左乙拉西坦片仿制药与原研药溶出度一致性评价

Consistency Evaluation of Dissolubility of Generic and Original Preparation of Levetiracetam Tablets

目的建立测定左乙拉西坦片体外溶出曲线的方法,评价仿制药与原研药溶出度的一致性。方法按2015年版《中国药典(四部)》通则0931第二法,采用高效液相色谱法测定溶出曲线,色谱柱为Agilent Eclipse XBD-C18柱(150 mm×4.6 mm,5μm),流动相为0.2%磷酸氢二钾溶液-乙腈(950∶50,V/V,用稀磷酸调节p H值至6.0),流速为1.0 m L/min,检测波长为205 nm,柱温为30℃,进样量为20μL;溶出介质分别为500 m L水、pH1.0盐酸溶液、p H4.5醋酸盐缓冲液、pH6.8磷酸盐缓冲液,温度为(37±0.5)℃,转速为75 r/min。结果在4种不同pH溶出介质中,15 min时样品累积溶出度均大于85%,属快速溶出,可判定仿制药与原研药溶出曲线基本相似。结论左乙拉西坦仿制药与原研药的体外溶出行为一致。

Objective To establish a method for the determination of the dissolution profile of Levetiracetam Tablets in vitro,and to evaluate the consistency of the dissolubility of generic and original preparations.Methods According to the second dissolution method(paddle method)in general rule 0931 of Chinese Pharmacopoeia(2015 Edition,Volume Ⅳ),the dissolution profile of Levetiracetam Tablets was determined by the HPLC method,the chromatographic column was Agilent Eclipse XBD-C18 column(150 mm×4.6 mm,5μm),the mobile phase was 0.2% dipotassium hydrogen phosphate-acetonitrile(950∶50,V/V,the pH was adjusted to 6.0 with clilute phosphoric acid),the flow rate was 1.0 m L/min,the detection wavelength was 205 nm,the column temperature was 30℃,and the injection volume was 20μL.The dissolution media were 500 m L water,ph 1.0 hydrochloric acid solution,p H 4.5 acetate buffer solution,pH6.8 phosphate buffer solution,the temperature was(37±0.5)℃and the rotation speed was 75 r/min.Results In four different p H dissolution media,the cumulative dissolution rate of the sample at 15 min was more than 85%,which was a rapid dissolution.It could be judged that the dissolution profiles of the generic preparations were similar to the original ones.Conclusion The in vitro dissolution behavior of generic Levetiracetam Tablets is consistent with that of the original ones.