黄芩苷温敏凝胶在家兔体内的药动学研究

摘要

OBJECTIVE: To study of Baicalin thermosensitive hydrogel in rabbits after rectal administration. METHODS: Rabbits were given Baicalin thermosensitive hydrogel and water-solubility suppository respectively. Drug concentrations in serum were measured by HPLC. The determination was performed on Shim-pack VP-ODS C18(150 mm×4.6 mm, 5μm) column with mobile phase consisted of methanol-water-phosphoric acid (47: 53: 0.2, V/V/V) at the flow rate of 0.8 mL · min-1. The column temperature was 40 ℃ and injection volume was 10 μL. The detection wavelength was set at 274 nm. RESULTS: The main pharmacokinetic parameters of 2 kinds of preparations were as follows:Cmax: (3.639 ± 0.23) μg-L-1 and (2.832 ± 0.18) μg·L-1; AUCo— (796.46 ± 65,35) μg·h·L-1 and (493.86 ±42.52) μg·h·L-1. Compared with water-solubility suppository,Cmax and AUC0→∞ increased after rectal administration, there was significant difference. Relative bioavailability was 161.2%. CONCLUSION: The bioavailability of Baicalin thermosensitive hydrogel is improved significantly with rectal administration.%目的:研究黄芩苷温敏凝胶直肠给药后在家兔体内的药动学.方法:家兔经直肠分别给予黄芩苷温敏凝胶剂和水溶性栓剂,采用高效液相色谱法检测血清中的药物浓度,色谱柱为Shim-pack VP-ODS C18(150 mm×4.6 mm,5μm),流动相为甲醇-水-磷酸(47∶53∶0.2,V/V/V),流速为0.8 mL·min-1,柱温为40℃,进样量为10 μL,检测波长为274 nm.结果:黄芩苷温敏凝胶与黄芩苷水溶性栓剂主要药动学参数Cmax分别为(3.639±0.23)和(2.832±0.18)μg· L-1;AUC0～∞分别为(796.46±65.35)和(493.86±42.52)μg·h· L-1.与水溶性栓剂比较,黄芩苷温敏凝胶直肠给药后,Cmax和AUC0～∞均有增加,且有显著性差异,其相对生物利用度为161.2％.结论:黄芩苷制成温敏凝胶直肠给药后,生物利用度显著提高.