吲哚美辛缓释胶囊单剂量与多剂量达稳态时的相对生物利用度

Study on relative bioavailability of sustained release indomathacin capsule single dose and in steady state of multiple dose

采用反相高效液相色谱法测定１１名健康志愿受试者单剂量口服７５ｍｇ和多剂量口服吲哚美辛缓释胶囊和吲哚美辛片后，吲哚美辛血药浓度变化情况。测得单剂量口服７５ｍｇ吲哚美辛缓释胶囊与吲哚美辛片的达峰时间分别是４．０ｈ与１．５ｈ，峰浓度分别是１．０２μｇ·ｍｌ－１与３．７μｇ·ｍｌ－１，吲哚美辛缓释胶囊的相对生物利用度为１０２％。测得多剂量口服吲哚美辛缓释胶囊与吲哚美辛片达稳态后的Ｃｍｉｎ分别是０．２０８μｇ·ｍｌ－１与０．２６３μｇ·ｍｌ－１，Ｃｍａｘ分别是１．２６μｇ·ｍｌ－１与１．２２６μｇ·ｍｌ－１，Ｔｍａｘ分别为２．７７ｈ与１．８２ｈ，ＦＩ分别是１４０．８１％与１２８．２１％。以ＡＵＣ为指标，经统计分析，吲哚美辛缓释胶囊与吲哚美辛片在单剂量和多剂量达稳态时是生物等效制剂。

The plasma concentration of indomathacin were determined by a HPLC in 11 volunteers after oral administration 75mg sustained release indomathacin capsule (capsule) or indomathacin tablets (tablet) in single dose and in multiple dose. T max of capsule and tablets were 4.0h and 1.5h , C max were 1.019 μg·ml -1 and 3.662 μg·ml -1 respectively in single dose. The relative bioavailability of capsule was 102.38% . C min in steady state of capsule and tablets were 0.208 μg·ml -1 and 0.263 μg·ml -1 , C max were 1.262 μg·ml -1 and 1.226 μg·ml -1 , T max were 2.77h and 1.82h and FI were 140.81% and 128.21% respectively. The results of statistical analysis showed that capsule and tablets was bioequivalence in single dose and in steady state of multiple dose after oral administation.