Bioavailability and pharmacokinetics of furosemide marketed in Thailand. 1990

S Kaojarern, and O Poobrasert, and A Utiswannakul, and U Kositchaiwat
Department of Medicine, Faculty of Medicine, Ramathibodi Hospital, Mahidol University, Bangkok, Thailand.

Thirteen different brands of 40 mg furosemide tablets available in Thailand were evaluated. In vitro studies revealed that all products met the requirement of United States Pharmacopoeia XX for weight variation, per cent labeled amount, and disintegration time. However, there were only 4 brands that passed the dissolution test specification. The original brand (brand A) and the three local brands (brand B, C and D) with differences in dissolution characteristics were selected for bioavailability study. Relative bioavailability of 40 mg furosemide tablets were performed on eight healthy Thai males using a crossover design. Plasma furosemide concentrations were determined by high-performance liquid chromatographic method. Clinical response to these tablets were also studied by determination of urine output and electrolyte excretion. Individual plasma data was analyzed according to one-compartment open model using the PCNONLIN computer program. The elimination half-life of furosemide was 1.27 hours. The mean individual peak plasma levels ranged from 0.61-1.12 micrograms/ml and the time required to reach the peak ranged from 1.63-2.00 hours. There were no statistically significant differences in parameters studied between the original and the local brands (p greater than 0.05). The relative bioavailability of furosemide with respect to brand A were 70.29, 113.41, and 94.93 per cent for brand B, C and D, respectively. There was no relationship between in vitro and in vivo characteristics. Clinical response, in terms of diuresis and electrolyte excretion, e.g., sodium, chloride and potassium, between four brands of furosemide tablets were also not significantly different (p greater than 0.05), indicating that the four brands are clinically equivalent.

UI MeSH Term Description Entries
D007408 Intestinal Absorption Uptake of substances through the lining of the INTESTINES. Absorption, Intestinal
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
D005665 Furosemide A benzoic-sulfonamide-furan. It is a diuretic with fast onset and short duration that is used for EDEMA and chronic RENAL INSUFFICIENCY. Frusemide,Fursemide,Errolon,Frusemid,Furanthril,Furantral,Furosemide Monohydrochloride,Furosemide Monosodium Salt,Fusid,Lasix
D006207 Half-Life The time it takes for a substance (drug, radioactive nuclide, or other) to lose half of its pharmacologic, physiologic, or radiologic activity. Halflife,Half Life,Half-Lifes,Halflifes
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

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