Bioequivalence Study of 100-mg Cilostazol Tablets in Healthy Thai Adult Volunteers

Chatsiricharoenkul, Somruedee; Nanchaipruek, Yanisorn; Manopinives, Patcharaporn; Atakulreka, Suparat; Niyomnaitham, Suvimol

doi:10.1016/j.curtheres.2019.06.004

Cited by 2 publications

(2 citation statements)

References 24 publications

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“…The PK profile of cilostazol has been reported 10,14 . The maximum plasma concentration of cilostazol occurs ~3 h after administration 15 . Hepatic metabolism is the major route of elimination for cilostazol.…”

Section: Introductionmentioning

confidence: 99%

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Physiologically based absorption modeling to predict the bioequivalence of two cilostazol formulations

Wang,

Zhao,

Luo

et al. 2023

Clinical Translational Sci

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In vivo pharmacokinetic simulations and virtual bioequivalence evaluation of cilostazol have not yet been described for humans. Here, we successfully developed a physiologically based absorption model to simulate plasma concentrations of cilostazol. In addition, virtual population simulations integrating dissolution of 0.3% sodium dodecyl sulfate water media were executed to evaluate the bioequivalence of test and reference formulations. Simulation results show that test and reference formulations were bioequivalent among 28 subjects, but not nine subjects, consistent with clinical studies. The model proved to be an important tool to show potential bioequivalence for cilostazol. This finding may facilitate understanding of the potential risks during the development of generic products.

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Section: Introductionmentioning

confidence: 99%

“…10,14 The maximum plasma concentration of cilostazol occurs ~3 h after administration. 15 Hepatic metabolism is the major route of elimination for cilostazol. Two of its metabolites, 3,4-dehydro-cilostazol (OPC-13015) and 4′-trans-hydroxy-cilostazol (OPC-13213), are identifiable and considered pharmacologically active.…”

Section: Introductionmentioning

confidence: 99%

Physiologically based absorption modeling to predict the bioequivalence of two cilostazol formulations

Wang,

Zhao,

Luo

et al. 2023

Clinical Translational Sci

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Development and Assessment of the Cilostazol Solid Dispersion Employing Melt and Solvent Evaporation Method and Its Comparison

NARAYANANKUTTY ANJANA,

KUMAR,

B. S.

et al. 2023

Int J App Pharm

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Objective: Development and assessment of the Cilostazol solid dispersion employing melt and solvent evaporation method and its comparison. BCS class II and IV drugs are low solubility and low permeability properties. Most of the active drugs are pharmacologically ineffective due to a lack of solubility and permeability. To overcome these problems Solid Dispersion (SD) is one of the best conventional methods. The objective of this study is to improve the dissolution rate of Cilostazol using economical and simple solid dispersion technique. Methods: Physicochemical properties of Cilostazol was studied. Cilostazol and polymers (PEG 6000 and PVPK30) interactions were studied by FT-IR spectroscopy. SD was prepared using PVP K30 polymer by melt and solvent evaporation, and the polymer interactions of Cilostazol, Physical Mixture (PM), and SD were studied using FT-IR. Using a USP dissolution type 2 test apparatus (n=3) and settings of 50 rpm and 37 °C 0.5 °C, in vitro dissolution experiments for Cilostazol, PM and SD were conducted. Dissolution study and saturation solubility study was the main evaluating parameters. Results: The FTIR study confirmed sharp peaks in the spectrum without merging, indicating that no drug interactions were present in the PM and SD formulations. Solubility and dissolution studies confirmed that drug release patterns of the pure drugs Cilostazol, PM (1:3), and SD (1:3) resulted in a markedly higher release rate. SD (1:3) released 97.2% of the drug after 60 min. PM (1:3) released 68.6% of the drug in 60 min, and the pure drug released 35.4% in 60 min. The formulation stability study confirmed that there was no significant loss of the drug under the storage conditions. The cilostazol SD was formulated using a conventional method. The solubility and drug release increased significantly (p<0.05) compared with Cilostazol and PM. FT-IR studies confirmed that there were no interactions between the drug and the polymer. Conclusion: The present study concluded that cilostazol and PVP K30 Solid Dispersion (SD) was one of the choice used to enhance the solubility and drug release properties. However, in vivo studies are required before clinical application.

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Bioequivalence Study of 100-mg Cilostazol Tablets in Healthy Thai Adult Volunteers

Cited by 2 publications

References 24 publications

Physiologically based absorption modeling to predict the bioequivalence of two cilostazol formulations

Physiologically based absorption modeling to predict the bioequivalence of two cilostazol formulations

Development and Assessment of the Cilostazol Solid Dispersion Employing Melt and Solvent Evaporation Method and Its Comparison

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