Ogata H, Shibazaki T, Inoue T, Ejima A
J Pharm Sci. 1979 Jun;68(6):712-5. doi: 10.1002/jps.2600680615.
The relationship between chloramphenicol (I) tablet bioavailability and in vitro dissolution rates was examined. The effect of solid food on the I tablet and powder bioavailability was also studied. Five tablets of I were selected for bioavailability testing on the basis of the dissolution rates of 18 I tablets (250 mg) determined by several methods. Compound I, 500 mg, was administered orally to five subjects, following overnight fasting, according to a crossover design. The bioavailability parameters were obtained from urinary I excretion. Among the five formulations studied, only one tablet (F) showed significantly poorer bioavailability. The dissolution rates at pH 1.2 did not give the same rank order as the bioavailability. The dissolution rate of Tablet F showed remarkable pH dependency. The dissolution rates at pH 4 showed good correlation with in vivo bioavailability data. The bioavailability of I powder was not affected by solid food. Tablet F, which had poor bioavailability in the fasting state, showed good bioavailability when administered just after the standard breakfast.
考察了氯霉素（I）片的生物利用度与体外溶出速率之间的关系。还研究了固体食物对I片和粉末生物利用度的影响。根据用几种方法测定的18片I片（250mg）的溶出速率，选择5片I片进行生物利用度测试。按照交叉设计，在隔夜禁食后，给5名受试者口服500mg化合物I。生物利用度参数通过尿中I的排泄获得。在所研究的5种制剂中，只有1种片剂（F）的生物利用度明显较差。在pH 1.2时的溶出速率排序与生物利用度不同。片剂F的溶出速率表现出显著的pH依赖性。在pH 4时的溶出速率与体内生物利用度数据显示出良好的相关性。I粉末的生物利用度不受固体食物的影响。在禁食状态下生物利用度较差的片剂F，在标准早餐后立即给药时显示出良好的生物利用度。
