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Bioavailability: Overview01:13

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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...
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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...
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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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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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In certain scenarios, in vitro dissolution tests can replace in vivo bioequivalence studies. This is particularly true when a drug product, though available in varying strengths, maintains proportional similarity in its active and inactive ingredients. In such cases, the need for in vivo bioequivalence studies for lower strength variants may be waived, provided dissolution tests and in vivo studies on the highest strength yield satisfactory results.Bioequivalence can be indicated through...
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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,...
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Comparative oral bioavailability advantage from curcumin formulations.

Bhushan Munjal1, Yogesh Bapurao Pawar, Sarsvatkumar Babulal Patel

  • 1Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research (NIPER), Sector-67, S.A.S. Nagar, Punjab, 160062, India.

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|March 20, 2015
PubMed
Summary
This summary is machine-generated.

This study enhanced curcumin (CRM) oral bioavailability using nanosuspension, amorphous solid dispersion, and HP-β-CD complex, significantly increasing absorption. Other formulations like piperine and milk composites showed limited or reduced bioavailability.

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Area of Science:

  • Pharmacology
  • Drug Delivery
  • Natural Products

Background:

  • Curcumin (CRM) exhibits poor oral bioavailability due to low solubility and rapid metabolism.
  • Developing effective CRM formulations is crucial for its therapeutic potential.

Purpose of the Study:

  • To evaluate and compare the oral bioavailability of seven different curcumin (CRM) formulations.
  • To identify formulation strategies that enhance CRM absorption in vivo.

Main Methods:

  • Oral administration of various CRM formulations (aqueous suspension, nanosuspension, amorphous solid dispersion, HP-β-CD complex, piperine combination, milk composite) to Sprague-Dawley rats.
  • Quantification of CRM plasma concentrations using validated high-performance liquid chromatography (HPLC).
  • Assessment of pharmacokinetic parameters including C max, AUC(0–t), and T max.

Main Results:

  • Nanosuspension, amorphous solid dispersion, and HP-β-CD inclusion complex significantly increased CRM oral bioavailability (AUC(0–t) by 251%, 446%, and 567%, respectively; C max by 405%, 270%, and 415%, respectively).
  • Piperine and micronized suspension showed no significant improvement in bioavailability.
  • CRM-milk composite reduced oral bioavailability.

Conclusions:

  • Formulation strategies like nanosuspension, amorphous solid dispersion, and HP-β-CD complex are effective in enhancing curcumin oral bioavailability.
  • Solubility enhancement and potentially metabolism inhibition are key factors for improving CRM absorption.
  • Further research into optimized formulations can unlock the therapeutic benefits of curcumin.