Lui C Y, Oberle R, Fleisher D, Amidon G L
J Pharm Sci. 1986 May;75(5):469-74. doi: 10.1002/jps.2600750510.
The bioavailability of enteric coated and plain aspirin tablets was studied in four beagle dogs. Blood sampling for enteric coated tablets was planned with the aid of a radiotelemetric system. The release of aspirin from its dosage form was detected by monitoring the change in intestinal pH. Aspirin and salicylic acid levels in plasma obtained from the enteric coated dosage form exhibited familiar concentration versus time absorption profiles. Variation in the plasma concentrations of these two compounds within each dog studied (four runs each) was relatively small when time zero was adjusted to the commencement of tablet dissolution. The plasma levels obtained from plain aspirin (three runs each), however, show atypical absorption. The estimated absolute bioavailability was 0.432 +/- 0.0213 and 0.527 +/- 0.0260 for enteric coated and plain aspirin, respectively. Other pharmacokinetic parameters for these two dosage forms such as the highest observed plasma concentration (Cmax) (10.9 +/- 0.535 microgram/mL versus 13.6 +/- 1.88 micrograms/mL) and the time to reach Cmax (tmax) (26.6 +/- 1.94 min versus 31.0 +/- 7.04 min) agree well. The mean values for gastric emptying time, in vivo coating dissolution time, and in vivo disintegration/dissolution time of the tablet core for enteric coated aspirin are 48.7 +/- 7.23 min, 44.3 +/- 3.80 min, and 34.7 +/- 2.04 min, respectively.
在四只比格犬身上研究了肠溶包衣阿司匹林片和普通阿司匹林片的生物利用度。借助无线电遥测系统对肠溶包衣片进行采血计划。通过监测肠道pH值的变化来检测阿司匹林从其剂型中的释放情况。从肠溶包衣剂型获得的血浆中阿司匹林和水杨酸水平呈现出常见的浓度-时间吸收曲线。当将零时间调整为片剂溶解开始时,在所研究的每只犬(每只进行四次试验)体内这两种化合物的血浆浓度变化相对较小。然而,从普通阿司匹林(每只进行三次试验)获得的血浆水平显示出非典型吸收。肠溶包衣阿司匹林和普通阿司匹林的估计绝对生物利用度分别为0.432±0.0213和0.527±0.0260。这两种剂型的其他药代动力学参数,如最高观察到的血浆浓度(Cmax)(分别为10.9±0.535微克/毫升和13.6±1.88微克/毫升)以及达到Cmax的时间(tmax)(分别为26.6±1.94分钟和31.0±7.04分钟)也很吻合。肠溶包衣阿司匹林的胃排空时间、体内包衣溶解时间和片剂核心的体内崩解/溶解时间的平均值分别为48.7±7.23分钟、44.3±3.80分钟和34.7±2.04分钟。