盐酸左氧氟沙星片的溶出行为评价  

Evaluation of Dissolution Behavior for Levofloxacin Hydrochloride Tablets

作　　者：吴静萍 WU Jing-ping(Fujian Institute for Food and Drug Quality Control,Fujian Fuzhou 350001,China)

机构地区：[1]福建省食品药品质量检验研究院,福建福州350001

出　　处：《中国药物评价》2024年第2期115-119,共5页Chinese Journal of Drug Evaluation

摘　　要：目的:考察7家企业盐酸左氧氟沙星片的溶出行为,并评价其与参比制剂溶出行为的一致性。方法:采用桨法,转速50 r·min^(-1),以pH 1.2盐酸溶液、pH 4.5醋酸盐缓冲液、pH 6.8磷酸盐缓冲液及水为溶出介质,体积900 mL,采用HPLC法测定溶出量,用f 2因子法评价溶出曲线的相似性,并结合含量、有关物质、硬度、晶型、结晶度及稳定性等相关因素分析。结果:有3家企业产品的溶出行为与参比一致,其余产品与参比的溶出行为差异显著,表现出较低的溶出速率,该部分产品与原料药相比均存在转晶现象,且结晶度不佳。结论:盐酸左氧氟沙星片的生产工艺对晶型影响较大,多晶型本身的表观溶解度和溶解速率差异,对制剂的溶出产生滞后影响,提示相关企业应合理优化工艺、重点关注其转晶行为。Objective:To investigate the dissolution curves of levofloxacin hydrochloride tablets from 7 manufacturers and the reference preparation.Methods:The dissolution behaviors were detected using 900 mL of pH 1.2 hydrochloric acid solution,pH 4.5 acetate buffer solution,pH 6.8 phosphate buffer solution and water under the slurry method at the rotational speed of 50 r·min^(-1),HPLC was used for detecting cumulative dissolution,and the consistency was evaluated by the similarity factor(f 2).Content,related substances,hardness,crystal form and stability were analyzed to interpret the results.Results:The products from 3 manufacturers were all in line with the reference in the dissolution curve similarities,while the other products showing differences from the reference preparation.The dissolution rate of levofloxacin hydrochloride tablets was lower,the probable cause was crystal form transformation.Conclusion:The production process of levofloxacin hydrochloride was closely related to the crystal form,differences of intrinsic dissolution rate and dissolution rate of tablets between various polymorphic forms were confirmed.Crystal form transformation of the production process should be fully considered.

关 键 词：盐酸左氧氟沙星片 溶出行为 溶出曲线 一致性 转晶 

分 类 号：R927.11[医药卫生—药学]