Factors that restrict the cell permeation of cyclic prodrugs of an opioid peptide, part 4: Characterization of the biopharmaceutical and physicochemical properties of two new cyclic prodrugs designed to be stable to oxidative metabolism by cytochrome P-450 enzymes in the intestinal mucosa

Journal of Pharmaceutical Sciences

Volumn 101, Issue 9, 2012, Pages 3500-3510

  Nofsinger, Rebecca ^a,b   Borchardt, Ronald T ^a  

^a UNIVERSITY OF KANSAS   (United States)

^b MERCK RESEARCH LABORATORIES   (United States)

Author keywords

Cyclic peptide prodrug; Cytrochrome P 450; DADLE; Ester prodrug; Molecular dynamics; Opioid peptide; Permeability; Physicochemical properties; Structure

Indexed keywords

COUMARIN DERIVATIVE; COUMARINIC ACID; COUMARINIC ACID[CYCHEXALANINE 4, DEXTRO LEUCINE 5]ENKEPHALIN; COUMARINIC ACID[CYCHEXALANINE, DEXTRO ALANINE 5]ENKEPHALIN; CYTOCHROME P450; ENKEPHALIN DERIVATIVE; ENKEPHALIN[2 DEXTRO ALANINE 5 DEXTRO LEUCINE]; PRODRUG; UNCLASSIFIED DRUG;

AEROBIC METABOLISM; ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; CELL MEMBRANE PERMEABILITY; CELL PERMEABILIZATION; CELL STRAIN CACO 2; CONTROLLED STUDY; DRUG METABOLISM; DRUG SOLUBILITY; DRUG STABILITY; DRUG STRUCTURE; EFFUSION; INTESTINE MUCOSA; INTESTINE PERFUSION; LIPOPHILICITY; MOLECULAR DYNAMICS; MOLECULAR SIZE; NONHUMAN; NUCLEAR MAGNETIC RESONANCE; RAT;

EID: 84864052734     PISSN: 00223549     EISSN: 15206017     Source Type: Journal    
DOI: 10.1002/jps.23079     Document Type: Article

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