摘要
目的:建立一种灵敏的HPLC测定氯雷他定血药浓度的方法,以评价氯雷他定片的相对生物利用度?方法:固定相μBondapak C18,流动相为甲醇-乙腈-0.01mol·L-1 pH7.5磷酸盐缓冲液(35∶35∶30),内标为盐酸萘唑啉,检测波长为275nm;12个健康志愿者采用交叉给药进行氯雷他定片的生物利用度评价?结果:HPLC测定的线性范围为0.2～30ng·ml-1;最低检测浓度为0.1ng·ml-1;方法回收率为97.39%～103.96% ?人体生物利用度试验结果表明,试验片与对照片间的AUC,tmax,cmax和t1/2β无显著性差异(P>0.05),相对生物利用度为(105.60±20.76)%(n=12)?AUC经单双侧t检验示为生物等效?结论:两种制剂生物等效?
Abstract
OBJECTIVE:To establish a sensitve HPLC method for the determination of loratadine in plasma and to evaluate its bioavailability.METHODS:A HPLC system consisted of a μBondapak C18 column and a mobile phase of methanol-acetone-0.01mol·L-1 phosphate buffer (pH7.5)(35∶35∶30).The detector was set to 275nm.Naphthozoline hydrochloride was selected as an internal standard.A crossover relative bioavilability study for two loratadine tablets was carried out in 12 healthy volunteers.RESULTS:The HPLC method had a linearity over the range of 0.2～30ng·ml-1.The limit of quantity was 0.1ng·ml-1.The average recoveries varied from 97.39%～103.96%.The results showed that AUC,cmax,tmax and t1/2β of two formulations had no significant difference (P>0.05).Relative bioavailability was (105.60±20.76)% (n=12).CONCLUSION:Two formulations of loratadine were bioequivalent.
关键词
氯雷他定 /
生物利用度 /
高效液相色谱法
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Key words
loratadine /
bioavailability /
HPLC
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江志强;蒋新国;奚念朱;陈桂良;刘倩;张顺妹.
氯雷他定血药浓度HPLC测定方法建立和生物利用度[J]. 中国药学杂志, 1999, 34(11): 757-759
Jing Zhiqing.
Determination of loratadine in human plasma by a sensitive HPLC method and evaluation of its bioavailability[J]. Chinese Pharmaceutical Journal, 1999, 34(11): 757-759
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参考文献
1 Batenhorst R，Batenhorst A，Graves D，et al．Pharmacologic evaluation of loratadine (SCH 29851)，chlorpheniramine and placebo．Eur J Clin Pharmacol，1986，3l：247．
2 Barnett A，Iorio LC，Kreutner S，et al．Evaluation of the CNS properties of SCH 29851，a potential non-sedating antihistadine．Agents Actions，1984，14：590．
3 Hibert J，Radwanski E，Weglein R，et al．Pharmacokinetics and dose proportionality of loratadine．J Clin Pharmacol，1987，27： 694．
4 Johnson R，Christensen J，Lin CC．Sensitive gas-liquid chromatogrphic method for the determination of loratadine and itS major active metabolite，descarboethoxyloratadine，in human plsasma using a nitrogen-phosphorus detector．J Chromatogr B，1994，657：125．
5 Holeman JA．Danielson ND．Liquid chromatography of antihistamines using post-column tris (2，2’-bipyridine) ruthenium Ⅲ chemiluminescence detection．J Chromatogr A，1994，679：277．
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脚注
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