褪黑素口腔崩解片与普通片在犬体内药动学研究

 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ρ_max分别为(52.2±23.0)和(37.8±22.7)μg·L^-1;t_max分别为(0.37±0.10)和(0.56±0.17)h;AUC_0-6分别为(45.52±32.39)和(43.46±29.42)μg·h·L^-1;t_1/2分别为(1.05±0.76)和(1.13±0.52)h;口崩片的相对生物利用度F_0-6和F_{0-∞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。}

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

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:ρ_max(52.2±23.0) and(37.8±22.7) μg·L^-1,t_max(0.37±0.10)and(0.56±0.17)h,AUC_0-6(45.52±32.39) and(43.46±29.42) μg·h·L^-1,t_1/2(1.05±0.76) and(1.13±0.52)h.The relative bioavailability F_0-6 was(106.91±17.30)% and F_0-∞ 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.