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Related Concept Videos

Factors Influencing Drug Absorption: Pharmaceutical Parameters01:28

Factors Influencing Drug Absorption: Pharmaceutical Parameters

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Solid dosage forms such as tablets and capsules undergo rigorous manufacturing processes to ensure stability and effectiveness. Their dissolution and absorption properties are influenced significantly by the choice of excipients (inactive ingredients that serve various roles in the formulation), and the methodology applied during production. The manufacturing parameters, such as compression force and granulation techniques, significantly affect dissolution rates. Elevated compression forces...
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The enteral drug administration involves three primary routes: oral, sublingual, and buccal. Oral ingestion is the most prevalent, safe, economical, and convenient method for drug administration. However, it has certain drawbacks, including limited absorption due to the drug's low water solubility or poor membrane permeability, possible emesis from GI mucosa irritation, destruction of drugs by digestive enzymes or low gastric pH, and irregular absorption along with food or other drugs.
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Orally administered drugs primarily enter the systemic circulation via passive diffusion through the intestinal membranes. The drug's absorption is influenced by drug stability in the gastrointestinal GI tract, membrane permeability, the surface area available for absorption, luminal drug concentration, and residence time in the lumen. Drug permeability can be enhanced by adjusting the lipophilicity, polarity, or molecular size of the drug, promoting its passive transport across intestinal...
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Bergamot Essential Oil: A Method for Introducing It in Solid Dosage Forms.

Ylenia Zambito1,2, Anna Maria Piras1, Angela Fabiano1

  • 1Department of Pharmacy, University of Pisa, Via Bonanno 33, 56126 Pisa, Italy.

Foods (Basel, Switzerland)
|December 11, 2022
PubMed
Summary
This summary is machine-generated.

This study developed a novel bergamot essential oil (BEO) conjugate, BEO/QA-Ch-MCD, to stabilize volatile compounds and create a solid oral dosage form. The conjugate enhanced stability and masked unpleasant taste, improving potential bioavailability.

Keywords:
bergamot essential oilconjugate chitosan derivative/cyclodextrinmethyl-β-cyclodextrinpolyphenol protectionquaternary ammonium chitosan derivative

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Area of Science:

  • Pharmacology and Drug Delivery
  • Natural Product Chemistry
  • Materials Science

Background:

  • Bergamot essential oil (BEO) exhibits diverse therapeutic properties but contains volatile compounds prone to degradation.
  • Stabilizing BEO's active components, like limonene and polyphenols, is crucial for its pharmaceutical applications.
  • Developing stable, solid oral dosage forms for BEO is necessary to overcome challenges with liquid formulations and unpleasant taste.

Purpose of the Study:

  • To create a stable, solid oral dosage form of bergamot essential oil (BEO) by encapsulating it within a novel quaternary ammonium chitosan derivative (QA-Ch) and methyl-β-cyclodextrin (MCD) conjugate (BEO/QA-Ch-MCD).
  • To enhance the stability of BEO's volatile compounds, eliminate its unpleasant taste, and improve its suitability for oral administration.
  • To evaluate the association efficiency and stability of the encapsulated BEO compared to free BEO and BEO complexed solely with MCD.

Main Methods:

  • Preparation of a BEO/QA-Ch-MCD conjugate via complexation and lyophilization.
  • Determination of association efficiency (AE %) for polyphenols and limonene.
  • Stability assessment of the conjugate under UV stress and simulated gastric fluid conditions, comparing it with free BEO and BEO/MCD.

Main Results:

  • The BEO/QA-Ch-MCD conjugate demonstrated high solubility and significant association efficiency for polyphenols (22.0 ± 0.9%) and limonene (21.9 ± 1.2%).
  • Stability studies indicated superior protection of polyphenols and limonene against degradation under UV stress and simulated gastric fluid compared to free BEO or BEO/MCD.
  • The complexation and lyophilization process successfully converted liquid BEO into a solid dosage form, masking its unpleasant taste.

Conclusions:

  • The novel BEO/QA-Ch-MCD conjugate effectively stabilizes volatile compounds in bergamot essential oil.
  • This formulation provides a solid oral dosage form with masked taste and enhanced stability, suitable for powders, granules, or tablets.
  • The resulting nanosized agglomerates upon contact with physiological fluids may increase the stability and bioavailability of BEO's active components.