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| Content Provider | Springer Nature Link |
|---|---|
| Author | Cuiné, Jean F. Charman, William N. Pouton, Colin W. Edwards, Glenn A. Porter, Christopher J. H. |
| Copyright Year | 2007 |
| Abstract | To investigate the impact of a change in the proportions of lipid, surfactant and co-solvent on the solubilisation capacity of self-emulsifying formulations of danazol during in vitro dispersion and digestion studies and correlation with in vivo bioavailability in beagle dogs.Formulations from within the phase diagram of the pseudo-ternary system composed of soybean oil:maisine 35-1 (1:1 w/w), Cremophor EL and ethanol were assessed in vitro on dispersion and digestion. The relative bioavailability of danazol after administration of a series of these formulations was also determined.All formulations formed microemulsions in the presence of water and no drug precipitation was observed on dispersion. In contrast, drug solubilisation was markedly affected by lipase-mediated digestion and a reduction in lipid (and increase in surfactant) content resulted in increased drug precipitation. Consistent with these data, the bioavailability of danazol decreased significantly when the lipid content in the formulations was reduced.A rank-order correlation was observed between the patterns of solubilisation obtained during in vitro digestion and the in vivo performance of self-emulsifying formulations of danazol. In general a decrease in the lipid content and an increase in the proportions of surfactant and co-solvent resulted in reduced danazol bioavailability. |
| Starting Page | 748 |
| Ending Page | 757 |
| Page Count | 10 |
| File Format | |
| ISSN | 07248741 |
| Journal | Pharmaceutical Research |
| Volume Number | 24 |
| Issue Number | 4 |
| e-ISSN | 1573904X |
| Language | English |
| Publisher | Kluwer Academic Publishers-Plenum Publishers |
| Publisher Date | 2007-02-15 |
| Publisher Place | New York |
| Access Restriction | One Nation One Subscription (ONOS) |
| Subject Keyword | self-emulsifying lipid-based formulations poorly water-soluble drugs in vitro lipid digestion oral bioavailability lipolysis danazol Biomedical Engineering Medical Law Biochemistry Pharmacy Pharmacology/Toxicology |
| Content Type | Text |
| Resource Type | Article |
| Subject | Organic Chemistry Pharmacology Molecular Medicine Pharmacology (medical) Biotechnology Pharmaceutical Science |
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