期刊
JOURNAL OF PHARMACEUTICAL SCIENCES
卷 108, 期 2, 页码 1047-1052出版社
ELSEVIER SCIENCE INC
DOI: 10.1016/j.xphs.2018.09.025
关键词
lipid-based formulation; absorption; solubility; bioavailability; lymphatic transport
资金
- National Research Foundation of Korea (NRF) [2018R1A2B6004928]
- National Research Foundation of Korea [2018R1A2B6004928] Funding Source: Korea Institute of Science & Technology Information (KISTI), National Science & Technology Information Service (NTIS)
For performance assessment of the lipid-based drug delivery systems (LBDDSs), in vitro lipolysis is commonly applied because traditional dissolution tests do not reflect the complicated in vivo micellar formation and solubilization processes. Much of previous research on in vitro lipolysis has mostly focused on rank-ordering formulations for their predicted performances. In this study, we have incorporated in vitro lipolysis with microsomal stability to quantitatively predict the oral bioavailability of a lipophilic antineoplastic drug bexarotene (BEX) administered in LBDDS. Two types of LBDDS were applied: lipid solution and lipid suspension. The predicted oral bioavailability values of BEX from linking in vitro lipolysis with microsomal stability for lipid solution and lipid suspension were 34.2 +/- 1.6% and 36.2 +/- 2.6%, respectively, whereas the in vivo oral bioavailability of BEX was tested as 31.5 +/- 13.4% and 31.4 +/- 5.2%, respectively. The predicted oral bioavailability corresponded well with the oral bioavailability for both formulations, demonstrating that the combination of in vitro lipolysis and microsomal stability can quantitatively predict oral bioavailability of BEX. In vivo intestinal lymphatic uptake was also assessed for the formulations and resulted in <1% of the dose, which confirmed that liver microsomal stability was necessary for correct prediction of the bioavailability. (c) 2019 Published by Elsevier Inc. on behalf of the American Pharmacists Association.
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