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目的:研究维胺酯软胶囊与硬胶囊的人体相对生物利用度。方法:采用反相高效液相色谱法测定10名男性健康志愿者随机单剂量po维胺酯硬胶囊150mg(25mg×6粒)和软胶囊100mg(5mg×20粒)后,药物在体内的经时过程。结果:药物制成软胶囊后,药物的吸收相和消除相无明显改变,但可以显著提高口服维胺酯的生物利用度,软胶囊与硬胶囊的t1/2ka分别为(1.457±0.508)h和(1.349±0.482)h,t1/2ke分别为(2.378±0.871)h和(2.744±1.097)h,tmax分别为(2.612±0.778)h和(2.649±0.700)h,cmax分别为(17.496±8.992)μg·L-1和(16.031±7.732)μg·L-1,体内平均驻留时间(MRT)分别为(3.618±0.540)h和(3.728±0.379)h,AUC分别为(93.467±54.148)μg·h·L-1和(89.658±45.814)μg·h·L-1。其相对生物利用度为(169.41±29.08)%。结论:软胶囊与硬胶囊相比具有较高的生物利用度
OBJECTIVE: To study the relative bioavailability of human retinamide capsules and hard capsules. Methods: Ten male healthy volunteers were randomly divided into two groups: normal control group (n = 10), normal control group (n = 10) When the process. Results: After the drug was made into soft capsules, the absorption and elimination phases of the drug did not change obviously, but the bioavailability of oral administration of retinamide could be significantly improved. The t1 / 2ka of soft capsule and hard capsule were (1.457 ± 0 .508) h and (1.349 ± 0.482) h, t1 / 2ke were (2.378 ± 0.871) h and (2.744 ± 1.097) h respectively, tmax were (2.612 ± 0.778) h and (2.649 ± 0.700) h respectively, and the values of cmax were (17.496 ± 8.992) μg · L-1 and (16.031 ± 7.732) μg · L-1 (3.618 ± 0.540) h and (3.728 ± 0.379) h, respectively, and the AUC values were (93.467 ± 54.148) μg · h · L -1 and (89.658 ± 45.814) μg · h · L-1, respectively. The relative bioavailability was (169.41 ± 29.08)%. Conclusion: Soft capsules have higher bioavailability than hard capsules