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Related Concept Videos

Bioequivalence: Overview01:16

Bioequivalence: Overview

Pharmaceutical equivalents, by definition, are drug products with the same active ingredient in the same quantities, encapsulated in identical dosage forms, and intended for the same administration routes. These pharmaceutical equivalents are deemed bioequivalent if the bioavailability of the active entity in the drug preparations is similar. Moreover, pharmaceutical equivalents demonstrating bioequivalence are also regarded as therapeutically equivalent. This means that when used as directed,...
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...
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...
Bioequivalence Data: Statistical Interpretation01:16

Bioequivalence Data: Statistical Interpretation

The statistical interpretation of bioequivalence data is a significant aspect of pharmaceutical research. Bioequivalence refers to the absence of any significant difference in the rate and extent to which the active ingredient in pharmaceutical products becomes available at the site of drug action when administered at the same molar dose under similar conditions. This helps determine if different drug products have similar absorption rates, ensuring their interchangeability.Statistical...
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...
Bioavailability Study Design: Absolute Versus Relative Bioavailability01:27

Bioavailability Study Design: Absolute Versus Relative Bioavailability

Bioavailability is a crucial pharmacokinetic parameter that quantifies the proportion of an administered drug that reaches the systemic circulation and is available for therapeutic action. Regulatory agencies mandate the assessment of bioavailability, typically measured as the area under the drug plasma concentration-versus-time curve (AUC), to ensure the efficacy and safety of pharmaceutical products. These evaluations are categorized as absolute and relative bioavailability studies.Absolute...

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Screening for Phytoestrogens using a Cell-based Estrogen Receptor &#946; Reporter Assay
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Published on: June 7, 2020

[What about bioavailable estradiol?].

T D T Nguyen1, L Dolomie-Fagour, A Georges

  • 1Service de médecine nucléaire, CHU de Bordeaux, Hôpital Haut-Lévêque, Pessac. diemtien.nguyen@wanadoo.fr

Annales De Biologie Clinique
|October 30, 2008
PubMed
Summary
This summary is machine-generated.

Bioavailable estradiol (E(2)), the hormone not bound to SHBG, is crucial for tissue diffusion and cellular uptake. Measuring this bioavailable E(2) offers insights into chronic diseases like osteoporosis and cardiovascular conditions.

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Area of Science:

  • Endocrinology
  • Biochemistry
  • Reproductive Health

Background:

  • Estradiol (E(2)) circulates in serum primarily bound to sex hormone-binding globulin (SHBG) and albumin.
  • Only the non-SHBG-bound fraction, encompassing free and albumin-bound estradiol, is readily available for diffusion into tissues and cellular interaction.
  • This bioavailable hormone fraction is considered a key indicator of the bioactive hormone concentration.

Purpose of the Study:

  • To highlight the significance of bioavailable estradiol (E(2)) measurement.
  • To discuss the potential role of bioavailable E(2) in understanding chronic diseases in both men and women.
  • To emphasize the need for sensitive assays for low E(2) concentrations.

Main Methods:

  • Review of existing studies reporting on bioavailable E(2) measurements.
  • Discussion of the implications of bioavailable E(2) in epidemiological research.
  • Consideration of assay sensitivity requirements for E(2) detection.

Main Results:

  • Bioavailable estradiol (E(2)) represents the easily diffusible and target cell-accessible hormone fraction.
  • Studies suggest bioavailable E(2) measurement is valuable for understanding chronic conditions such as osteoporosis, cardiovascular disease, and Alzheimer's disease.
  • Epidemiological studies increasingly report the relevance of bioavailable E(2).

Conclusions:

  • Bioavailable estradiol (E(2)) is a critical determinant of hormone availability to target tissues.
  • While its direct implication in specific pathologies requires further investigation, bioavailable E(2) holds significant interest in chronic disease research.
  • Accurate and sensitive measurement of bioavailable E(2) is essential for advancing our understanding of its role in health and disease.