对乙酰氨基酚片的溶出速率及生物利用度研究

Relationship between dissolution rate and bioavailability of paracetamol tablet

目的研究对乙酰氨基酚片的溶出速率与人体相对生物利用度,并探讨二者之间的关系。方法按药典方法测定对乙酰氨基酚片的溶出速率,用紫外分光光度法测定尿液中的对乙酰氨基酚浓度,以25名男性健康志愿者为实验对象,测定其相对生物利用度,并考察二者之间的线性关系。结果5种对乙酰氨基酚片的溶出度均符合药典规定,15 min溶出百分率分别为100.43±2.61、99.76±1.97、96.47±3.52、89.58±1.85、85.85±1.83,相对生物利用度分别为86.34±10.06、85.82±11.21、87.10±10.86、81.71±12.34、76.53±11.73,二者之间呈明显的线性相关关系,回归方程为y= 0.6122x+25.175,r= 0.9642。结论可通过对乙酰氨基酚片的体外溶出速率的测定来反映其生物利用度。

Objective To investigate the relationship between the dissolution rate and bioavailability of paracetamol tablets. Methods The dissolution rate of paracetamol tablet was determined according to methods described in the Pharmacopoeia of the People's Republic of China. Ultraviolet spectrophotometry was employed to measure urine concentration of paracetamol, and the relative bioavailability was determined in 25 male healthy volunteers, with the relationship between the dissolution rate and bioavailbility of paracetamol assessed. Results The 15-min dissolution rates of 5 kinds of paracetamol tablets were 100.43±2.61, 99.76±1.97, 96.47±3.52, 89.58±1.85, and 85.85±1.83 respectively, with their bioavailability of 86.34±10.06, 85.82±11.21, 87.10±10.86, 81.71±12.34, and 76.53±11.73 respectively, showing obvious linear relationship between them, which conformed to the equation y= 0.6122x+25.175, r= 0.9642. Conclusion As there is a good linear relationship between the dissolution rate and bioavailability of paracetamol tablets, the latter parameter can be derived from the measurement of the former.