Erscheint 6 Ausgaben pro Jahr
ISSN Druckformat: 0743-4863
ISSN Online: 2162-660X
Indexed in
Oral Delivery of HIV-Protease Inhibitors
ABSTRAKT
Strategies for optimizing the oral delivery of HIV-protease inhibitors draw from drug discovery efforts in molecular design, drug development tools in dosage formulation, and dosage regimen considerations in clinical medicine. This review outlines the evolution of these strategies for drugs that have been approved for human use, drug candidates still in development, and molecules that are no longer in development but from which valuable delivery information was obtained. Molecular design for obtaining desirable pharmacokinetics following oral administration primarily involved maximizing aqueous solubility and minimizing first-pass metabolism. Optimization of molecular design for oral drug delivery purposes is tempered by additional considerations for drug potency, toxicity, potential for interactions, and development of viral resistance. Strategies for improving oral bioavailability dirough dosage formulation use information from the effects of coadministered meals on drug plasma levels. Patient adherence to dosage regimens remains a major issue in assuring effective oral drug treatment and in preventing the development of resistance. Progress has been made in clinical studies where improved oral bioavailability and reductions in drug plasma level variability have been achieved with appropriate dosage regimen adjustment.
-
Li Lilian Y, Rodríguez-Hornedo Naír, Heimbach Tycho, Fleisher David, In-vitro crystallization of indinavir in the presence of ritonavir and as a function of pH, Journal of Pharmacy and Pharmacology, 55, 5, 2010. Crossref
-
Sheng Jennifer J., Kasim Nehal A., Chandrasekharan Ramachandran, Amidon Gordon L., Solubilization and dissolution of insoluble weak acid, ketoprofen: Effects of pH combined with surfactant, European Journal of Pharmaceutical Sciences, 29, 3-4, 2006. Crossref
-
Demir Huriye, Arica-Yegin Betül, Oner Levent, Application of an artificial neural network to predict dissolution data and determine the combined effect of pH and surfactant addition on the solubility and dissolution of the weak acid drug etodolac, Journal of Drug Delivery Science and Technology, 47, 2018. Crossref
-
Fleisher David, Sweet Burgunda V., Parekh Ameeta, Drug Absorption With Food, in Handbook of Drug-Nutrient Interactions, 2004. Crossref