Characterization and evaluation of an oral microemulsion containing the antitumor diterpenoid compound ent-11alpha-hydroxy-15-oxo-kaur-16-en-19-oic-acid.
作者： Liang , Bozhong Mu , Yingnian Lu , Wu , Li
DOI: 10.2147/IJN.S42002
关键词:
摘要: The objective of this study was to develop an oral microemulsion formulation the antitumor diterpenoid agent, ent-11α-hydroxy-15-oxo-kaur-16-en-19-oic-acid (henceforth referred as 5F), enhance its bioavailability and evaluate hepatotoxicity. Pseudoternary phase diagrams showed that optimal contained 45% water, 10% castor oil phase, 15% Cremophor EL surfactant, 30% a cosurfactant mixture 1,2-propanediol polyethylene glycol (PEG)-400 (2:1, w/w). preparation characterized droplet diameter within 50 nm. Release 5F in vitro from slightly increased compared with suspension containing same amount active drug. Pharmacokinetic parameters vivo indicated markedly improved, relative being 616.15% higher for than suspension. Toxicity tests had no hepatotoxicity mice. These results suggest potential be administered by route.
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