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Related Concept Videos

Modified-Release Drug Delivery Systems: Bioavailability01:30

Modified-Release Drug Delivery Systems: Bioavailability

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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: Influencing Factors01:22

Bioavailability: Influencing Factors

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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...
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Bioavailability Enhancement: Determination and Conceptual Approaches in Overcoming Bioavailability Problems01:22

Bioavailability Enhancement: Determination and Conceptual Approaches in Overcoming Bioavailability Problems

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Bioavailability is a critical pharmacological concept that measures the extent and rate at which an active drug ingredient or therapeutic moiety enters the systemic circulation, remaining unchanged. It's a pivotal factor in determining a drug's efficacy and safety.The Biopharmaceutics Classification System (BCS) plays an essential role in drug development by categorizing drugs into four classes based on their solubility and permeability. This classification aids in understanding drug absorption...
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Bioavailability: Overview01:17

Bioavailability: Overview

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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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Bioavailability: Overview01:13

Bioavailability: Overview

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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 Study Design: Single Versus Multiple Dose Studies01:11

Bioavailability Study Design: Single Versus Multiple Dose Studies

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Bioavailability studies are essential for understanding how a drug is absorbed, distributed, metabolized, and excreted in the body. These studies assess the extent and rate at which the active pharmaceutical agent becomes available at the site of action. The design of bioavailability studies can involve single-dose or multiple-dose regimens, each with distinct advantages and limitations.Single-dose studies are the preferred approach due to their simplicity and reduced drug exposure for...
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How does curcumin work with poor bioavailability? Clues from experimental and theoretical studies.

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Area of Science:

  • Natural product chemistry
  • Neuropharmacology
  • Biochemistry

Background:

  • Curcumin exhibits diverse biological activities but suffers from poor bioavailability.
  • This limitation hinders its clinical application for diseases like Alzheimer's disease (AD).

Purpose of the Study:

  • To investigate and compare the biological activities of curcumin and its degradation products against Alzheimer's disease.
  • To elucidate the role of curcumin degradation products in its observed pharmacological effects.

Main Methods:

  • Experimental assays for superoxide anion radical scavenging and amyloid-beta (Aβ) fibril formation inhibition.
  • Enzymatic inhibition assays and molecular docking simulations.

Main Results:

  • Curcumin degradation products demonstrated superior superoxide radical scavenging and Aβ fibril formation inhibition compared to curcumin.
  • Docking simulations indicated significant contributions of degradation products to enzymatic inhibition activities.

Conclusions:

  • Curcumin's degradation products are crucial contributors to its diverse biological activities, particularly against Alzheimer's disease.
  • These findings offer new perspectives on curcumin's pharmacology and therapeutic potential, addressing bioavailability challenges.