Deconvolution analysis for absorption and metabolism of aspirin in microcapsules.
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.
Wu
X
X
Department of Drug Delivery Research, Graduate School of Pharmaceutical Sciences, Kyoto University, Japan.
Yamashita
F
F
Hashida
M
M
D000042:Absorption; D000180:Acrylic Resins; D000465:Algorithms; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage / Q000493:pharmacokinetics*; D001241:Aspirin / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D002214:Capsules; D002482:Cellulose / Q000031:analogs & derivatives; D002851:Chromatography, High Pressure Liquid; D005079:Excipients; D005782:Gels; D008297:Male; D008954:Models, Biological; D011109:Polymethacrylic Acids; D051381:Rats; D017208:Rats, Wistar; D012995:Solubility
D000180:Acrylic Resins; D000894:Anti-Inflammatory Agents, Non-Steroidal; D002214:Capsules; D005079:Excipients; D005782:Gels; D011109:Polymethacrylic Acids; C038300:methylmethacrylate-methacrylic acid copolymer; C013517:ethyl cellulose; D002482:Cellulose; D001241:Aspirin