HPLC测定对乙酰氨基酚鼻腔滴剂的人体相对生物利用度

 目的：测定对乙酰氨基酚鼻腔滴剂po对片剂在正常志愿者体内的相对生物利用度。方法：建立了血浆中对乙酰氨基酚的反相高效液相色谱测定法，测定了对乙酰氨基酚鼻腔滴剂与po片剂在正常志愿者体内的药动学参数和血药-时间曲线，并且比较了二者的药动学参数。结果：对乙酰氨基酚鼻腔滴剂吸收速度与po片剂无显著差异，吸收分数高于po片剂，相对生物利用度为121.57%（t_1/2校正后）。结论：对乙酰氨基酚鼻腔吸收效果良好，为其鼻腔给药提供科学证据。

Relative bioavailability of acetaminophen nasal drops in human volunteers by reversed phase HPLC

OBJECTIVE: To study the bioavailabilities of acetaminophen nasal drops relative to oral tablet in human volunteers. METHOD: The concentration of acetaminophen in plasma was determined by reversed phase HPLC to evaluate the absorption of acetaminophen via nasal administration. The chromatographic conditions for determination were as follows: A Waters Model 481 instrument was used, theophylline was shown to be the most suitable internal standard at the wave length of 254 nm, a mixture of redistilled water and methanol (80∶20) was used as the mobile phase with a flow rate of 1 ml·min^-1, and YWG-C₁₈H₃₇as stationary phase. The bioavailability of acetaminophen nasal drops was studied in 8 men relative to oral tablets, at the dose of 250 mg acetaminophen in different preparations administered by cross over method. RESULTS: No significant difference was found between the absorption rate of acetaminophen nasal drop and that of oral tablet. The relative bioavailability was 121.57% (revised with t_1/2). CONCLUSION: Acetaminophen nasal drops presented a higher bioavailability relative to oral tablets, so it may be suitable to be developed as a nasal preparation.