Guar gum-based sustained release diltiazem. 1998

S A Altaf, and K Yu, and J Parasrampuria, and D R Friend
CIBUS Pharmaceutical, Inc., Menlo Park, California 94026-1226, USA.

OBJECTIVE This study was performed to examine the use of guar gum to sustain the release of diltiazem under in vitro and in vivo conditions. METHODS Guar gum tablet formulations were prepared and evaluated under a variety of in vitro dissolution conditions. The formulations, along with Dilacor XR, were administered to a group eight fasted, healthy volunteers in a four period crossover study. RESULTS Varying the lot of guar gum as well as using guar from different suppliers had little effect on diltiazem dissolution. Also, dissolution of diltiazem from guar gum tablets was essentially independent of stir speed under normal conditions (USP Apparatus II) The stability of guar-based formulations under stressed conditions (40 degrees C/75% relative humidity for 3 months) was also established. All four formulations gave similar plasma concentrations over time in the healthy volunteers pharmacokinetic study. CONCLUSIONS Guar gum-based matrix tablets represent a simple and economical alternative to existing diltiazem sustained release dosage forms.

UI MeSH Term Description Entries
D008351 Mannans Polysaccharides consisting of mannose units. Mannan
D010316 Particle Size Relating to the size of solids. Particle Sizes,Size, Particle,Sizes, Particle
D012016 Reference Values The range or frequency distribution of a measurement in a population (of organisms, organs or things) that has not been selected for the presence of disease or abnormality. Normal Range,Normal Values,Reference Ranges,Normal Ranges,Normal Value,Range, Normal,Range, Reference,Ranges, Normal,Ranges, Reference,Reference Range,Reference Value,Value, Normal,Value, Reference,Values, Normal,Values, Reference
D004110 Diltiazem A benzothiazepine derivative with vasodilating action due to its antagonism of the actions of CALCIUM ion on membrane functions. Aldizem,CRD-401,Cardil,Cardizem,Dilacor,Dilacor XR,Dilren,Diltiazem Hydrochloride,Diltiazem Malate,Dilzem,Tiazac,CRD 401,CRD401
D004337 Drug Carriers Forms to which substances are incorporated to improve the delivery and the effectiveness of drugs. Drug carriers are used in drug-delivery systems such as the controlled-release technology to prolong in vivo drug actions, decrease drug metabolism, and reduce drug toxicity. Carriers are also used in designs to increase the effectiveness of drug delivery to the target sites of pharmacological actions. Liposomes, albumin microspheres, soluble synthetic polymers, DNA complexes, protein-drug conjugates, and carrier erythrocytes among others have been employed as biodegradable drug carriers. Drug Carrier
D005685 Galactans Polysaccharides composed of repeating galactose units. They can consist of branched or unbranched chains in any linkages. Galactan,Polygalactose,Polygalactoses
D006244 Hardness The mechanical property of material that determines its resistance to force. HARDNESS TESTS measure this property. Hardnesses
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D006813 Humidity A measure of the amount of WATER VAPOR in the air. Humidities
D006863 Hydrogen-Ion Concentration The normality of a solution with respect to HYDROGEN ions; H+. It is related to acidity measurements in most cases by pH pH,Concentration, Hydrogen-Ion,Concentrations, Hydrogen-Ion,Hydrogen Ion Concentration,Hydrogen-Ion Concentrations

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