Related Experiment Video
Updated: Jun 28, 2026
05:44
Formation of Dispersible Taohong Siwu Tablets
Published on: February 3, 2023
Physicochemical interactions between drugs and superdisintegrants.
Nelly Fransén1, Malin Morin, Erik Björk
1Department of Pharmacy, Uppsala University, Sweden.
The Journal of Pharmacy and Pharmacology
|November 13, 2008
Summary
Superdisintegrant-drug interactions were studied to assess in-vivo absorption. At physiological salt concentrations, interactions were minimal, suggesting no significant impact on drug bioavailability.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
Background:
- Superdisintegrants are crucial for rapid drug dissolution.
- Drug physicochemical properties influence interactions with excipients.
- Understanding these interactions is vital for predicting in-vivo performance, especially for mucosal administration.
Purpose of the Study:
- To evaluate the binding interactions between various drugs and superdisintegrants.
- To assess the impact of ionic strength on these interactions.
- To determine the potential influence on in-vivo drug absorption.
Main Methods:
- Spectrophotometric analysis of drug-superdisintegrant binding.
- Study of interactions with sodium starch glycolate (SSG), croscarmellose sodium (CCS), crospovidone, and starch.
- Measurement of interactions at physiological salt concentrations.
- Investigation of release profiles and binding correlation with ionic strength for SSG.
Main Results:
- Anionic superdisintegrants (SSG, CCS) showed ion-exchange interactions.
- Neutral crospovidone exhibited lipophilic interactions with non-ionic drugs.
- Ion-exchange interactions were significantly reduced at physiological salt concentrations.
- Diphenhydramine release was notably affected by salt addition.
Conclusions:
- Buffer choice is critical for in-vitro studies involving ionic drugs.
- Observed drug-superdisintegrant interactions at physiological conditions are unlikely to affect in-vivo bioavailability.
- Superdisintegrant selection should consider drug properties and physiological conditions.
Related Concept Videos
01:28Factors Influencing Drug Absorption: Pharmaceutical Parameters
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...
01:22Factors Influencing Drug Absorption: Physicochemical Parameters
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.
Enhanced drug absorption can be achieved by reducing particle sizes and increasing surface areas, thereby facilitating...
Enhanced drug absorption can be achieved by reducing particle sizes and increasing surface areas, thereby facilitating...
01:23Factors Affecting Dissolution: Particle Size and Effective Surface Area
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 employed to...
01:20Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry
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...
01:27Factors Influencing Drug Absorption: Drug Dissolution
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...
01:21Factors Affecting Dissolution: Polymorphism, Amorphism and Pseudopolymorphism
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...
Some polymorphic crystals possess lower aqueous solubility than their amorphous counterparts, leading to incomplete absorption. For instance, the oral suspension of Chloramphenicol, which...