| Autor: | Katz B, Baron Da, Belonio B, Tugrul T. Kararli, Grant L. Schoenhard, Thomas E. Needham, Schmidt Re |
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| Rok vydání: | 1992 |
| Předmět: |
Pharmacology
PEG 400 Chromatography biology medicine.drug_class Organic Chemistry Pharmaceutical Science Absorption (skin) Renin inhibitor chemistry.chemical_compound Nasal Absorption Oleic acid chemistry Pharmacokinetics Enzyme inhibitor Emulsion medicine biology.protein Molecular Medicine Pharmacology (medical) Biotechnology |
| Zdroj: | Pharmaceutical Research. :1024-1028 |
| ISSN: | 0724-8741 |
| Popis: | Nasal absorption of O-(N-morpholino-carbonyl-3-L-phenylaspartyl-L-leucinamide of (2S,3R,4S)-2-amino-1-cyclohexyl-3,4-dihydroxy-6-methylheptane (I), a renin inhibitor, was evaluated in two rat nasal models, one involving surgery and the other requiring no surgical intervention. Oleic acid/monoolein emulsion formulations were tested along with a control PEG 400 solution. The percent absolute bioavailability of the compound was enhanced from 3–6% (PEG 400 solution) to 15–27% when the emulsion formulations were used. The different nasal model techniques (with and without surgery) did not produce any statistical difference in the absolute bioavailability values for I. Emulsion formulations did not produce appreciable damage as assessed morphologically. It is suggested that emulsion formulations containing membrane adjuvants such as oleic acid and monoolein can be used to enhance the nasal delivery of low-bioavailable, lipid-soluble drugs.____________________ |
| Databáze: | OpenAIRE |
| Externí odkaz: |
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