Improving the solubility of nevirapine using A hydrotropy and mixed hydrotropy based solid dispersion approach
Jyotsana R Madan1, Virendra J Kamate1, Kamal Dua2,3,4
1Department of Pharmaceutics, Sinhgad Technical Education Society's, Smt. Kashibai Navale College of Pharmacy, Pune, Maharashtra, India.
Polimery W Medycynie
|July 17, 2018
Summary
This study developed a novel mixed hydrotropic solid dispersion technique to enhance nevirapine solubility. This cost-effective method improves bioavailability for poorly soluble drugs like nevirapine, crucial for HIV treatment.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Formulation Development
Background:
- Nevirapine is a reverse transcriptase inhibitor (NNRTI) used for HIV-1 treatment.
- It is a BCS class II drug with absorption limited by dissolution rate.
- Enhancing nevirapine's solubility is key to improving its bioavailability.
Purpose of the Study:
- To develop a fast-dissolving solid dispersion of nevirapine.
- To investigate the use of mixed hydrotropic agents to enhance nevirapine solubility.
- To create a cost-effective formulation for improved drug delivery.
Main Methods:
- Solubility of nevirapine was tested in various concentrations of urea, lactose, citric acid, and mannitol.
- Optimal hydrotropic combinations were identified based on solubility studies.
- Solid dispersions were prepared using a common solvent technique and characterized (XRD, DSC, FTIR).
Main Results:
- A 40% citric acid solution showed the highest nevirapine solubility.
- An optimized ratio of lactose and citric acid (15:25) yielded the best solubility.
- Characterization confirmed no drug-hydrotrope interaction in the prepared solid dispersions.
Conclusions:
- Mixed hydrotropic solid dispersion is a safe, novel, and cost-effective technique.
- This method enhances the bioavailability of poorly water-soluble drugs by dissolving them in a non-ionized form.
- The approach shows potential for improving the delivery of other poorly soluble drugs with bioavailability concerns.
Related Concept Videos
02:55Solubility of Ionic Compounds
68.3K
Solubility is the measure of the maximum amount of solute that can be dissolved in a given quantity of solvent at a given temperature and pressure. Solubility is usually measured in molarity (M) or moles per liter (mol/L). A compound is termed soluble if it dissolves in water.
68.3K
03:07Solubility Equilibria
57.6K
Solubility equilibria are established when the dissolution and precipitation of a solute species occur at equal rates. These equilibria underlie many natural and technological processes, ranging from tooth decay to water purification. An understanding of the factors affecting compound solubility is, therefore, essential to the effective management of these processes. This section applies previously introduced equilibrium concepts and tools to systems involving dissolution and precipitation.
The...
The...
57.6K
04:01Factors Affecting Solubility
37.2K
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:
37.2K
02:19Physical Properties Affecting Solubility
26.6K
Solutions of Gases in Liquids
As for any solution, the solubility of a gas in a liquid is affected by the attractive intermolecular forces between solute and solvent species. Unlike solid and liquid solutes, however, there is no solute-solute intermolecular attraction to overcome when a gaseous solute dissolves in a liquid solvent since the atoms or molecules comprising a gas are far separated and experience negligible interactions. Consequently, solute-solvent interactions are the sole...
As for any solution, the solubility of a gas in a liquid is affected by the attractive intermolecular forces between solute and solvent species. Unlike solid and liquid solutes, however, there is no solute-solute intermolecular attraction to overcome when a gaseous solute dissolves in a liquid solvent since the atoms or molecules comprising a gas are far separated and experience negligible interactions. Consequently, solute-solvent interactions are the sole...
26.6K
02:54Molecular and Ionic Solids
20.2K
Crystalline solids are divided into four types: molecular, ionic, metallic, and covalent network based on the type of constituent units and their interparticle interactions.
Molecular Solids
Molecular crystalline solids, such as ice, sucrose (table sugar), and iodine, are solids that are composed of neutral molecules as their constituent units. These molecules are held together by weak intermolecular forces such as London dispersion forces, dipole-dipole interactions, or hydrogen bonds, which...
Molecular Solids
Molecular crystalline solids, such as ice, sucrose (table sugar), and iodine, are solids that are composed of neutral molecules as their constituent units. These molecules are held together by weak intermolecular forces such as London dispersion forces, dipole-dipole interactions, or hydrogen bonds, which...
20.2K
02:18Network Covalent Solids
16.2K
Network covalent solids contain a three-dimensional network of covalently bonded atoms as found in the crystal structures of nonmetals like diamond, graphite, silicon, and some covalent compounds, such as silicon dioxide (sand) and silicon carbide (carborundum, the abrasive on sandpaper). Many minerals have networks of covalent bonds.
To break or to melt a covalent network solid, covalent bonds must be broken. Because covalent bonds are relatively strong, covalent network solids are typically...
To break or to melt a covalent network solid, covalent bonds must be broken. Because covalent bonds are relatively strong, covalent network solids are typically...
16.2K