Tanigawara Y, Yamaoka K, Nakagawa T, Uno T
J Pharm Sci. 1982 Oct;71(10):1129-33. doi: 10.1002/jps.2600711013.
The in vivo disintegration, dissolution, absorption, and disposition processes of ampicillin products are separated by means of moment analysis. This method is model-independent, that is, any specific model is not assumed. The mean residence time (MRT), mean absorption time (MAT), mean dissolution time (MDT), and mean disintegration time (MDIT) are calculated for several dosage forms of ampicillin. The fraction of dose absorbed (F) is also separated into several fractions corresponding to these in vivo processes. Bioavailability and bioequivalence are discussed in terms of the zero and first moments. The flip-flop behavior of ampicillin is proved by the fact that the MRT following intravenous injection is less than the MAT of any oral dosage form. Absorption of released ampicillin is proved by the fact that the MRT following intravenous injection is less than the MAT of any oral dosage form. Absorption of released ampicillin is proved to be a rate-determining step, since the MRT of released ampicillin in the GI tract is the greatest of all MRT corresponding to the in vivo processes. Moment analysis is compared with classical compartment theory, and a new component concept is introduced.
通过矩量分析来分离氨苄西林产品的体内崩解、溶解、吸收和处置过程。该方法不依赖于模型,即不假定任何特定模型。计算了几种氨苄西林剂型的平均驻留时间(MRT)、平均吸收时间(MAT)、平均溶解时间(MDT)和平均崩解时间(MDIT)。吸收剂量分数(F)也被分离为对应于这些体内过程的几个分数。从零阶矩和一阶矩的角度讨论了生物利用度和生物等效性。静脉注射后的MRT小于任何口服剂型的MAT,这一事实证明了氨苄西林的翻转行为。释放的氨苄西林的吸收也通过静脉注射后的MRT小于任何口服剂型的MAT这一事实得到证明。由于释放的氨苄西林在胃肠道中的MRT在所有对应于体内过程的MRT中是最大的,因此释放的氨苄西林的吸收被证明是一个速率决定步骤。将矩量分析与经典房室理论进行了比较,并引入了一个新的组分概念。