Is itraconazole water soluble?
Is itraconazole water soluble?
Introduction
| Itraconazole: Physicochemical Properties | |
|---|---|
| Melting Point | 170°C |
| Solubility – 0.1 N HCl | 4 – 6 μg/mL |
| Solubility – Water | 1 – 4 ng/mL |
| LogP | 5.66 |
How do you increase the solubility of a lipophilic drug?
A number of methodologies can be adapted to improve solubilization of poor water-soluble drugs and further to improve its bioavailability.
- Particle size reduction.
- Nanosuspension technology.
- Surfactant.
- Salt formation.
- pH adjustment.
- Hydrotrophy.
- Solid dispersion.
How co solvents increase the solubility of poorly soluble drugs?
Thus, the polarity of solvents is an important factor governing the solubility of drugs. Hydrophobicity of solvents also showed that the solubility increases with the solvent’s hydrophobicity. However, polarity and hydrophobicity are not only the factors involved.
Can I crush itraconazole?
The itraconazole capsule should be taken with food. Swallow the capsule whole and do not crush, chew, break, or open it.
How do you increase the bioavailability of itraconazole?
Absorption of the capsule formulation is enhance by high-fat food and at acidic pH (15). Thus, dissolution of the capsules can be facilitated in the stomach using a cola drink or a vitamin C-containing beverage at an acidic pH between 1 and 4 (16, 17).
What is the need to enhance the solubility of a poorly soluble drug?
Various techniques are used for the enhancement of the solubility of poorly soluble drugs which include physical and chemical modifications of drug and other methods like particle size reduction, crystal engineering, salt formation, solid dispersion, use of surfactant, complexation, and so forth.
What is a poorly soluble drug?
Examples of poorly soluble compounds that use Micellar solubilization are antidiabetic drugs, gliclazide, glyburide, glimepiride, glipizide, repaglinide, pioglitazone, and rosiglitazone [53].
How does co solvent increase solubility?
This process is known as cosolvency, and the solvents used to increase solubility are known as cosolvent. Cosolvent system works by reducing the interfacial tension between the aqueous solution and hydrophobic solute. It is also commonly referred to as solvent blending.
Which co solvent increases solubility?
Co-solvent solubilization approach has been used to enhance the solubility of seven antidiabetic drugs: gliclazide, glyburide, glipizide, glimepiride, repaglinide, pioglitazone, and roziglitazone.
What is the solubility of itraconazole in micelles?
Itraconazole solubility up to 3.6 g/L is reached in anionic micelles at pH = 3. Electrostatic attraction between the drug and surfactant molecules drives the effect. Itraconazole has a charge of 2+ at these conditions ( 1 H NMR results).
What is the pKa of itraconazole?
Itraconazole is weakly basic (pKa =3.7) and highly hydrophobic drug. It is categorized as a BCS class II drug.
Do Surfactants affect solubilization capacity of the “brick-dust” molecule itraconazole?
Although surfactants are frequently used in enabling formulations of poorly water-soluble drugs, the link between their structure and drug solubilization capacity is still unclear. We studied the solubilization of the “brick-dust” molecule itraconazole by 16 surfactants and 3 phospholipid:surfactant mixtures.
