Pharmacokinetics/Pharmacodynamics study of Fixtral SB as compared to supra bioavailable itraconazole and conventional itraconazole

Naqvi, Syed Mujtaba Hussain; Gala, Monil Yogesh Neena; Muchhala, Snehal; Arumugam, Anand; Panigrahi, Dhananjay; Patil, Dipak N.; Rathod, Rahul H.; Mane, Amey

doi:10.5497/wjp.v12.i1.1

Cited by 2 publications

(4 citation statements)

References 20 publications

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“…This indicates that similar therapeutic effect was proven with almost 35% lesser drug as compared to CITZ [1]. With regards to safety, from this study, the test drug was found to be safe and well tolerated which is in line with historical data [7].…”

Section: Discussionsupporting

confidence: 80%

“…Bioequivalence studies form an essential core in the development of new drug [6,7]. According to United States Food and Drug Administration (US FDA) and Central Drugs Standard Control Organization (CDSCO), two drugs are considered bioequivalent if 90% CI of Geometric Mean Ratio (GMR) of primary PK (Cmax, AUC(0-t)) variables fall within the range of 80%-125% [8,9].…”

Section: Discussionmentioning

confidence: 99%

“…Bioavailability of a drug is defined as the extent and rate to which the active drug ingredient or active moiety from the drug product is absorbed and becomes available at the site of drug action. In addition, for the efficacy of any anti-fungal drugs, its AUC/MIC ratio should be correlated [7]. In a recently published clinical study, SITZ 130 mg was found to be bioequivalent to CITZ 200 mg once daily dosing.…”

Section: Discussionmentioning

confidence: 99%

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Open-Label Crossover Oral Bioequivalence Pharmacokinetics Comparison of a Single Dose of Super-bioavailable Itraconazole 130 mg and Innovator SUBA®-Itraconazole Capsules 130 mg (2 x 65 mg) in Healthy Adults Under Fed Conditions

Dhoot

2024

JDR

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Introduction: Itraconazole (ITZ), an antifungal agent taken orally, demonstrates intricate and variable absorption kinetics, significantly impacted by food intake. The invention of Super-Bioavailable Itraconazole (SITZ) has led to a surge in various brands offering different dosages of SB ITZ, overcoming barriers associated with conventional itraconazole. Hence, this study was planned to evaluate the bioequivalence of Itraconazole Capsules 130 mg (Test) of Glenmark Pharmaceuticals Ltd, India, with Innovator SITZ 130 mg (2× 65 mg; Reference) in healthy, adult, male, human subjects under fed condition in addition to safety and tolerability. Materials and methods: A total of 36 subjects were enrolled in an open-label, balanced, randomized, two-treatment, two-sequence, two-period, two-way crossover, single dose oral bioavailability study which was conducted in healthy, adult, human male subjects under fed conditions. Test and reference product were administered sequentially. 22 blood samples per subject were collected as pre and post dose within 2 hours of intake of food. The concentrations of ITZ and Hydroxy-itraconazole (OH-ITZ) in plasma were measured by High-Performance Liquid Chromatography-Tandem Mass Spectrometry (HPLC-MS/MS). Assessment of bioequivalence was done on the basis of the 90% CIs of the differences of least squares treatment means for Ln-transformed Cmax and AUC0-t of ITZ obtained after single-dose administration under fed conditions for Test (T) vs Reference (R) Results: The mean value of the area under curve (AUC0-t) of test drug (SITZ 130 mg) was 4604.98 ng.hr/mL whereas for reference drug (SITZ, 2 x 65 mg), it was 4812.04 ng.hr/mL which was statistically non-significant. The Pharmacokinetic parameters for OH-ITZ measured from both formulations followed a pattern in terms of bioavailability similar to that for the ITZ plasma blood levels for the test/reference ratios for Cmax (100.88%) and AUC0-t (97.44%). Subjects crossed over from one period of administration of either test or reference drugs to a second period with dosing with the opposite drug attained higher Cmax and AUC0-t values for ITZ, than the same subjects administered reference drug in this study. The administration of both the drugs were well tolerated by all the subjects with no added adverse events Conclusion: The pharmacokinetics activity was found to be comparable and bioequivalent between test product at 130 mg dose and innovator itraconazole 130 mg (2x 65 mg). Also, both the drugs were found to be safe and well tolerated with no adverse effects.

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Section: Discussionsupporting

confidence: 80%

Section: Discussionmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

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Open-Label Crossover Oral Bioequivalence Pharmacokinetics Comparison of a Single Dose of Super-bioavailable Itraconazole 130 mg and Innovator SUBA®-Itraconazole Capsules 130 mg (2 x 65 mg) in Healthy Adults Under Fed Conditions

Dhoot

2024

JDR

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“…It is a weakly basic drug with a pH-dependent (pKa=3.7) dissolution rate and requires an acidic gastric environment for dissolution and absorption. 12,13 It has a bioavailability of 55%, which is influenced by food intake; however, several drawbacks are associated with the use of ITZ-C. 12,14…”

Section: Pharmacokinetics Of Itzmentioning

confidence: 99%

Efficacy of super bioavailable itraconazole in the management of dermatophytosis in India

M.,

Hawelia,

Bharadwaj

et al. 2023

Int J Res Dermatol

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Itraconazole (ITZ) is a commonly prescribed oral antifungal agent in India and has a low minimum inhibitory concentration when compared to other oral antifungals. However, clinicians have reported inconsistent clinical responses despite its high skin levels, which may be due to variations in pelletization parameters, which affect its bioavailability and serum levels. Conventional ITZ has a maximum bioavailability of 55%; however, this is unpredictable and inconsistent. In contrast, the novel ITZ formulation, super bioavailable ITZ (ITZ-SB), has targeted drug release in the small intestine, resulting in predictable serum levels with minimal interindividual variability. This makes it a potentially useful drug in treating recalcitrant dermatophytosis. This expert opinion highlights the benefits of novel ITZ-SB with the incorporation of SUBA® technology. The SUBA® technology improves the bioavailability of poorly soluble drugs by ‘solid dispersion’ in polymer to increase drug absorbency. This technology also has potential to reduce variability in absorption and adverse effects. Benefits of this technology include more predictable clinical response and lower drug quantities necessary to achieve therapeutic blood levels, making it a promising treatment option for recalcitrant dermatophytosis. Fixtral SB, which uses this technology, is a novel weapon in the arsenal of treatments for superficial mycoses.

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Pharmacokinetics/Pharmacodynamics study of Fixtral SB as compared to supra bioavailable itraconazole and conventional itraconazole

Cited by 2 publications

References 20 publications

Open-Label Crossover Oral Bioequivalence Pharmacokinetics Comparison of a Single Dose of Super-bioavailable Itraconazole 130 mg and Innovator SUBA®-Itraconazole Capsules 130 mg (2 x 65 mg) in Healthy Adults Under Fed Conditions

Open-Label Crossover Oral Bioequivalence Pharmacokinetics Comparison of a Single Dose of Super-bioavailable Itraconazole 130 mg and Innovator SUBA®-Itraconazole Capsules 130 mg (2 x 65 mg) in Healthy Adults Under Fed Conditions

Efficacy of super bioavailable itraconazole in the management of dermatophytosis in India

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