In Vitro – In Vivo Correlation of Pentoxifylline: A Comprehensive Kinetic Analysis
DOI:
https://doi.org/10.24193/subbchem.2024.4.13Keywords:
In Vitro – In Vivo Correlations (IVIVCs), pentoxifylline, in vitro dissolution, bioequivalence, Level A CorrelationAbstract
This study presents an analysis of In Vitro-In Vivo Correlation (IVIVC) for pentoxifylline modified-release tablets, with a focus on deriving robust predictive models. In vitro dissolution tests were conducted in three pH media (1.2, 4.5, and 6.8) to simulate various gastrointestinal conditions. Data was collected under fed conditions from a bioequivalence (BE) study. The modeling and calculations were performed using Phoenix WinNonlin® version 8.4 software, enabling estimation of drug absorption kinetics. A Level A IVIVC model was employed for each in vivo data to establish a direct and reliable correlation between the in vitro dissolution profiles and the in vivo pharmacokinetic data. The determination coefficient (R²) exceeded 0.97, demonstrating a high degree of predictability and robustness in the established IVIVC.
References
1. N. Alimpertis; A. Simitopoulos; A.A. Tsekouras; P. Macheras; Pharm. Res., 2024, 41, 235–246.
2. M.G. Davanço; D.R. Campos; P.D.O. Carvalho; Int J Pharm, 2020, 580,119210.
3. P.K. Tuszyński; J. Szlęk; S. Polak; R. Jachowicz; A Mendyk; Dissolution. Technol., 2018, 20-24.
4. S. Jacob; A.B. Nair; Drug Development Research, 2018, 79, 97–110.
5. Y. Qiu; J.Z. Duan; Pharmaceutical Theory and Practice, 2nd ed.; Academic Press, Amsterdam, 2017, chapter 16.
6. A. Fortuna; J. Bioequiv. Availab., 2011, S3,1-12.
7. P. Kaur, X. Jiang, J. Duan, E. Stier.; AAPS J, 2015,17,1035–1039.
8. S. Suarez-Sharp, M. Li, J. Duan, H. Shah, P. Seo; AAPS J, 2016,18,1379–1390.
9. I. González-García, V. Mangas-Sanjuán, M. Merino-Sanjuán, M. Bermejo; Drug Dev. Ind. Pharm., 2015, 1-13.
10. J.M. Cardot, J.C. Lukas, P. Muniz; AAPS J, 2018, 20, 95.
11. U.S. Department of Health and Human Services, Food and Drug Administration, Center for Drug Evaluation and Research. Guidance for Industry. Waiver of In Vivo Bioavailability and Bioequivalence Studies for Immediate-Release Solid Oral Dosage Forms Based on a Biopharmaceutics Classification System, 2017 [cited 2024 Oct. 12]. Available at: https://digirepo.nlm.nih.gov/master/borndig/101720038/UCM070246.pdf
12. U.S. Department of Health and Human Services, Food and Drug Administration, Center for Drug Evaluation and Research. Draft Guidance, The Use of Physio¬logically Based Pharmacokinetic Analyses Biopharmaceutics Applications for Oral Drug Product Development, Manufacturing Changes, and Controls Guidance for Industry [cited 2024 Oct. 12]. Available at: https://www.fda.gov/media/142500/download
13. European Medicines Agency, Committee for Medicinal Products for Human Use (CHMP), Guideline on quality of oral modified-release products, 2014 [cited 2024 Oct. 12]. Available from: https://www.ema.europa.eu/en/documents/scientific-guideline/guideline-quality-oral-modified-release-products_en.pdf
14. European Medicines Agency, Committee for Medicinal Products for Human Use (CHMP), Guideline on the pharmacokinetic and clinical evaluation of modified-release dosage forms, 2014 [cited 2024 Oct. 12]. Available from: https://www.ema.europa.eu/en/documents/scientific-guideline/guideline-pharmacokinetic-and-clinical-evaluation-modified-release-dosage-forms_en.pdf
15. U.S. Department of Health and Human Services, Food and Drug Administration, Centre for Drug Evaluation and Research. Guidance for Industry. Extended-Release Oral Dosage Forms: Development, Evaluation, and Application of In Vitro/In Vivo Correlations, 1997 [cited 2024 Oct. 12]. Available at: https://www.fda.gov/media/70939/download
16. Health Canada. Guidance Document: Quality (Chemistry and Manufacturing) Guidance: New Drug Submissions (NDSs) and Abbreviated New Drug Submissions (ANDSs). 2017 [cited 2024 Oct. 12]. Available from: https://www.canada.ca/en/health-canada/services/drugs-health-products/drug-products/applications-submissions/guidance-documents/chemical-entity-products-quality/guidance-document-quality-chemistry-manufacturing-guidance-new-drug-submissions-ndss-abbreviated-new-drug-submissions.html
17. U.S. Department of Health and Human Services, Food and Drug Administration, Center for Drug Evaluation and Research. Guidance for Industry: SUPAC-MR: Modified-release Solid Oral Dosage Forms Scale-Up and Postapproval Changes: Chemistry, Manufacturing, and Controls; In Vitro Dissolution Testing and In Vivo Bioequivalence Documentation. 1997 [cited 2024 Oct. 12]. Available from: https://www.fda.gov/regulatory-information/search-fda-guidance-documents/supac-mr-modified-release-solid-oral-dosage-forms-scale-and-postapproval-changes-chemistry
18. N.F. Taha, L.H. Emara; AAPS Pharm.Sci.Tech., 2024, 25, 243.
19. A.R. Pawar, N.A. Shete, P.V. Jadhav, V.K. Deshmukh, J.S. Mehetre; Pharmaceut. Fronts, 2021,3, e200-e207.
20. European Directorate for the Quality of Medicines & HealthCare, European Pharmacopoeia, Pentoxifylline monograph 0851, Ph. Eur. 11th ed., 2020.
21. M.F. McCarty, J.H. O’Keefe, J.J. DiNicolantonio; Open Heart, 2016, 3, e000365.
22. A.M. Shailendrakumar, V.M. Ghate, M. Kinra, S.A. Lewis; AAPS Pharm. Sci. Tech.,2020, 21,118.
23. D.I. Pop, A. Marcovici, M. Oroian, A.M. Gheldiu, L. Vlase; Studia UBB Chemia, 2019, 64, 217-229.
24. Certara. IVIVC Toolkit™ User’s Guide Applies to: IVIVC Toolkit 8.3 for Phoenix WinNonlin® Phoenix WinNonlin 8.3 reference manual user. 2020 [cited 2024 Oct. 12]. Available from: https://onlinehelp.certara.com/phoenix/8.3/responsive_html5_!MasterPage!/IVIVC%20Toolkit%20User%27s%20Guide.pdf
25. J. Fallinborg; Dan Med Bull, 1999, 46(3), 183-196.
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