FORMULATION AND CHARACTERIZATION OF ODT USING DIFFERENT CO-PROCESS CONTAINNG DACLATSVIR: IN VITRO AND IN VIVO PHARMACOKINETICS STUDY ON HEALTHY VOLUNTEERS FOR HEPATITIS C TREATMENT

Authors

  • DALIA ABOUHUSSEIN Pharmaceutics Department, Egyptian Drug Authority (EDA), Cairo, Egypt
  • MAHMOUD H. TEAIMA Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo, Egypt https://orcid.org/0000-0002-7565-301X
  • ADI AL-NUSEIRAT Access to Medicines and Health Technologies Unit, World Health Organization Office for the Eastern Mediterranean Region, Cairo, Egypt https://orcid.org/0000-0002-7259-7577
  • OSAMA BADARY Department of Clinical Pharmacy Practice, Faculty of Pharmacy, the British University in Egypt, Cairo, Egypt
  • MOHAMED A. EL-NABARAWI Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo, Egypt
  • REHAB ABD EL-MONEM College of Pharmacy, Misr University for Science and Technology, Giza, Egypt

DOI:

https://doi.org/10.22159/ijap.2022v14i5.44289

Keywords:

Oral disintegrating Tablets, Co-processed Excipients, Daclatasvir Dihydrochloride, Hepatitis C, Direct Compression, In-vivo Pharmacokinetic Study

Abstract

Objective: This study aimed to prepare and evaluate oral disintegrating tablets (ODTs) of Daclatasvir dihydrochloride (DCV) using different co-processed excipients to enhance drug dissolution and improve oral bioavailability for treatment of hepatitis C infection.

Methods: Ten Daclatasvir-ODTs formulae were prepared using co-processed excipients via direct compression. The prepared formulae were evaluated according to taste masking, weight variation, thickness, friability, hardness, drug content, and wetting time. In-vitro disintegration time, in-vivo disintegration time, and in-vitro dissolution tests were also evaluated and taken as parameters for the selection of the best formula. The selected best formula was subjected to an in-vivo study on volunteers and compared to a marketed product.

Results: All DCV-ODTs had acceptable physical properties in accordance with pharmacopeial standards. DCV-ODTs prepared with Pharmaburst® (F10) recorded the shortest wetting time (14±0.08s), fastest invitro disintegration time (46±0.16s), shortest in-vivo disintegration time (27±0.16s), and attained the fastest onset of dissolution (94.3±0.03 %) at 5 min to all other excipients and has been identified as the best formula. The in-vivo pharmacokinetic study showed that Pharmaburst-based formula has a significant Cmax increase of (2.17 ± 0.28 μg/ml) compared to (1.42±0.59) for the marketed product and a significant decrease of Tmax to 60 min instead of 110 min for the marketed product.

Conclusion: The in-vivo pharmacokinetic study in humans showed that the ODTs was found to be appropriate for delivery of Daclatasvir with a faster drug absorption rate when compared to the marketed products with applicable taste related to the nature of dosage form.

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Published

04-07-2022

How to Cite

ABOUHUSSEIN, D., TEAIMA, M. H., AL-NUSEIRAT, A., BADARY, O., EL-NABARAWI, M. A., & EL-MONEM, R. A. (2022). FORMULATION AND CHARACTERIZATION OF ODT USING DIFFERENT CO-PROCESS CONTAINNG DACLATSVIR: IN VITRO AND IN VIVO PHARMACOKINETICS STUDY ON HEALTHY VOLUNTEERS FOR HEPATITIS C TREATMENT. International Journal of Applied Pharmaceutics, 14(5). https://doi.org/10.22159/ijap.2022v14i5.44289

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