Aliache J M, Briot M, Couquelet J, Vigo P
Eur J Drug Metab Pharmacokinet. 1981;6(3):221-4. doi: 10.1007/BF03189491.
In this preliminary study, using a radioimmunoassay, we demonstrate that the DHET blood levels observed after administration of an oral solution to human subjects, were different from those obtained after administration of a slow-release table. After administration of the oral solution, the DHET blood levels rose quickly, reached a peak between 1 and 2 hours and the decrease rapidly. On the contrary, after ingestion of a slow-release tablet of DHET, the plasma levels took 6 hours to reach the maximum due to the slow release of the drug from this dosage form. In both cases, the areas under the curves were very similar but the relative bioavailability of DHET in these two forms is very different if one considers the two components of availability extent and rate. The equality of the areas under the curves indicated that the extent of DHET available was the same, but time-course of the plasma levels showed that the rate at which DHET became available was significantly slower. Therefore the tablet form has given the desired "slow-release" availability for which it was designed.
在这项初步研究中,我们使用放射免疫分析法证明,给人类受试者服用口服溶液后观察到的DHET血药浓度,与服用缓释片后获得的血药浓度不同。服用口服溶液后,DHET血药浓度迅速上升,在1至2小时之间达到峰值,然后迅速下降。相反,服用DHET缓释片后,由于药物从该剂型中缓慢释放,血浆浓度需要6小时才能达到最大值。在这两种情况下,曲线下面积非常相似,但如果考虑可用性程度和速率这两个组成部分,DHET在这两种剂型中的相对生物利用度非常不同。曲线下面积相等表明可利用的DHET程度相同,但血浆浓度随时间的变化表明DHET的可用速率明显较慢。因此,片剂形式提供了其设计所需的“缓释”可用性。