复方左旋多巴微囊漂浮片质量标准的研究

The study on quality standard of compound levodopa microcapsule floating tablets

目的初步建立复方左旋多巴微囊漂浮片的质量标准。方法随机抽检10批微囊漂浮片,考察微囊漂浮片的性状、重量差异、起漂时间与持续漂浮时间、释放度。建立同时测定微囊漂浮片中左旋多巴与苄丝肼含量HPLC测定方法。结果初步建立了符合制剂特点的性状、鉴别标准。片重差异在±5%以内,符合药典规定。微囊漂浮片应在1 s内起漂,持续漂浮时间〉12 h。规定微囊漂浮片2、6、12 h的盐酸苄丝肼累积释放量分别为10%~20%、40%~60%、90%~100%,左旋多巴的累积释放量分别为15%~25%、25%~40%、90%~100%。测定微囊漂浮片中左旋多巴与苄丝肼含量HPLC条件为：色谱柱：Agilent ZORBAX SB-C18柱（250 mm×4.6 mm,5μm）;流动相：三氟乙酸-甲醇-水（1∶20∶1 000）;流速：0.5 m L/min;检测波长：220 nm;进样量：20μL;柱温：30℃。结合10批测定结果,初步规定微囊漂浮片中盐酸苄丝肼的含量限度为（100±5）%,左旋多巴的含量限度为（100±5）%。结论该质量控制体系简单、可行,可用于复方左旋多巴微囊漂浮片的质量控制。

Objective To set up the quality standard of compound levodopa microcapsule floating tablets. Methods The appearance,tablets weight difference,drift time,floating time and dissolution rate were evaluated. The content of levodopa and benserazide in the microcapsule floating tablets were determined by HPLC at the same time. Results The characteristics and identification criteria of the characteristics of the floating tablets were preliminarily established. The weight difference of the tablets was within 5%,and was in accordance with the Pharmacopoeia. The floating tablets should be floating in 1s,and the floating time should be more than 12 h. At 2h,6h and 12 h,the cumulative release amount of Benserazide Hydrochloride in microcapsule floating tablets was 10% to20%,40% to 60%,90 to 100%,and the cumulative release amount of levodopa was 15% to 25%,25% to40%,90% to 100%. The HPLC conditions,which were used to determine the contents of levodopa and benserazide in microcapsule floating tablets and was in line with the method requirements,were as following： Agilent Zorbax sb-C18 column（250 mm x 4. 6 mm,5 m） was used,the mobile phase was the mixture of trifluoro acetate and methanol and water（1：20：1 000）,velocity of flow was 0. 5 m L / min,detection wavelength is 220 nm,sample size is 20 μL,and column temperature is 30℃. According to the determination results of 10 batches samples,the content limit of Benserazide Hydrochloride and levodopa were（100 ± 5） % and（100 ± 5） %. Conclusion The system of quality control is simple and feasible,which can be used to control the quality of compound levodopa microcapsule floating tablets.