Wu X, Yamashita F, Hashida M
Department of Drug Delivery Research, Graduate School of Pharmaceutical Sciences, Kyoto University, Japan.
Biol Pharm Bull. 1999 Nov;22(11):1212-6. doi: 10.1248/bpb.22.1212.
We have previously proposed a novel deconvolution method, which can estimate first-pass metabolism of orally administered drugs. In the present study, we examined whether this deconvolution method is useful for evaluating oral dosage forms. The absorption and first-pass metabolism of orally administered aspirin formulated in several forms were analyzed. Two types of microcapsules consisting of Eudragit L100 alone and Eudragit L100/ethylcellulose (4:6) were prepared as sustained release formulations, for comparison with aspirin in powder form. The deconvolution analysis revealed that absorption of aspirin was sustained by encapsulating it in microcapsules. Interestingly, it also revealed that the percentage metabolized during absorption was different among the three types of formulations. Thus, the deconvolution method has enabled a comprehensive analysis of orally administered drugs. This method is believed to contribute to the evaluation of oral drug formulations.
我们之前提出了一种新型的反卷积方法,该方法可以估算口服药物的首过代谢。在本研究中,我们考察了这种反卷积方法是否有助于评估口服剂型。分析了以几种形式配制的口服阿司匹林的吸收和首过代谢情况。制备了两种分别由单独的丙烯酸树脂L100和丙烯酸树脂L100/乙基纤维素(4:6)组成的微胶囊作为缓释制剂,用于与粉末状阿司匹林进行比较。反卷积分析表明,将阿司匹林包裹在微胶囊中可使其吸收持续。有趣的是,分析还表明三种制剂在吸收过程中代谢的百分比有所不同。因此,反卷积方法能够对口服药物进行全面分析。据信该方法有助于口服药物制剂的评估。