Comparative analysis of serum and sebum concentration of super-bioavailable itraconazole 50 versus 65 mg in healthy adult volunteers

Dhiraj S. Dhoot; Namrata Mahadkar; Gaurav Jain; Prashant Kesharwani

doi:10.18203/issn.2455-4529.IntJResDermatol20223279

Authors

Dhiraj S. Dhoot Global Medical Affairs, Glenmark Pharmaceuticals Ltd. Mumbai, Maharashtra, India
Namrata Mahadkar Global Medical Affairs, Glenmark Pharmaceuticals Ltd. Mumbai, Maharashtra, India
Gaurav Jain Centre of Advanced Formulation Technology, Delhi Pharmaceutical Science and Research University, New Delhi, India
Prashant Kesharwani Department of Pharmaceutics, School of Pharmaceutical Education and Research, Jamia Hamdard, New Delhi, India

DOI:

https://doi.org/10.18203/issn.2455-4529.IntJResDermatol20223279

Keywords:

Serum, Sebum, Super-bioavailable itraconazole, Dermatophytosis

Abstract

Super-bioavailable itraconazole (SBITZ) is a new form of itraconazole which overcomes the pharmacokinetic issues of conventional itraconazole (CITZ). Currently two strengths are approved globally for SBITZ; 50 mg and 65 mg which exhibit greater bioavailability than CITZ and widely prescribed in systemic mycosis and dermatophytosis. Though both the strengths have proven to be bioequivalent with CITZ 100 mg but difference was reported in achieving therapeutic concentration of ITZ in patients. Secondly, skin kinetics study in terms of sebum concentration is lacking for both the strengths.

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References

Abuhelwa AY, Foster DJ, Mudge S, Hayes D, Upton RN. Population pharmacokinetic modeling of itraconazole and hydroxyitraconazole for oral SUBA-itraconazole and sporanox capsule formulations in healthy subjects in fed and fasted states. Antimicrob Agents Chemother. 2015;59(9):5681-96.

Lindsay J, Sandaradura I, Wong K, Arthur C, Stevenson W, Kerridge I et al. Serum levels, safety and tolerability of new formulation SUBA-itraconazole prophylaxis in patients with haematological malignancy or undergoing allogeneic stem cell transplantation. J Antimicrob Chemother. 2017;72(12):3414-9.

Thompson GR 3rd, Lewis P, Mudge S, Patterson TF, Burnett BP. Open-Label Crossover Oral Bioequivalence Pharmacokinetics Comparison for a 3-Day Loading Dose Regimen and 15-Day Steady-State Administration of SUBA-Itraconazole and Conventional Itraconazole Capsules in Healthy Adults. Antimicrob Agents Chemother. 2020;64(8):e00400-20.

Bae SK, Park SJ, Shim EJ, Mun JH, Kim EY, Shin JG et al. Increased oral bioavailability of itraconazole and its active metabolite, 7-hydroxyitraconazole, when co-administered with a vitamin C beverage in healthy participants. J Clin Pharmacol. 2011;51:444-51.

Firooz A, Rajabi-Estarabadi A, Zartab H. Measurement of skin surface sebum. In: Humbert P, Fanian F, Maibach H, Agache P, editors. Agache’s Measuring the Skin. Cham: Springer. 2017.

Cauwenbergh G, Degreef H, Heykants J, Woestenborghs R, Van Rooy P, Haeverans K. Pharmacokinetic profile of orally administered itraconazole in human skin. J Am Acad Dermatol. 1988;18(2 Pt 1):263-8.

Khurana A, Agarwal A, Singh A. Predicting a therapeutic cut-off serum level of itraconazole in recalcitrant tinea corporis and cruris-A prospective trial. Mycoses. 2021;64(12):1480-8.

Sardana K, Mathachan SR. Super bioavailable itraconazole and its place and relevance in recalcitrant dermatophytosis: revisiting skin levels of itraconazole and minimum inhibitory concentration data. Indian Dermatol Online J. 2021;12:1-5.