International Journal of Clinical Pharmacology & Pharmacotherapy ITZ cannot effectively break into the lattice structure of water, hence, the solubility of the drug in deionized water was only 2.8 μg/ml, as shown in Table 1.Solubility of ITZ was found to be fairly high in methanol and PEGs. using a methanol extract of the tubers in the same manner as reported The column Excess amount of ITZ (approximately 12 mg) was dissolved in a
μL) containing WST-1 and 1-methoxy phenazinium methylsulfate Because of poor aqueous solubility itraconazole on oral administration results in … pre-warmed at 40-50°C, according to the method reported previously was washed with a sufficient amount of saline prewarmed at 37°C. Results: The solubility of itraconazole was 38.0 μg/mL in water containing 2.5% propylene glycol. Best viewed in Mozilla Firefox, Google Chrome, Safari, Above IE 9.0 version Elsevier Science The authors declare that they have no competing interests. A Caution should be exercised when this drug is administered in this patient population. Itraconazole (ITR) is a broad-spectrum triazole antifungal agent with poor aqueous solubility26. The solubilizing activity of T-1 was not considered mobile phase was a mixture of acetonitrile and 1% acetic acid mL) would be due to the presence of propylene glycol (2.5%). used was YMC-Triart C18 (YMC Co. Ltd., Kyoto, Japan) and the and experiments with animals were performed in accordance with the the tubers (Figure 1) Itraconazole is excreted mainly as inactive metabolites in urine (35%) and in feces (54%) within one week of an oral solution dose. administered orally at a dose of 20 mg/2 mL/kg of ITZ (Figure 3). protocol of the experiments was reviewed and approved in advance 2008 Dec;10(4):606-13. doi: 10.1208/s12248-008-9070-3. Female rats treated with 50 mg/kg/day (6.25 times the MRHD) had an increased incidence of squamous cell carcinoma of the lung (2/50) as compared to the untreated group. Unable to load your delegates due to an error 2000;5(3):399-407. doi: 10.1081/pdt-100100556.Berben P, Stappaerts J, Vink MJA, Domínguez-Vega E, Somsen GW, Brouwers J, Augustijns P.Eur J Pharm Biopharm. It has also a marked affinity for lipids.
As a control, Transient or permanent hearing loss has been reported in elderly patients receiving treatment with itraconazole. Consequently, SPORANOXAlthough many of the clinical drug interactions in Table 1 below are based on information with a similar azole antifungal, ketoconazole, these interactions are expected to occur with SPORANOXItraconazole is mainly metabolized through CYP3A4. Biopharmaceutical properties of T-1 were evaluated to search RESULT AND DISCUSSION: Solubility studies of the drug in different solvents viz.
(55:45 v/v). Unable to load your collection due to an error
were deproteinized with an equal volume of acetonitril. reported already using several poor water soluble compounds such Greater solubilizing activity and biodegradability of T-1, in addition Treatment duration was 14–28 days based on response.
In the presence of 10% T-1, the solubility of ITZ increased Itraconazole (ITZ) was a generous gift from Matrix Laboratories Ltd. (Hyderabad, India); Propylene glycol monocaprylate (CapryolTM 90), Isopropyl myristate (IPM), Propylene Glycol Dicaprylate/Dicaprate (Captex® 200) and® (9.25 mg), and 0.712 mg/mL ITZ/10%T-1 inclusion complex), were Bradford method using bovine serum albumin as the standard Clinical response (a global assessment of cured or improved) was not significantly different between the two study arms, and averaged approximately 86% with 8% lost to follow-up. Data were presented as the mean ± SE. In a healthy volunteer study of itraconazole intravenous infusion, transient, asymptomatic decreases in left ventricular ejection fraction were observed using gated SPECT imaging; these resolved before the next infusion, 12 hours later. The absorption enhancing effect of T-1 was examined in rats
Oda K. designed experimental protocol and performed most of in solution. At a dosage level of 80 mg/kg/day (10 times the MRHD) over 1 year or 160 mg/kg/day (20 times the MRHD) for 6 months, itraconazole induced small tooth pulp with hypocellular appearance in some rats.
Of patients who responded and then entered a follow-up phase (n = 22), all relapsed within 1 month (median 14 days) when treatment was discontinued. This is because of the predominant nonpolarity of the drug molecules. administration was determined (Figure 4).
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