasma[J]. Journal of Chromatography B, 2006, 832: 191.
  • 4国家药典委员会编.中国药典[s].北京:中国医药科技出版社,2010,194.
  • 5Kentaro HK,Teruyuki IO,Haruo KK,et al. Pyridine derivatives[P].USP:5260440,1993:11~19.
  • 6H.科伊克,M.卡巴基,N.P.泰勒,等.(E)6-{2-[4-(4-氟苯基)-6-异丙基-2-(甲基(甲磺酰基)氨基]嘧啶-5-基]-乙烯基}(4R,6S)-2,2-二甲基[1,3]二氧杂-4-基)乙酸叔丁酯的制备方法[P].CN:1340052A,2002,3~13.
  • 7Toshiro Konoike,Yoshitaka Araki.Practical synthesis of chiral synthons for the preparation of HMG-CoA reductase inhibitors[J].J Org Chem,1994,59(25),7849~7854.
  • 8Fazli Nasir, Zafar Iqbal, Abad Khan, et al. Simultaneous determination of timolol maleate, rosuvastatin calcium and diclofenac sodium in pharmaceuticals and physiological fluids using HPLC-UV CJ).Journal of Chromatography B, 879(30):3434-3443.
  • 9吕晓东,贡联兵.瑞舒伐他汀[J].中国新药杂志,2002,11(8):650-651. 被引量:17

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