Lymphatic Transport of Halofantrine in the Conscious Rat When Administered as Either the Free Base or the Hydrochloride Salt: Effect of Lipid Class and Lipid Vehicle Dispersion

• Published in: Journal of pharmaceutical sciences Vol. 85; no. 4; pp. 357 - 361
• Main Authors: Porter, Christopher J.H., Charman, Susan A., Humberstone, Andrew J., Charman, William N.
• Format: Journal Article
• Language: English
• Published: New York Elsevier Inc 01.04.1996; John Wiley & Sons, Inc; Wiley; American Pharmaceutical Association
• Subjects: Administration, Oral; Animals; Antibiotics. Antiinfectious agents. Antiparasitic agents; Antimalarials - administration & dosage; Antiparasitic agents; Biological and medical sciences; Drug Carriers; Fatty Acids - metabolism; Intestinal Absorption; Lipoproteins - metabolism; Lymphatic System - metabolism; Male; Medical sciences; Micelles; Pharmacology. Drug treatments; Phenanthrenes - administration & dosage; Phenanthrenes - metabolism; Protein Binding; Rats; Rats, Sprague-Dawley; Triglycerides - metabolism; Antimalarial; Rat; Rodentia; Vehicle(excipient); Gut; Oral administration; Lipids; Lymphatic circulation; Dispersion; Property formulation relationship; Lipophilic compound; Vertebrata; Mammalia; Absorption; Animal; Pharmacokinetics

The intestinal lymphatic transport of halofantrine, an important, highly lipophilic antimalarial drug, has been studied in a conscious rat model after oral administration. In these studies, the lymphatic transport of Hf free base when coadministered with lipid was ∼20% of the administered dose compa...