Lin C, Lim J, Symchowicz S
J Int Med Res. 1982;10(2):122-5. doi: 10.1177/030006058201000210.
The objective of this study was to compare in man the bioavailability of d-pseudoephedrine and azatadine from a repeat action tablet formulation and from conventional tablets. The repeat action tablet, containing 1 mg of azatadine maleate in the coat, and 60 mg of d-pseudoephedrine sulfate in both the coat and the core, was given at 0 hour. A conventional tablet of 60 mg of d-pseudoephedrine sulfate was given at 0 and 4 hours and a conventional tablet of 1 mg of azatadine maleate was given at 0 hour. The plasma levels of d-pseudoephedrine were measured by gas-liquid chromatography and the amount of azatadine in the urine was determined by a mass fragmentographic procedure. The results showed that there were no statistically significant differences in the measured bioavailability parameters (area under plasma concentrations-time curve, maximum plasma concentration and time to reach maximum plasma concentration) for pseudoephedrine from repeat action tablets and conventional d-pseudoephedrine sulfate tablets; neither was there any statistically significant difference in the cumulative urinary excretion of azatadine from the repeat action tablets and conventional azatadine maleate tablets (p less than 0.10). These data clearly demonstrate the bioequivalence of the repeat action tablets and the conventional tablets of d-pseudoephedrine and azatadine.
本研究的目的是比较人服用复方长效片剂和普通片剂后右美沙芬和氮卓斯汀的生物利用度。在0小时给予复方长效片剂，其包衣中含有1mg马来酸氮卓斯汀，包衣和片芯中均含有60mg硫酸右美沙芬。在0小时和4小时给予60mg硫酸右美沙芬普通片剂，在0小时给予1mg马来酸氮卓斯汀普通片剂。采用气液色谱法测定血浆中右美沙芬的水平，用质量碎片分析法测定尿液中氮卓斯汀的含量。结果表明，复方长效片剂与普通硫酸右美沙芬片剂中右美沙芬的生物利用度参数（血浆浓度-时间曲线下面积、最大血浆浓度和达最大血浆浓度时间）无统计学显著差异；复方长效片剂与普通马来酸氮卓斯汀片剂中氮卓斯汀的累积尿排泄量也无统计学显著差异（p<0.10）。这些数据清楚地表明了复方长效片剂与普通右美沙芬和氮卓斯汀片剂的生物等效性。
