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作 者:张磊[1] 胡霞[2] 张莉[2] 仲博[2] 陈莉[2] 袁园[2]
机构地区:[1]武警后勤学院附属医院药剂科,天津300162 [2]武警后勤学院药剂学教研室,天津300162
出 处:《中国药房》2012年第47期4446-4448,共3页China Pharmacy
基 金:武警医学院科研课题资助
摘 要: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-packVP-ODSC1(8150mm×4.6mm,5μm),流动相为甲醇-水-磷酸(47∶53∶0.2,V/V/V),流速为0.8mL·min-1,柱温为40℃,进样量为10μL,检测波长为274nm。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。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; AUC0~∞(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.
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