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Expandable gastroretentive dosage forms.
TLDR
Using the dog as a preclinical screening model prior to human studies, relevant imaging techniques and pharmacokinetic-pharmacodynamic aspects of such delivery systems are discussed and findings are an important step towards the implementation of expandable GRDFs in the clinical setting.
Uptake of lipophilic drugs by plasma derived isolated chylomicrons: linear correlation with intestinal lymphatic bioavailability.
TLDR
The degree of association of lipophilic compounds with isolated chylomicrons can be used as a simple screening model for estimation of intestinal lymphatic transport potential of drug molecules.
The role of the lymphatic system in subcutaneous absorption of macromolecules in the rat model.
TLDR
In the rat model, following SC administration, the macromolecules were absorbed mainly through the blood capillaries with minimal contribution of the lymphatic system to systemic bioavailability.
The effect of different lipid based formulations on the oral absorption of lipophilic drugs: the ability of in vitro lipolysis and consecutive ex vivo intestinal permeability data to predict in vivo
  • A. Dahan, A. Hoffman
  • Chemistry, Medicine
    European journal of pharmaceutics and…
  • 1 August 2007
TLDR
The in vitro lipolysis model was found to be useful in the intelligent optimization of oral lipid formulations for lipophilic drugs, even in the case where the intestinal permeability is enhanced by the formulation.
Novel levodopa gastroretentive dosage form: in-vivo evaluation in dogs.
TLDR
The outcomes demonstrate that the CR-GRDF may be used to improve levodopa therapy and can be applied to extend the absorption of other narrow absorption window drugs that require continuous input.
Rationalizing the selection of oral lipid based drug delivery systems by an in vitro dynamic lipolysis model for improved oral bioavailability of poorly water soluble drugs.
  • A. Dahan, A. Hoffman
  • Chemistry, Medicine
    Journal of controlled release : official journal…
  • 2 July 2008
TLDR
The dynamic in vitro lipolysis model seems to provide highly useful initial guidelines in the development process of oral lipid based drug delivery systems for poorly water soluble drugs, and it predicts phenomena that occur in the pre-enterocyte stages of the intestinal absorption cascade.
A peptide prodrug approach for improving bisphosphonate oral absorption.
TLDR
The results indicate that the oral absorption of bisphosphonates can be improved by peptidyl prodrugs via the hPEPT1; however, other transporters may also be involved.
Evaluation of a chylomicron flow blocking approach to investigate the intestinal lymphatic transport of lipophilic drugs.
  • A. Dahan, A. Hoffman
  • Chemistry, Medicine
    European journal of pharmaceutical sciences…
  • 1 March 2005
TLDR
The chemical blockage of chylomicron flow provides a potential approach for lymphatic transport investigation, and may elucidate processes involving in the absorption of lipophilic compounds.
Carrier‐mediated transport of metformin across the human placenta determined by using the ex vivo perfusion of the placental cotyledon model
TLDR
The aim of the study was to characterize its permeability across the human placenta using the ex vivo placental perfusion model.
Improving oral bioavailability of peptides by multiple N-methylation: somatostatin analogues.
TLDR
It is possible to overcome the above mentioned bioavailability drawbacks of peptides providing both the biological activity and the receptor selectivity by multiple N-methylation of cyclic peptides.
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