Comparative bioavailability of three commercial acetaminophen tablets. 1987

S Hekimoğlu, and G Ayanoğlu-Dülger, and A A Hincal

Three brands of acetaminophen tablets marketed in Turkey were evaluated for their in vitro properties, and their in vivo bioavailabilities were determined in comparison to a standard acetaminophen solution containing an equivalent amount of the drug. The total amount of acetaminophen in urine or in tablets was determined by the colorimetric method of Welch and Conney [1965]. No significant difference between the manufacturing parameters, namely the assay, hardness, diameter and thickness of the brands was observed except that the coefficients of variation for brand A were greater than the other two brands. Brand A also disintegrated more slowly and its dissolution time (80% of the drug dissolved in 45 min) did not meet the requirements of USP XX. In vivo bioavailability studies were carried out in six healthy volunteers who received the tablets or the standard solution in a single dose, cross-over study. The urine was collected for 24 h and the total acetaminophen excreted was determined according to the method of Welch and Conney. The relative bioavailabilities for Brands A, B and C were found to be 97.87, 95.41 and 98.78%, respectively, with respect to the solution. The differences were not statistically significant and it can be concluded that all tablets were rapidly and almost completely absorbed. This study also demonstrates that there is not always a good correlation between the in vitro disintegration and dissolution tests and the in vivo bioavailability of a drug.

UI MeSH Term Description Entries
D008297 Male Males
D005260 Female Females
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
D000082 Acetaminophen Analgesic antipyretic derivative of acetanilide. It has weak anti-inflammatory properties and is used as a common analgesic, but may cause liver, blood cell, and kidney damage. Acetamidophenol,Hydroxyacetanilide,Paracetamol,APAP,Acamol,Acephen,Acetaco,Acetominophen,Algotropyl,Anacin-3,Datril,N-(4-Hydroxyphenyl)acetanilide,N-Acetyl-p-aminophenol,Panadol,Tylenol,p-Acetamidophenol,p-Hydroxyacetanilide,Anacin 3,Anacin3
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
D012995 Solubility The ability of a substance to be dissolved, i.e. to form a solution with another substance. (From McGraw-Hill Dictionary of Scientific and Technical Terms, 6th ed) Solubilities
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

Related Publications

S Hekimoğlu, and G Ayanoğlu-Dülger, and A A Hincal
April 1981, Journal of pharmaceutical sciences,
S Hekimoğlu, and G Ayanoğlu-Dülger, and A A Hincal
January 1991, European journal of drug metabolism and pharmacokinetics,
S Hekimoğlu, and G Ayanoğlu-Dülger, and A A Hincal
April 1976, Journal of pharmacokinetics and biopharmaceutics,
S Hekimoğlu, and G Ayanoğlu-Dülger, and A A Hincal
July 1979, European journal of clinical pharmacology,
S Hekimoğlu, and G Ayanoğlu-Dülger, and A A Hincal
January 1990, DICP : the annals of pharmacotherapy,
S Hekimoğlu, and G Ayanoğlu-Dülger, and A A Hincal
October 1978, Journal of pharmaceutical sciences,
S Hekimoğlu, and G Ayanoğlu-Dülger, and A A Hincal
January 1989, DICP : the annals of pharmacotherapy,
S Hekimoğlu, and G Ayanoğlu-Dülger, and A A Hincal
July 1984, Journal of pharmaceutical sciences,
S Hekimoğlu, and G Ayanoğlu-Dülger, and A A Hincal
January 1984, Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan,
S Hekimoğlu, and G Ayanoğlu-Dülger, and A A Hincal
December 1983, International journal of clinical pharmacology, therapy, and toxicology,
Copied contents to your clipboard!