Mitigation of Adverse Clinical Events of a Narrow Target Therapeutic Index Compound through Modified Release Formulation Design: An in Vitro, in Vivo, in Silico, and Clinical Pharmacokinetic Analysis

Molecular Pharmaceutics

Volumn 12, Issue 12, 2015, Pages 4434-4444

  Good, David J ^a   Hartley, Ruiling ^a   Mathias, Neil ^a   Crison, John ^a   Tirucherai, Giridhar ^a   Timmins, Peter ^a   Hussain, Munir ^a   Haddadin, Raja ^a   Koo, Otilia ^a   Nikfar, Faranak ^a   Fung, Nga Kit Eliza ^a  

^a BRISTOL MYERS SQUIBB   (United States)

Author keywords

BCS 2 weak base; enteric coating; hydrophilic matrix tablets; in vitro dissolution; in vivo site of absorption; modified release formulation; pH effect mitigation; pharmacokinetic absorption model

Indexed keywords

BMS 914392; CARDIOVASCULAR AGENT; FAMOTIDINE; UNCLASSIFIED DRUG; QUINOLINE; QUINOLINE DERIVATIVE;

ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; BEAGLE; COMPUTER MODEL; COMPUTER SIMULATION; CONTROLLED STUDY; CROSSOVER PROCEDURE; DIET RESTRICTION; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG DELIVERY SYSTEM; DRUG DOSAGE FORM; DRUG EXPOSURE; DRUG RELEASE; DRUG SAFETY; DRUG SOLUBILITY; HUMAN; HUMAN EXPERIMENT; IN VITRO STUDY; IN VIVO STUDY; MALE; MAXIMUM PLASMA CONCENTRATION; NONHUMAN; NORMAL HUMAN; PHARMACOKINETIC PARAMETERS; PLASMA; PLASMA CLEARANCE; PRIORITY JOURNAL; RISK ASSESSMENT; SIMULATOR; SINGLE DRUG DOSE; SLOW DRUG RELEASE; STOMACH EMPTYING; STOMACH PH; TABLET FORMULATION; UNSPECIFIED SIDE EFFECT; VOLUME OF DISTRIBUTION; ANIMAL; BIOAVAILABILITY; BIOLOGICAL MODEL; DOG; INTESTINE ABSORPTION; MEDICINAL CHEMISTRY; ORAL DRUG ADMINISTRATION; PROCEDURES; RANDOMIZED CONTROLLED TRIAL; SOLUBILITY;

ADMINISTRATION, ORAL; ANIMALS; BIOLOGICAL AVAILABILITY; CHEMISTRY, PHARMACEUTICAL; COMPUTER SIMULATION; CROSS-OVER STUDIES; DOGS; FAMOTIDINE; HUMANS; INTESTINAL ABSORPTION; MALE; MODELS, BIOLOGICAL; QUINOLINES; SOLUBILITY;

EID: 84948957019     PISSN: 15438384     EISSN: 15438392     Source Type: Journal    
DOI: 10.1021/acs.molpharmaceut.5b00624     Document Type: Article

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