Relationship between dissolution rate and bioavailability of paracetamol tablet. 2003

Xiao-ping Huang, and Xin-xiang Wan, and Qiang Liu
Teaching and Research Section of Pharmacy, Department of Medical Laboratory Technology, First Military Medical University, Guangzhou 510315, China.

OBJECTIVE To investigate the relationship between the dissolution rate and bioavailability of paracetamol tablets. METHODS The dissolution rate of paracetamol tablet was determined according to methods described in the Pharmacopoeia of the People's Republic of China. Ultraviolet spectrophotometry was employed to measure urine concentration of paracetamol, and the relative bioavailability was determined in 25 male healthy volunteers, with the relationship between the dissolution rate and bioavailability of paracetamol assessed. RESULTS The 15-min dissolution rates of 5 kinds of paracetamol tablets were 100.43+/-2.61, 99.76+/-1.97, 96.47+/-3.52, 89.58+/-1.85, and 85.85+/-1.83 respectively, with their bioavailability of 86.34+/-10.06, 85.82+/-11.21, 87.10+/-10.86, 81.71+/-12.34, and 76.53+/-11.73 respectively, showing obvious linear relationship between them, which conformed to the equation y = 0.6122x + 25.175, r = 0.9642. CONCLUSIONS As there is a good linear relationship between the dissolution rate and bioavailability of paracetamol tablets, the latter parameter can be derived from the measurement of the former.

UI MeSH Term Description Entries
D008297 Male Males
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
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
D018712 Analgesics, Non-Narcotic A subclass of analgesic agents that typically do not bind to OPIOID RECEPTORS and are not addictive. Many non-narcotic analgesics are offered as NONPRESCRIPTION DRUGS. Non Opioid Analgesic,Non-Opioid Analgesic,Nonopioid Analgesic,Nonopioid Analgesics,Analgesics, Nonnarcotic,Analgesics, Nonopioid,Non-Opioid Analgesics,Analgesic, Non Opioid,Analgesic, Non-Opioid,Analgesic, Nonopioid,Analgesics, Non Narcotic,Analgesics, Non-Opioid,Non Opioid Analgesics,Non-Narcotic Analgesics,Nonnarcotic Analgesics,Opioid Analgesic, Non

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