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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

Factors Affecting Dissolution: Polymorphism, Amorphism and Pseudopolymorphism

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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: Particle Size and Effective Surface Area01:23

Factors Affecting Dissolution: Particle Size and Effective Surface Area

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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...
655
Drug Delivery: Enteral Route01:18

Drug Delivery: Enteral Route

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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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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

Factors Influencing Drug Absorption: Physicochemical Parameters

192
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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Engineering pH-Dependent Orally Disintegrating Tablets for Modified Indomethacin Release: A Polymer-Based Approach.

Nihad Al-Hashimi1, Eman Zmaily Dahmash2,3, Mouhamad Khoder1

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Summary

This study developed pH-sensitive polymer pellets for orally disintegrating tablets (ODTs) to control indomethacin release. Optimized pellet size ensures tablet integrity and targeted drug delivery, improving patient compliance.

Keywords:
Delayed releaseEudragit L100IndomethacinOrally disintegrating tabletsPH-dependent polymersPellets

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Area of Science:

  • Pharmaceutical Sciences
  • Materials Science
  • Drug Delivery Systems

Background:

  • pH-sensitive polymers are crucial for targeted drug release in pharmaceutical formulations.
  • Orally disintegrating tablets (ODTs) offer improved patient compliance, but achieving controlled release within them presents challenges.
  • Indomethacin (IND), an anti-inflammatory drug, requires careful formulation to minimize gastrointestinal side effects.

Purpose of the Study:

  • To develop delayed-release orally disintegrating tablets (ODTs) for indomethacin (IND) using pH-dependent polymers.
  • To investigate the impact of polymer particle size on the mechanical and pharmaceutical properties of IND-containing pellets and ODTs.
  • To optimize pellet formulation for balanced integrity and controlled drug release characteristics.

Main Methods:

  • Indomethacin (IND) was incorporated into pellets using Eudragit L100, a pH-dependent polymer, via extrusion spheronization with varying particle sizes (45, 60, 93 µm).
  • Pellets were characterized for mechanical properties (Young's modulus, tensile strength) and pharmaceutical properties (aspect ratio, yield).
  • Pellets were embedded into ODT matrices, and their disintegration time and drug release profiles in acidic (pH 1.2) and alkaline (pH 6.8) media were evaluated.

Main Results:

  • Pellet particle size did not significantly affect Young's modulus (YM), indicating consistent elastic properties across sizes.
  • Pellet tensile strength correlated positively with YM, ensuring structural integrity under compression.
  • Pellets made from 63 µm Eudragit L100 demonstrated optimal mechanical and pharmaceutical properties, yielding ODTs with rapid disintegration (14 ± 0.6 s) and modified IND release.
  • The formulation achieved delayed release in acidic conditions (pH 1.2) and immediate release in neutral/alkaline conditions (pH 6.8), confirming pH-dependent drug release.

Conclusions:

  • Optimized pellet integrity is essential for achieving pH-dependent drug release in ODTs.
  • The 63 µm Eudragit L100 pellets provide a promising formulation strategy for controlled indomethacin release in ODTs.
  • This approach enhances drug delivery, potentially improving patient compliance and reducing side effects for irritant drugs, especially in elderly populations.