Comparative bioavailability of chlorpropamide tablet and suspension formulations. 1982

R L Batenhorst, and J A Bustrack, and B A Bivins, and T S Foster

The bioavailability of a chlorpropamide tablet formulation chlorpropamide tablet formulation was assessed by comparing it to a reference suspension of chlorpropamide. Eighteen healthy adult men received chlorpropamide 250 mg as a tablet (Diabinese, Pfizer) and suspension in an open two-way crossover study of Latin-square design with a 14-day washout period between treatments. Serial blood samples were obtained by venipuncture for 96 hours for chlorpropamide serum concentration determinations. Serum glucose concentrations were determined at 0, 0.5, 1, 2, and 4 hours. The area under the serum chlorpropamide concentration-time curve (AUC), peak serum chlorpropamide concentration (Cmax), time to Cmax, and mean glucose concentration at each time point for each treatment were compared using a two-tailed Student's t test for paired data (p less than 0.05). Microrate constants for a two-compartment model for oral absorption computed using nonlinear regression were also compared. There were no significant differences between the two formulations regarding AUC, Cmax, time to Cmax, and hypoglycemic response. The absorption rate for the tablet was significantly greater than for the suspension. The results suggest that the oral chlorpropamide tablet and reference suspension are bioequivalent. Although the tablet had a faster absorption rate than the suspension, this probably is not clinically important since both formulations similarly decreased serum glucose concentration.

UI MeSH Term Description Entries
D008297 Male Males
D011897 Random Allocation A process involving chance used in therapeutic trials or other research endeavor for allocating experimental subjects, human or animal, between treatment and control groups, or among treatment groups. It may also apply to experiments on inanimate objects. Randomization,Allocation, Random
D001786 Blood Glucose Glucose in blood. Blood Sugar,Glucose, Blood,Sugar, Blood
D002747 Chlorpropamide A sulfonylurea hypoglycemic agent used in the treatment of non-insulin-dependent diabetes mellitus not responding to dietary modification. (From Martindale, The Extra Pharmacopoeia, 30th ed, p277) Clorpropamid,Apo-Chlorpropamide,Diabinese,Glucamide,Insogen,Meldian
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000328 Adult A person having attained full growth or maturity. Adults are of 19 through 44 years of age. For a person between 19 and 24 years of age, YOUNG ADULT is available. Adults
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
D013535 Suspensions Colloids with liquid continuous phase and solid dispersed phase; the term is used loosely also for solid-in-gas (AEROSOLS) and other colloidal systems; water-insoluble drugs may be given as suspensions. Suspension
D013607 Tablets Solid dosage forms, of varying weight, size, and shape, which may be molded or compressed, and which contain a medicinal substance in pure or diluted form. (Dorland, 28th ed) Tablet
D013997 Time Factors Elements of limited time intervals, contributing to particular results or situations. Time Series,Factor, Time,Time Factor

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