Parrott E L
J Pharm Sci. 1975 May;64(5):875-80.
The rectal absorption of aspirin from theobroma oil suppositories was studied in seven human subjects using urinary excretion measurements. The effect of particle size on the excretion rate and cumulative amount of total salicylate excreted was demonstrated by the administration of a 600-mg dose as powdered aspirin and as aspirin disks having 0.023 as much surface as powdered aspirin. In vitro dissolution profiles of aspirin from the suppositories were studied. By the NF XIII Method II, the time required for 50% of the aspirin to dissolve from the suppository was 50 and 100 min for the powdered aspirin and the aspirin disks, respectively. In the bioavailability study, the diffusion equilibrium was attained at approximately 4-5 and 9-10 hr after the rectal administration of powdered aspirin and aspirin disks, respectively. No correlation was found between bioavailability and the dissolution profiles as determined by the USP XVIII dissolution method.
采用尿排泄量测定法，在7名人体受试者中研究了可可脂栓剂中阿司匹林的直肠吸收情况。通过给予600毫克剂量的粉末状阿司匹林和表面积仅为粉末状阿司匹林0.023倍的阿司匹林片，证明了粒径对总水杨酸排泄速率和累积排泄量的影响。研究了栓剂中阿司匹林的体外溶出曲线。采用美国国家处方集（NF）XIII方法II，粉末状阿司匹林和阿司匹林片的栓剂中分别有50%的阿司匹林溶解所需时间为50分钟和100分钟。在生物利用度研究中，分别在直肠给予粉末状阿司匹林和阿司匹林片后约4 - 5小时和9 - 10小时达到扩散平衡。通过美国药典（USP）XVIII溶出度方法测定的生物利用度与溶出曲线之间未发现相关性。
