Is itraconazole soluble in water?
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 I dissolve itraconazole?
The contents of itraconazole capsules (600 mg) were placed into a mortar with 10 mL of citric acid 1.5% in 5% dextrose in water (D5W) and allowed to dissolve for 20 minutes at 25°C.
What is salt itraconazole?
Itraconazole is an antifungal medication that is used in adults to treat infections caused by fungus. This includes infections in any part of the body including the lungs, mouth or throat, toenails, or fingernails.
How do you increase absorption of itraconazole?
On the basis of the phar- macokinetic data in the present study, we conclude that as with cola, the coadministration of a vitamin C beverage and itraconazole capsules may be useful for achieving maximum absorption of itraconazole in patients with drug- or disease-related gastric hypochlorhydria (pH > 4).
Which two heterocyclic rings are present in itraconazole?
Itraconazole is an N-arylpiperazine that is cis-ketoconazole in which the imidazol-1-yl group is replaced by a 1,2,4-triazol-1-yl group and in which the actyl group attached to the piperazine moiety is replaced by a p-[(+-)1-sec-butyl-5-oxo-1,5-dihydro-4H-1,2,4-triazol-4-yl]phenyl group.
How do you dissolve fluconazole?
A stock solution may be made by dissolving the fluconazole in the solvent of choice. Fluconazole is soluble in organic solvents such as ethanol, DMSO, and dimethyl formamide, which should be purged with an inert gas. The solubility of fluconazole in these solvents is approximately 20, 33, and 16 mg/ml, respectively.
Can itraconazole be crushed?
The itraconazole capsule should be taken with food. Swallow the capsule whole and do not crush, chew, break, or open it. Take itraconazole oral solution (liquid) on an empty stomach, at least 1 hour before or 2 hours after a meal.
How long should itraconazole be taken?
Itraconazole oral solution is usually taken on an empty stomach once or twice a day for 1 to 4 weeks or sometimes longer. Follow the directions on your prescription label carefully, and ask your doctor or pharmacist to explain any part you do not understand.
Can itraconazole be taken without food?
How do you take itraconazole oral solution?
How to use itraconazole oral. Take this medication by mouth without food as directed by your doctor, usually once or twice daily. Swish the solution in your mouth for several seconds, and then swallow. The dosage and length of treatment are based on your medical condition and response to treatment.
What is the mode of action of itraconazole?
Mechanism: Itraconazole acts by inhibiting the fungal cytochrome P-450 dependent enzyme lanosterol 14-α-demethylase. When this enzyme is inhibited it blocks the conversion of lanosterol to ergosterol, which disrupts fungal cell membrane synthesis.
Which is more solubility beta CD or itraconazole?
Aqueous solubility measurements showed that the solubility of the salt, its 1:1, 1:2 and 1:3 (w/w) physical mixtures with beta-cyclodextrin (beta-CD) was 6, 99, 236 and 388 times greater than itraconazole. More than 94% of itraconazole was dissolved out of the salt/beta-CD 1/3 physical mixture after 60min.
What was the purpose of the preparation of itraconazole?
Preparation and evaluation of itraconazole dihydrochloride for the solubility and dissolution rate enhancement The purpose of this work was to explore the feasibility of preparing itraconazole hydrochloride to improve the solubility and dissolution rate.
How long does itraconazole dihydrochloride stay stable?
The stability studies indicated that the physical mixture remained stable for 24 months in assay, the related substances and dissolution.
What should the pKa of itraconazole be?
A pKa of 3.7(1) indicates itraconazole will exist almost entirely in the cation form at pH values of 5 to 9 and therefore volatilization from water and moist soil surfaces is not expected to be an important fate process(SRC).