Table of Contents
What is the pH of ketoconazole?
It is least stable at pH 1 and most stable at pH 7 [6] . The poor aqueous solubility of ketoconazole is the limitation for topical delivery [3]. …
How does pH affect dissolution rate?
In general, dissolution rate increases with temperature and decreases with pH. The combined effect of pH and temperature is modeled by two independent proton promoted reaction paths. The first reaction path controls the overall dissolution rate at pH ≥ 2.5, whereas the second path controls it below pH 0.5.
Is Ketoconazole acidic or basic?
This study investigates the incorporation of a pH-modifier as a method to increase compound solubility and uses ketoconazole (KZ), which is weakly basic (pKa: 6.5), as a model compound. Organic acids are effective pH-modifiers and are generally used in pharmaceutical industries.
Is ketoconazole soluble in water?
Solubility. Practically insoluble in water; freely soluble in dichloromethane R; soluble in methanol R; sparingly soluble in ethanol (~750 g/l) TS. Ketoconazole contains not less than 99.0\% and not more than the equivalent of 101.0\% of C26H28Cl2N4O4, calculated with reference to the dried substance.
How do you dissolve ketoconazole?
For maximum solubility in aqueous buffers, ketoconazole should first be dissolved in DMF and then diluted with the aqueous buffer of choice. Ketoconazole has a solubility of approximately 0.5 mg/ml in a 1:1 solution of DMF:PBS (pH 7.2) using this method.
Is ketoconazole an acid?
Pharmacokinetics. Ketoconazole requires an acidic environment for dissolution and systemic absorption. It does not enter the central nervous system. Ketoconazole is a potent inhibitor of hepatic P450 enzymes; thus dosage adjustments may be necessary to prevent adverse drug interactions.
Why does pH affect dissolution?
Solubility is Affected by pH By changing the pH of the solution, you can change the charge state of the solute. If the pH of the solution is such that a particular molecule carries no net electric charge, the solute often has minimal solubility and precipitates out of the solution.
Which of the following inhibits ketoconazole absorption?
Absorption of ketoconazole is variable after oral administration, with large variability in peak serum concentrations. Antacids reduce, and food or dilute hydrochloric acid increase, absorption. Renal failure and bone marrow transplantation are associated with reduced absorption.
Is ketoconazole polar?
Ketoconazole is a well documented cause of clinically apparent acute drug induced liver injury and is no longer recommended as a first line antifungal agent….3.1Computed Properties.
| Property Name | Property Value | Reference |
|---|---|---|
| Topological Polar Surface Area | 69.1 Ų | Computed by Cactvs 3.4.8.18 (PubChem release 2021.05.07) |
How do you make ketoconazole?
Ketoconazole ointment was prepared by mixing 1 \% of the medicament with an oleaginous ointment base consisting of 10 \% liquid paraffin and 90 \% soft paraffin.
What is DMSO solution?
DMSO is used topically to decrease pain and speed the healing of wounds, burns, and muscle and skeletal injuries. DMSO is also used topically to treat painful conditions such as headache, inflammation, osteoarthritis, rheumatoid arthritis, and severe facial pain called tic douloureux.
How is ketoconazole absorbed?
Ketoconazole is absorbed from the gastrointestinal tract; it is better absorbed from acidic aqueous solutions, so drugs that alter the pH of the stomach affect ketoconazole absorption. Therapeutic plasma concentrations are maintained for several hours following ketoconazole administration.