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Factors Influencing Drug Absorption: Drug Dissolution

Factors 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...

Factors Affecting Dissolution: Polymorphism, Amorphism and Pseudopolymorphism

Factors 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).
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Drug Dissolution: Requirements and Profile Comparison

The acceptance criteria for dissolution profile data are anchored in Q values, representing the percentage of drug dissolved within a specified period. This assessment unfolds in three stages:First Stage: The test passes if all six drug dosage units are equal to or greater than Q plus 5%; otherwise, the sample proceeds to the second stage.Second Stage: The average of twelve units must be equal to or greater than Q, with no unit falling below Q - 15% to pass; if not, it progresses to the final...

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...

In Vitro Drug Dissolution: Alternative Methods

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Alternative drug dissolution methods include the rotating bottle, intrinsic dissolution test, peristalsis, and the Franz diffusion cell method. The rotating bottle method involves meticulously rotating tightly capped controlled-release beads in a temperature-controlled bath. Periodic decanting of samples allows for residue assay, followed by refilling with fresh medium and testing at various pH levels to emulate the gastrointestinal tract conditions.In contrast, the intrinsic dissolution test...

In Vitro Drug Dissolution: Compendial Testing Models II

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Related Experiment Video

Updated: Oct 31, 2025

Transport Properties of Ibuprofen Encapsulated in Cyclodextrin Nanosponge Hydrogels: A Proton HR-MAS NMR Spectroscopy Study

Transport Properties of Ibuprofen Encapsulated in Cyclodextrin Nanosponge Hydrogels: A Proton HR-MAS NMR Spectroscopy Study

Published on: August 15, 2016

Amorphous Drug Solubility and Maximum Free Drug Concentrations in Cyclodextrin Solutions: A Quantitative Study Using

Keisuke Ueda¹, Kenjirou Higashi¹, Kunikazu Moribe¹

¹Graduate School of Pharmaceutical Sciences, Chiba University, 1-8-1 Inohana, Chuo-ku, Chiba 260-8675, Japan.

Molecular Pharmaceutics

|June 28, 2021

Summary

Cyclodextrins (CDs) enhance amorphous drug solubility, but their impact on maximum drug activity varies. Dimethyl-β-cyclodextrin (DM-β-CD) reduces drug activity by partitioning into drug-rich phases, unlike other CDs.

Keywords:

1H NMR NMR diffusometry amorphous solubility cyclodextrin drug supersaturation liquid−liquid phase separation

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Last Updated: Oct 31, 2025

Transport Properties of Ibuprofen Encapsulated in Cyclodextrin Nanosponge Hydrogels: A Proton HR-MAS NMR Spectroscopy Study

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Published on: August 15, 2016

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A Package of Established Analytical Tools to Investigate the Solid-State Alteration of Lipid-Based Excipients

A Package of Established Analytical Tools to Investigate the Solid-State Alteration of Lipid-Based Excipients

Published on: August 9, 2022

Area of Science:

Pharmaceutical Sciences
Physical Chemistry
Drug Delivery

Background:

Cyclodextrins (CDs) are established solubilizing agents for poorly water-soluble drugs.
Understanding CD-drug interactions is crucial for optimizing drug formulation and bioavailability.

Purpose of the Study:

To investigate the effect of different cyclodextrins (β-CD, DM-β-CD, HP-β-CD) on the amorphous solubility and maximum thermodynamic activity of ibuprofen (IBP).
To elucidate the mechanism behind the observed changes in drug solubility and activity, particularly concerning liquid-liquid phase separation (LLPS).

Main Methods:

Amorphous solubility measurements of ibuprofen in various cyclodextrin solutions.
Nuclear Magnetic Resonance (NMR) spectroscopy and diffusometry to analyze drug-cyclodextrin interactions and phase behavior.
Investigation of liquid-liquid phase separation (LLPS) phenomena in drug-supersaturated solutions.

Main Results:

Amorphous solubility of ibuprofen increased linearly with cyclodextrin concentration, irrespective of crystalline solubility plateaus.
Dimethyl-β-cyclodextrin (DM-β-CD) partitioned into the ibuprofen-rich phase, reducing the maximum thermodynamic activity of ibuprofen in the aqueous phase.
β-cyclodextrin (β-CD) and hydroxypropyl-β-CD (HP-β-CD) showed minimal partitioning and did not significantly alter the maximum free ibuprofen concentration.

Conclusions:

The partitioning behavior of cyclodextrins into drug-rich phases significantly influences drug's maximum thermodynamic activity and apparent amorphous solubility.
DM-β-CD's hydrophobic substituents facilitate its entry into the drug-rich phase, impacting drug's chemical potential and activity.
These findings highlight the importance of considering cyclodextrin partitioning for effective formulation of poorly water-soluble drugs.