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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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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 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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Factors Influencing Drug Absorption: Physicochemical Parameters01:22

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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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Drug Delivery: Enteral Route01:18

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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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Ulcerative colitis is a chronic inflammatory condition primarily affecting the colon and rectum. The primary drugs used in the treatment of ulcerative colitis are aminosalicylates. They exhibit anti-inflammatory and immunosuppressive properties. They modulate inflammatory mediators and inhibit the activity of nuclear factor κB (NF-κB). Aminosalicylates also reduce inflammation by inhibiting prostaglandin and leukotriene production and decreasing neutrophil chemotaxis and superoxide...
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Poly(curcumin β-amino ester)-Based Tablet Formulation for a Sustained Release of Curcumin.

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Polymeric prodrugs like poly(β-amino ester) (PBAE) enhance oral drug delivery for poorly soluble compounds. PBAE tablets offer sustained release and improved stability, though moisture sensitivity requires consideration.

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Area of Science:

  • Materials Science
  • Pharmaceutical Sciences
  • Polymer Chemistry

Background:

  • Oral drug delivery is preferred but limited by poor drug solubility and stability.
  • Amorphous polymeric prodrugs, such as poly(β-amino ester) (PBAE), offer a solution by improving drug characteristics.
  • PBAE hydrogels are biodegradable, pH-responsive, and enhance drug stability and solubility for controlled release.

Purpose of the Study:

  • To evaluate poly(curcumin β-amino ester) (PCBAE) prodrugs in oral tablet formulations.
  • To investigate the sustained drug release potential of PCBAE tablets.
  • To assess the storage stability of PCBAE-based oral formulations.

Main Methods:

  • Synthesis of poly(curcumin β-amino ester) (PCBAE) via a crosslinked amorphous network.
  • Fabrication of PCBAE-based oral tablets.
  • In vitro drug release studies over 16 hours.
  • Preliminary storage stability assessment under standard and accelerated conditions.

Main Results:

  • PCBAE tablets demonstrated sustained release of curcumin for 16 hours.
  • Drug release was driven by the hydrolytic degradation of the PCBAE matrix.
  • Preliminary stability data indicated that PCBAE tablet stability is sensitive to moisture.

Conclusions:

  • PCBAE prodrugs show potential for oral tablet formulations, enabling sustained drug release.
  • The hydrolytic degradation mechanism allows for controlled release of the model drug, curcumin.
  • Moisture control is critical for ensuring the storage stability of these PCBAE-based tablets.