阿司匹林淀粉微球在兔体内的药动学

Pharmacokinetics of aspirin-carrying starch microspheres in rabbit as nasal administration

目的 :通过对阿司匹林淀粉微球在兔体内药动学研究 ,以评价淀粉微球作为鼻腔给药系统的应用价值及作用。方法 :取 12只家兔随机分为两组 ,分别进行鼻腔微球给药和口服片剂给药 ,采用反相高效液相色谱法测定家兔血浆中水杨酸的浓度 ,并用 3P87程序软件处理 ,用t检验法进行显著性检验。结果 :鼻腔给药的吸收半衰期长于口服给药 ,相对生物利用度达134 .4%,结论 :淀粉微球作为鼻腔给药系统 ,能提高药物的吸收 。

OBJECTIVE Starch microspheres were investigated as a nasal delivery system in rabbits using aspirin as a model drug. METHODS The fate of salicylic acid in the plasma of rabbits was followed after nasal and oral administration of 5.0 mg·kg -1 doses of aspirin. Salicylic acid in plasma was determinated by RP HPLC with UV detection. The concentration time data were fitted using 3P87 pharmacokinetic program and the pharmacokinetic parameters were compared by t test.RESULTS The detection limit was 0.1 μg·ml -1 .The concentration time curve fitted one compartment model in rabbits. The relative bioavailability of aspirin following nasal administration was 134.4% .CONCLUSIONS It was found that the combination of aspirin with the microspheres delivery system increased the uptake of the drug across the nasal membrane.