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目的 :以单硝酸异山梨酯 ( 5 ISMN)普通片为参比制剂 ,研究 5 ISMN控释胶囊的药代动力学性质和相对生物利用度。方法 :采用自身对照法 ,12名健康志愿者分别单剂量和多剂量口服控释胶囊与对照片 ,采用正相高效液相色谱法测定血药浓度变化情况。结果 :单剂量口服 5 0mg控释胶囊与 4 0mg片剂的AUC分别为 ( 95 94 .4 6± 15 90 .18) ,( 72 5 1.79± 1181.4 6)ng·h/ml,Cmax分别为 ( 5 63 .5 0± 10 1.0 5 ) ,( 819.80± 12 7.99)ng/ml,Tmax分别为( 6.3 0± 0 .67) ,( 1.3 3± 0 .4 8)h ,相对生物利用度为 ( 94 .4 8± 13 .4 3 ) %。多剂量口服 5 ISMN控释胶囊 ( 5 0mg/次 ,qd)其波动度为 ( 118.89± 11.66) % ,以配对t检验与双单侧t检验对上述参数进行统计分析 ,两种制剂的AUC无显著性差异 (P >0 .0 5 ) ,而其他参数有显著性差异 (P <0 .0 5 )。结论 :两种制剂具生物等效性 ,单硝酸异山梨酯控释胶囊具有显著的控释特征。
OBJECTIVE: To study the pharmacokinetics and relative bioavailability of 5 ISMN controlled release capsules with isoniazid mononitrate (5 ISMN) as reference preparation. Methods: The self-control method, 12 healthy volunteers were single-dose and multiple doses of oral controlled release capsules and the control group, the use of normal-phase high performance liquid chromatography determination of plasma concentration changes. Results: The AUC of single oral dose of 50 mg controlled release capsules and 40 mg tablets were (95 94.46 ± 15 90.18) and (72 5 1.79 ± 1181.4 6) ng · h / ml, respectively (63.0 ± 0.67) and (1.3 3 ± 0.48) h, respectively, and the relative bioavailability was (519.0 ± 10 1.05) and (819.80 ± 12 7.99) ng / 94 .4 8 ± 13 .4 3)%. The volatility of multi-dose oral 5 ISMN controlled release capsules (50 mg qd) was (118.89 ± 11.66)%. The above parameters were statistically analyzed by paired t-test and double unilateral t test. The AUC of the two preparations Significant difference (P> 0.05), while other parameters were significantly different (P <0.05). CONCLUSION: The two formulations are bioequivalent and isosorbide mononitrate controlled release capsules have significant controlled release characteristics.