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目的研究自制溴新斯的明缓释制片与溴新斯的明普通片在兔体内的药动学与相对生物利用度。方法新西兰兔随机分组,自身交叉对照,单剂量口服45 mg溴新斯的明缓释制片或普通片后,采用高效液相色谱法测定血浆中溴新斯的明药物浓度,计算药动学参数和相对生物利用度。结果溴新斯的明缓释片与普通片给药后,药动学参数tmax分别为(7.00±1.09)和(1.58±0.38)h;ρmax分别为(3.42±1.14)和(4.56±1.72)mg.L-1;AUC0-∞分别为(52.97±13.43)和(56.78±12.34)mg.h.L-1;与普通片相比,缓释片的相对生物利用度为(93.3±24.6)%。结论溴新斯的明缓释片tmax明显延后,ρmax降低,有明显的缓释效果,单次给药后的吸收程度与普通片无统计学差异。
Objective To study the pharmacokinetics and relative bioavailability of self-made bromine neostigmine sustained-release tablets and bromine neostigmine tablets in rabbits. Methods New Zealand white rabbits were randomized and crossed with each other. After a single oral dose of 45 mg bromocriptine or conventional tablets, the concentrations of neostigmine in plasma were determined by HPLC. The pharmacokinetics Parameters and relative bioavailability. Results The pharmacokinetic parameters (tmax) were (7.00 ± 1.09) and (1.58 ± 0.38) h, respectively, for bromosus sustained-release tablets and conventional tablets. The values of ρmax were (3.42 ± 1.14) and (4.56 ± 1.72) mg.L-1 and AUC0-∞ were (52.97 ± 13.43) and (56.78 ± 12.34) mg.hL-1, respectively. The relative bioavailability of the sustained release tablets was (93.3 ± 24.6)% compared with the normal tablets. Conclusion The bromocriptine sustained release tablets tmax significantly delayed, ρmax decreased, with a significant sustained release effect, after a single administration of the degree of absorption and conventional tablets no significant difference.