褪黑素口腔崩解片与普通片在犬体内药动学研究

Study on Pharmacokinetics of Melatonin Orally Disintegrating Tablets and Common Tablets in Beagle Dogs

目的比较褪黑素口腔崩解片与普通片在Beagle犬体内的药动学参数,计算褪黑素口腔崩解片的相对生物利用度。方法6条Beagle犬单剂量交叉口服褪黑素口腔崩解片和普通片6 mg后,用高效液相色谱法测定血浆药物浓度,用DAS软件计算药动学参数及口崩片的相对生物利用度。结果褪黑素口崩片和普通片在Beagle犬体内的ρmax分别为(52.2±23.0)和(37.8±22.7)μg.L-1;tmax分别为(0.37±0.10)和(0.56±0.17)h;AUC0-6分别为(45.52±32.39)和(43.46±29.42)μg.h.L-1;t1/2分别为(1.05±0.76)和(1.13±0.52)h;口崩片的相对生物利用度F0-6和F0-∞分别为(106.91±17.30)%和(107.62±16.71)%。结论与普通片比较,口崩片吸收更迅速,血药峰浓度高。两种制剂生物不等效。

OBJECTIVE To compare pharmacokinetic parameters of melatonin orally disintegrating tablets and common tablets in Beagle dogs. METHODS The plasma concentrations of melatonin in 6 Beagle dogs were determined by HPLC and the pharmacokinetic parameters were calculated with DAS software after a single dose of 6 mg melatonin common tablets or orally disintegrating tablets. RESULTS The pharmacokjinetic parameters of the orally disintegrating tablets and common tablets of melatonin were as follows ：Pro= （52.2±23.0） and （37.8±22.7） μg·L^-1 ,tmax,（0. 37±0. 10）and（0.56 ±0. 17）h,AUC0-6（45.52 ± 32.39） and （43.46±29.42） μg · h^-1·L^-1 ,t1/2 （ 1. 05 ±0. 76） and （ 1. 13± 0. 52） h. The relative bioavailability F0-6 was （ 106. 91 ± 17.30）% and F0-x was （ 107.62 ± 16. 71 ） %. CONCLUSION Compared with the common tablets , the orally disintegrating tablets showed faster absorption and higher peak concentration. The two preparations are not bioequivalent.