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Tytuł:
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Pharmacokinetics and bioequivalence assessment of optimized directly compressible Aceclofenac (100 mg) tablet formulation in healthy human subjects.
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Autorzy:
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Bushra R; Department of Pharmaceutics, Faculty of Pharmacy and Pharmaceutical Sciences, University of Karachi, Karachi, Pakistan.
Shoaib MH; Department of Pharmaceutics and Bioavailability and Bioequivalence Research Facility, Faculty of Pharmacy and Pharmaceutical Sciences, University of Karachi, Karachi, Pakistan.
Ali H; Department of Pharmaceutics, Faculty of Pharmacy and Pharmaceutical Sciences, University of Karachi, Karachi, Pakistan.
Ghayas S; Department of Pharmaceutics, Faculty of Pharmacy and Pharmaceutical Sciences, University of Karachi, Karachi, Pakistan.
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Źródło:
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PloS one [PLoS One] 2020 Sep 08; Vol. 15 (9), pp. e0238951. Date of Electronic Publication: 2020 Sep 08 (Print Publication: 2020).
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Typ publikacji:
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Journal Article
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Język:
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English
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Imprint Name(s):
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Original Publication: San Francisco, CA : Public Library of Science
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MeSH Terms:
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Diclofenac/*analogs & derivatives
Adult ; Analysis of Variance ; Area Under Curve ; Chemistry, Pharmaceutical/methods ; Chromatography, High Pressure Liquid/methods ; Cross-Over Studies ; Diclofenac/metabolism ; Diclofenac/pharmacokinetics ; Healthy Volunteers ; Humans ; Male ; Tablets/pharmacokinetics ; Therapeutic Equivalency
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References:
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Sci Pharm. 2015 Feb 02;83(3):501-10. (PMID: 26839834)
Biopharm Drug Dispos. 2009 Dec;30(9):542-50. (PMID: 19876936)
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Eur J Rheumatol. 2017 Mar;4(1):11-18. (PMID: 28293447)
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Substance Nomenclature:
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0 (Tablets)
144O8QL0L1 (Diclofenac)
RPK779R03H (aceclofenac)
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Entry Date(s):
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Date Created: 20200908 Date Completed: 20201030 Latest Revision: 20201030
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Update Code:
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20240105
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PubMed Central ID:
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PMC7478617
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DOI:
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10.1371/journal.pone.0238951
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PMID:
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32898192
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The aim of the study was to determine the various pharmacokinetic parameters of the newly developed cost-effective aceclofenac 100 mg tablet formulation (F-15) and to establish the bioequivalence against the marketed brand (ACEMED). Both products (test and reference) were given to 12 healthy non-smokers male subjects with overnight fasting of >10hr. The study was a randomized, single-dose, open-label, two sequence, and two treatment crossover design, with a washout period of 2 weeks. Blood samples (5 mL) from the human subjects were collected before (0 hr) and after drug administration at 13different time points (0.5, 1, 1.5, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 12 and 18 hrs). The drug plasma concentration was analyzed by a validated RP-HPLC method using a solvent system containing acetonitrile and deionized water (60:40% v/v). Linearity was found to be 0.999 over the drug concentration range of 50μg/mL to 0.05μg/mL with LLOQ and LOD of 0.05μg/mL and 0.025μg/mL respectively. Non-compartmental pharmacokinetic analysis was performed using Kinetica® (ver. 5.1) software. Using the log-transformed data Cmax, AUC0-t, AUC0-∞, AUMCtot, and MRT were calculated. The Cmax of the test and brand was found to be 8.629±1.251μg/mL and 8.478±0.913μg/mL. The AUC0-t and AUC0-∞ of the test and the reference were computed to be 20.890 ±2.2021μg/mL.h, 23.272 ±1.914 μg/mL.h and 19.850 ±2.911 μg/mL.h, 22.890 ± 2.110 μg/mL.h correspondingly. Two-way analysis of variance (ANOVA) test and two one-sided t-test (p>0.05; non-significant) were applied to assess the variation in the period, sequence, subjects, and treatment. Geometric mean ratios for above mentioned pharmacokinetic parameters of reference/test were found within the acceptable FDA limits of 80-125% using 90% CI. There was no inter and intrasubject variation (p> 0.05) that was observed. Therefore, the directly compressible aceclofenac (100 mg) test formulation and the commercial reference tablets were declared to be biosimilar.
Competing Interests: The authors have declared that no competing interests exist.
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