阿西美辛缓释片人体相对生物等效性

Bioequivalence of acemetacin sustained release tablet and sustained release capsule in healthy volunteers

目的 :对自制制剂阿西美辛缓释片和参比制剂缓释胶囊进行人体生物等效性评价。方法 :10名健康志愿者采用自身对照给药方案 ,单剂量、多剂量口服阿西美辛缓释片或缓释胶囊。采用 HPL C法测定阿西美辛及其活性代谢产物吲哚美辛的血药浓度 ,用 3P97计算机程序求算药物动力学参数 ,并进行生物等效性评价。结果 :阿西美辛缓释片、缓释胶囊的主要药物动力学参数 T1 /2 分别为 :(9.349± 2 .0 49)和 (8.130± 2 .2 5 3) h,tmax分别为 :(3.70 0± 0 .483)和 (3.6 0 0± 0 .5 16 ) h,cmax分别为 :(1.0 6 7± 0 .12 4)和 (1.0 86± 0 .12 2 ) ︼g/ m l,AU C0→ 2 4分别为 :(8.0 5 5± 1.35 0 )和 (7.981± 1.30 6 ) h· ︼g/ m l,阿西美辛缓释片的相对生物利用度为 (10 2 .7± 2 5 .6 ) %。结论 :经双单侧 t检验结果显示两种制剂生物等效。

AIM: To study the bioequivalence of self prepared sustained release tablets and available sustained release capsules of acemetacin in 10 healthy male volunteers. METHODS: A single oral dose and multiple oral dose were given to 10 volunteers in the randomized crossover studies. Concentration of metabolite indometacin of acemetacin was determined by high performance liquid chromatography (HPLC) method. All data were analyzed by 3P97 computer program. RESULTS: The pharmacokinetic parameters of the test drug and reference drug were as follows T 1/2 :(9 349±2 049) and (8 130±2 253) h, t max :(3 700±0 483) and (3 600±0 516) h, c max :(1 067±0 124) and (1 086±0 122) μg/ml, AUC 0→24 :(8 055±1 350) and (7 981±1 306) μg·h/ml, respectively. Relative bioavailability of acemetacin sustained release tablet was (102 7±25 6)%. CONCLUSION: The results of two one side tests show that 2 formulations are bioequivalent.