左氧氟沙星薄膜衣片的制备及其质量评价

The Quality and Preparation of Levofloxacin Film-Coated Tablets

自研制剂和原研制剂的质量一致可以较大程度地保证二者临床效果一致。因此,以颗粒成型、脆碎度、体外溶出度等为评价指标,通过试验对润湿剂种类、填充剂和崩解剂、润滑剂、粘合剂和包衣粉等辅料的用量进行筛选及优化自研制剂的处方。经试验选择最优处方:左氧氟沙星512.5mg、微晶纤维素70mg、羧甲纤维素钙30mg、羟丙纤维素3.75mg、硬脂富马酸钠27mg。包衣增重选择3~5%范围。对优选处方制备的薄膜衣片进行质量检查,并与原研制剂进行对比,在磷酸盐缓冲(pH6.8)溶液、盐酸溶液(pH1.0)以及水和醋酸盐缓冲(pH4.5)溶液这四种不同的溶出介质中,自研产品和原研产品都可以15min达到85%以上的溶出度,具有相似的溶出行为;且它们的晶体结构和含量都是一致的。此外,经过6个月的稳定性加速试验,这些产品的检测结果没有发生任何明显的改变。证明自研左氧氟沙星片的处方及工艺稳定可行,与原研制剂具有质量一致性。

The consistency of the quality between the self-crafted and original preparations can ensure the clinical effect of the two preparations to a greater extent.Therefore,the particle forming,fragility,and in vitro dissolution was used as the evaluation indicators,the prescription of self-developed formulations by screened and optimized experiments of the types of wetting agents,fillers and disintegrants,lubricants,adhesives,and coating powders.The optimum prescription of levofloxacin film-coated tablet contained Levofloxacin 512.5mg,microcrystalline cellulose 70mg,calcium carboxymethyl cellulose 30mg,hydroxypropyl cellulose 3.75mg and sodium stearate 27mg.Coating material 3-5%was the optimal weight of levofloxacin tablets.Conduct quality inspection on the film coated tablets prepared by the selected prescription and compare them with the original research formulation,the self-developed drug and reference listed drug,when dissolved in four media-phosphate buffer solution(pH 6.8),hydrochloric acid(pH 1.0),acetate buffer solution(pH 4.5),and water-all had dissolution rates higher than 85%for 15 minutes,suggesting a similar dissolution behavior.Same crystal form and content;there was no significant change in the sample control indicators after 6 months of accelerated tested compared to 0 days.It is proved that the formulation and technology of self-developed levofloxacin tablets are stable and feasible,and the quality was consistent with the original preparation.