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Related Concept Videos

Bioavailability: Overview01:13

Bioavailability: Overview

Bioavailability refers to the proportion of an unaltered drug that, after administration, enters the systemic circulation and can be distributed to the desired action site. Factors such as gastrointestinal (GI) absorption and liver biotransformation influence the bioavailability of a drug when it is administered orally. When a drug is administered intravenously, it enters the systemic circulation directly; by definition, its bioavailability is assumed to be 100%. The bioavailability of an...
Factors Influencing Bioavailability: First-Pass Elimination01:23

Factors Influencing Bioavailability: First-Pass Elimination

When a drug is taken orally, it undergoes a journey starting from the gastrointestinal (GI) tract, passing through the portal vein, reaching the liver, and finally entering the systemic circulation. This process involves the absorption of the drug across the GI tract. The liver is the primary site for metabolizing the drug, with some metabolism also occurring in the gut wall. This journey significantly reduces the quantity of the drug that reaches the systemic circulation, a phenomenon known as...
Bioavailability: Overview01:17

Bioavailability: Overview

Bioavailability refers to the proportion of an administered drug that reaches the systemic circulation in its active, unaltered form. It is a crucial pharmacokinetic parameter that determines the effectiveness of a drug in achieving its intended therapeutic outcomes. The route of administration significantly influences bioavailability, with intravenous administration achieving 100% bioavailability as the drug directly enters the bloodstream. In contrast, oral administration often results in...
Bioavailability: Influencing Factors01:22

Bioavailability: Influencing Factors

Bioavailability refers to the extent and rate at which a drug reaches systemic circulation in its active form. Extent refers to the amount of the drug that makes it into circulation, while rate is the speed at which it enters circulation. It is influenced by several factors critical for optimizing drug formulations, dosing regimens, and therapeutic outcomes.Physicochemical properties of drugs and formulationsThe solubility, stability, and dissolution rate of a drug significantly impact its...
Measurement of Bioavailability: Pharmacokinetic Methods01:30

Measurement of Bioavailability: Pharmacokinetic Methods

Pharmacokinetics is a vital branch of pharmacology that examines how drugs are absorbed, distributed, metabolized, and excreted by the body. Two key methodologies in pharmacokinetics are plasma drug concentration studies and urinary drug excretion analyses, both of which provide critical insights into a drug's therapeutic efficacy and bioavailability.Plasma Drug Concentration-Time StudiesPlasma drug concentration-time studies involve analyzing blood samples at specific intervals to quantify...
Modified-Release Drug Delivery Systems: Bioavailability01:30

Modified-Release Drug Delivery Systems: Bioavailability

Modified-release (MR) dosage forms are designed to extend drug release over time, thereby maintaining stable plasma concentrations and reducing dosing frequency. However, their bioavailability is typically below 100% due to incomplete drug release and presystemic metabolism, and limitations in drug permeability across the gastrointestinal epithelium, all of which can restrict the fraction of the drug reaching systemic circulation. Consequently, studying the in vivo bioavailability of MR...

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Related Experiment Video

Updated: Jun 18, 2026

Mass Spectrometry and Luminogenic-based Approaches to Characterize Phase I Metabolic Competency of In Vitro Cell Cultures
10:44

Mass Spectrometry and Luminogenic-based Approaches to Characterize Phase I Metabolic Competency of In Vitro Cell Cultures

Published on: March 28, 2017

Bioavailability of cimetidine in man.

S S Walkenstein, J W Dubb, W C Randolph

    Gastroenterology
    |February 1, 1978
    PubMed
    Summary
    This summary is machine-generated.

    Parenteral cimetidine (intramuscular and intravenous) showed interchangeable bioavailability. Oral cimetidine liquid demonstrated comparable efficacy to parenteral routes, and cimetidine tablets were bioequivalent to the oral liquid.

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    Area of Science:

    • Pharmacokinetics
    • Drug bioavailability
    • Gastrointestinal pharmacology

    Background:

    • Cimetidine is a histamine H2 receptor antagonist used to treat conditions like peptic ulcers.
    • Understanding the bioavailability of different cimetidine formulations is crucial for optimizing therapeutic efficacy.
    • Parenteral administration bypasses first-pass metabolism, potentially altering drug absorption compared to oral routes.

    Purpose of the Study:

    • To compare the bioavailability of parenteral cimetidine (intramuscular vs. intravenous) and oral cimetidine liquid.
    • To assess the bioequivalence of cimetidine tablets compared to an oral liquid formulation.
    • To evaluate pharmacokinetic parameters including blood levels and urinary excretion.

    Main Methods:

    • A balanced three-way crossover study involving 12 healthy volunteers.
    • Comparison of blood levels and urinary excretion following intramuscular, intravenous, and oral administration of 300 mg cimetidine.
    • A separate study assessed the bioequivalence of 300 mg cimetidine tablets versus oral liquid in another group of 12 volunteers.

    Main Results:

    • Intramuscular and intravenous routes of cimetidine administration exhibited virtually interchangeable bioavailability.
    • Oral cimetidine liquid showed a reduced area under the blood level curve compared to parenteral doses.
    • Oral liquid demonstrated equivalence in maintaining blood levels above 0.5 microgram/mL compared to parenteral routes.
    • Cimetidine 300 mg tablets were found to be bioequivalent to the 300 mg oral liquid formulation.

    Conclusions:

    • Parenteral routes (IM/IV) of cimetidine are interchangeable for achieving systemic drug exposure.
    • Oral cimetidine liquid offers comparable therapeutic potential to parenteral administration based on sustained therapeutic blood levels.
    • Cimetidine tablet formulation provides equivalent bioavailability to the oral liquid, ensuring consistent therapeutic outcomes.