Biomaterial Database

Pharmacokinetics of multiparticulate sustained-release diltiazem preparations in dogs. 1994

K Murata, and K Noda

Pharmaceutics Research Laboratory, Tanabe Seiyaku Company, Ltd., Osaka, Japan.

The in vivo performance of multiparticulate sustained-release diltiazem preparations [HER-SR(A,B,C)] coated with water-insoluble polymer (ethylcellulose), to control the in vitro dissolution rate, was evaluated in dogs. With a decrease in dissolution rate, HER-SR maintained sustained-release characteristics, although the bioavailability decreased slightly. The bioavailability of HER-SR(A,B,C) was comparable with that of a conventional diltiazem tablet (HER). Plasma diltiazem concentrations for the HER-SR preparations were analyzed with a two-fraction absorption model and the pharmacokinetic characteristics were discussed. From the results, it was considered that HER-SR(B) preparation had desirable pharmacokinetic characteristics as sustained-release diltiazem preparations. The absorption site of the slow-release component of HER-SR(B) in the gastrointestinal tract was examined. Almost all of the component had reached the colon within 5 h of administration, the diltiazem content remaining in the component being approximately 60% of the initial amount. Thus, it was shown that the HER-SR(B) preparation had particular absorption characteristics that resulted in the colon being the part of the gastrointestinal tract most receptive to its release. In vivo release profiles of diltiazem from the HER-SR(B) preparation were calculated by the Wagner-Nelson method, and in vitro and in vivo release profiles of HER-SR(B) were further analyzed with a two-fraction release equation. A close correlation of in vitro and in vivo release profiles of HER-SR(B) was found.

UI	MeSH Term	Description	Entries
D003692	Delayed-Action Preparations	Dosage forms of a drug that act over a period of time by controlled-release processes or technology.	Controlled Release Formulation,Controlled-Release Formulation,Controlled-Release Preparation,Delayed-Action Preparation,Depot Preparation,Depot Preparations,Extended Release Formulation,Extended Release Preparation,Prolonged-Action Preparation,Prolonged-Action Preparations,Sustained Release Formulation,Sustained-Release Preparation,Sustained-Release Preparations,Timed-Release Preparation,Timed-Release Preparations,Controlled-Release Formulations,Controlled-Release Preparations,Extended Release Formulations,Extended Release Preparations,Slow Release Formulation,Sustained Release Formulations,Controlled Release Formulations,Controlled Release Preparation,Controlled Release Preparations,Delayed Action Preparation,Delayed Action Preparations,Formulation, Controlled Release,Formulations, Controlled Release,Prolonged Action Preparation,Release Formulation, Controlled,Release Formulations, Controlled,Sustained Release Preparation,Timed Release Preparation,Timed Release Preparations
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
D004285	Dogs	The domestic dog, Canis familiaris, comprising about 400 breeds, of the carnivore family CANIDAE. They are worldwide in distribution and live in association with people. (Walker's Mammals of the World, 5th ed, p1065)	Canis familiaris,Dog
D000042	Absorption	The physical or physiological processes by which substances, tissue, cells, etc. take up or take in other substances or energy.
D000284	Administration, Oral	The giving of drugs, chemicals, or other substances by mouth.	Drug Administration, Oral,Administration, Oral Drug,Oral Administration,Oral Drug Administration,Administrations, Oral,Administrations, Oral Drug,Drug Administrations, Oral,Oral Administrations,Oral Drug Administrations
D000818	Animals	Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA.	Animal,Metazoa,Animalia
D001682	Biological Availability	The extent to which the active ingredient of a drug dosage form becomes available at the site of drug action or in a biological medium believed to reflect accessibility to a site of action.	Availability Equivalency,Bioavailability,Physiologic Availability,Availability, Biologic,Availability, Biological,Availability, Physiologic,Biologic Availability,Availabilities, Biologic,Availabilities, Biological,Availabilities, Physiologic,Availability Equivalencies,Bioavailabilities,Biologic Availabilities,Biological Availabilities,Equivalencies, Availability,Equivalency, Availability,Physiologic Availabilities