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Factors Influencing Drug Absorption: Pharmaceutical Parameters01:28

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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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Dissolution kinetics, an essential aspect of oral drug delivery, is significantly influenced by the drug's particle size. According to the Noyes-Whitney dissolution model, the dissolution rate correlates directly with the drug's surface area. The larger the surface area, the higher the drug's solubility in water, leading to a faster drug dissolution rate. Reducing particle size increases the effective surface area, enhancing the dissolution process. Micronization and nanosizing are...
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Factors Affecting Dissolution: Polymorphism, Amorphism and Pseudopolymorphism01:21

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Polymorphism refers to the existence of a drug substance in multiple crystalline forms, known as polymorphs. Recently, this term has been expanded to include solvates (forms containing a solvent), amorphous forms (non-crystalline forms), and desolvated solvates (forms from which the solvent has been removed).
Some polymorphic crystals possess lower aqueous solubility than their amorphous counterparts, leading to incomplete absorption. For instance, the oral suspension of Chloramphenicol, which...
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Factors Influencing Drug Absorption: Drug Dissolution01:27

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The pharmacokinetic journey of drugs from solid oral dosage forms into systemic circulation is multifaceted. It begins with disintegration, a prerequisite ensuring a solid dosage form's subdivision into minute particles. Dissolution occurs next as these granulated entities solubilize in gastrointestinal fluids. This solubilization is crucial for the succeeding stage, permeation, which describes the traversal of the drug across the intestinal membrane and its subsequent entry into the blood...
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Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry01:20

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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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The physicochemical characteristics of drugs play a crucial role in formulating stable and bioavailable drug products. The solubility of a drug, governed by the varying pH along the GI tract and its dissociation constant (pKa), is pivotal in determining its ionization state and absorption rate. Notably, weak acids and bases remain unionized and are absorbed more rapidly.
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3D printed matrix solid forms: Can the drug solubility and dose customisation affect their controlled release

Juliana Dos Santos1,2, Gabriela de Souza Balbinot3, Silvio Buchner4

  • 1Programa de Pós-Graduação em Ciências Farmacêuticas, Faculdade de Farmácia Universidade Federal do Rio Grande do Sul, Avenida Ipiranga, 2752, Porto Alegre, Rio Grande do Sul 90610-000, Brazil.

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3D printed medications using poly(Ɛ-caprolactone) show controlled release. Drug solubility impacts release rates, but dosage form size can be adjusted to customize drug content without altering release behavior.

Keywords:
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Area of Science:

  • Pharmaceutics
  • Materials Science
  • Biomedical Engineering

Background:

  • 3D printing in pharmaceutics is expanding, with research focusing on formulation composition's impact on drug properties.
  • Previous studies examined infill percentage and pore formers in 3D printed drug delivery systems.
  • Further investigation is needed on drug solubility and dosage form size effects on controlled release.

Purpose of the Study:

  • To investigate the influence of dexamethasone solubility and dosage form size on the controlled release from 3D printed poly(Ɛ-caprolactone) matrix solid forms.
  • To assess the printability and mechanical properties of poly(Ɛ-caprolactone) filaments containing different dexamethasone forms.
  • To determine if dosage form size can be used to customize drug content without affecting release profiles.

Main Methods:

  • Fused deposition modeling was used to 3D print poly(Ɛ-caprolactone) matrix solid forms.
  • Filaments incorporated three soluble forms of dexamethasone: free acid (DEX), acetate ester (DEX-A), and phosphate salt (DEX-P).
  • Two different sizes of 3D printed solid forms were produced and tested for drug release.

Main Results:

  • Poly(Ɛ-caprolactone) filaments exhibited suitable mechanical properties and printability.
  • Formulations with DEX-P released approximately 50% of the drug within 10 hours.
  • Formulations with DEX or DEX-A showed only about 9% drug release in the same timeframe.
  • Drug release profiles were nearly identical for different sizes of dosage forms containing the same drug form.

Conclusions:

  • Dexamethasone solubility significantly affects drug release rates from 3D printed matrices.
  • The size of 3D printed dosage forms can be modified to adjust drug content.
  • Adjusting dosage form size allows for drug content customization without altering the controlled release behavior.