Non‐compartmental and population pharmacokinetic analysis of dapsone in healthy NIGERIANS: A pilot study

Author:

Kotila Olayinka A.12ORCID,Ajayi David T.3,Masimirembwa Collen4,Thelingwani Roslyn4ORCID,Odetunde Abayomi5,Falusi Adeyinka G.56,Babalola Chinedum P.1257

Affiliation:

1. Department of Pharmaceutical Chemistry, Faculty of Pharmacy University of Ibadan Ibadan Nigeria

2. Centre for Drug Discovery, Development and Production (CDDDP), Faculty of Pharmacy University of Ibadan Ibadan Nigeria

3. Department of Public Health, College of Basic Medical Sciences Chrisland University Abeokuta Nigeria

4. African Institute for Biomedical Sciences and Technology (AiBST) Harare Zimbabwe

5. Genetic and Bioethics Unit, Institute for Advanced Medical Research and Training (IAMRAT), College of Medicine University of Ibadan Ibadan Nigeria

6. Sickle Cell Hope Alive Foundation Ibadan Nigeria

7. Department of Physiology/Pharmacology, College of Basic Medical Sciences Chrisland University Abeokuta Nigeria

Abstract

AbstractDapsone is employed for both non‐dermatological and dermatological indications but with non‐existent population pharmacokinetics (popPK) data in Nigerians. This study was therefore designed to develop a popPK model in Nigerians. Non‐compartmental analysis and nonlinear mixed effects modelling were utilized for data analysis. Eleven participants administered 50 mg dapsone tablet were included in the analysis. Derived pharmacokinetic parameters were: Cmax = 1.16 ± 0.32 μg/mL, Tmax = 3.77 ± 2.40 h, and t1/2z = 30.23 ± 11.76 h. PopPK model parameter estimates with inter‐individual variability were Tlag = 0.40 h (10.0%, fixed); ka = 1.78 h−1 (75.9%); V/F = 89.25 L (21.6%); and Cl/F = 1.32 Lh−1 (27.7%). Sex was significantly associated with Cl/F, and body weight with V/F. Best popPK model was one‐compartment with lag time, and first‐order absorption and elimination. Sex and body weight significantly influenced the clearance and distribution volume of dapsone respectively.

Publisher

Wiley

Subject

Pharmacology (medical),Pharmacology

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