Related Experiment Video
Updated: Aug 10, 2026
10:52
A Novel Method of Drug Administration to Multiple Zebrafish (Danio rerio) and the Quantification of Withdrawal
Published on: November 12, 2014
Deaggregation during the dissolution of benzodiazepines in interactive mixtures
1Department of Pharmaceutics, Victorian College of Pharmacy, Monash University, Parkville, Australia.
Journal of Pharmaceutical Sciences
|April 3, 1999
Summary
Surfactants like sodium lauryl sulfate significantly enhance benzodiazepine dissolution by deaggregating particles and increasing dissolution rates in interactive mixtures. Sodium lauryl sulfate proved more effective than cetrimide for improving drug dissolution.
Area of Science:
- Pharmaceutical Sciences
- Physical Chemistry
- Materials Science
Background:
- Benzodiazepines are a class of psychoactive drugs.
- Drug dissolution is critical for bioavailability.
- Interactive mixtures can affect drug dissolution properties.
Purpose of the Study:
- To investigate the impact of surfactants on benzodiazepine dissolution.
- To analyze dissolution from both dispersed and aggregated drug particles.
- To model dissolution kinetics using multiexponential equations.
Main Methods:
- Utilized USP/NF paddle method for dissolution testing.
- Employed ternary interactive mixtures with micronized benzodiazepines and surfactants on a lactose carrier.
- Applied a Marquardt-Levenberg nonlinear least squares algorithm for data analysis.
Main Results:
- Increasing surfactant concentration (sodium lauryl sulfate, cetrimide) markedly increased benzodiazepine dissolution rates.
- Sodium lauryl sulfate reduced drug aggregates from 85% to <10% and doubled the dispersed particle dissolution rate constant.
- Surfactant presence in the particulate matrix was crucial for deaggregation, with sodium lauryl sulfate being more potent than cetrimide.
Conclusions:
- Surfactants effectively enhance benzodiazepine dissolution through particle deaggregation and increased dissolution rate constants.
- The formulation of interactive mixtures with specific surfactants can optimize drug release profiles.
- Sodium lauryl sulfate demonstrates superior efficacy in deaggregating benzodiazepine particles compared to cetrimide.
Related Concept Videos
04:01Factors Affecting Solubility
Compared with pure water, the solubility of an ionic compound is less in aqueous solutions containing a common ion (one also produced by dissolution of the ionic compound). This is an example of a phenomenon known as the common ion effect, which is a consequence of the law of mass action that may be explained using Le Chȃtelier’s principle. Consider the dissolution of silver iodide:
01:14CNS Depressants: Barbiturates and Benzodiazepines
CNS depressants include drugs from the category of barbiturates and benzodiazepines. They are valuable medications for managing anxiety disorders and insomnia. Barbiturates, once used to induce and maintain sleep, have been replaced mainly by benzodiazepines due to barbiturate's toxicity, tolerance, and overdose risks. They interact with GABAA receptors, leading to sedation at low doses and potentially coma and death at higher doses. Phenobarbital, a long-acting barbiturate, possesses...
01:29Anxiolytic Drugs: Benzodiazepines and Buspirone
Benzodiazepines are a class of anxiolytic drugs known for their rapid efficacy and high therapeutic-to-lethal dose ratio, but with a potential risk of drug dependence. These drugs are lipophilic, allowing for rapid absorption after oral administration, eventually reaching the central nervous system (CNS). Once in the CNS, benzodiazepines bind to the allosteric site of the GABAA receptor. This binding enhances the inhibitory effects of the neurotransmitter GABA. By doing so, they prevent...
01:19Sedatives and Hypnotics Drugs: Benzodiazepines
Benzodiazepines have both sedative and hypnotic properties. They include compounds such as diazepam (Valium) and alprazolam (Xanax). Structurally, their cores are similar, consisting of the fusion of a benzene ring and a diazepine ring, but they share a common mechanism of action in the central nervous system (CNS).
Benzodiazepines work by enhancing the effects of the inhibitory neurotransmitter GABA. They bind to the GABAA receptor, increasing its affinity for GABA, which opens chloride...
Benzodiazepines work by enhancing the effects of the inhibitory neurotransmitter GABA. They bind to the GABAA receptor, increasing its affinity for GABA, which opens chloride...
01:15Theories of Dissolution: Diffusion Layer Model
Dissolution, the process by which drug particles dissolve in a solvent, is explained by the diffusion layer model, a theoretical framework that simulates the absorption of oral drugs and allows us to analyze experimental data.
This process starts with a thin layer, saturated with the drug, forming at the interface between the solid and liquid. The solute then diffuses from this layer into the main solution. The Noyes-Whitney equation suggests that the rate of dissolution relies on the diffusion...
This process starts with a thin layer, saturated with the drug, forming at the interface between the solid and liquid. The solute then diffuses from this layer into the main solution. The Noyes-Whitney equation suggests that the rate of dissolution relies on the diffusion...
01:09Theories of Dissolution: The Danckwerts' Model and Interfacial Barrier Model
Various dissolution theories provide insight into the factors that influence the dissolution rate. Danckwerts' Model suggests that turbulence, rather than a stagnant layer, characterizes the dissolution medium at the solid-liquid interface. In this model, the agitated solvent contains macroscopic packets that move to the interface via eddy currents, facilitating the absorption and delivery of the drug to the bulk solution. The regular replenishment of solvent packets maintains the concentration...