Open Access, Peer-reviewed
pISSN 2289-0882   eISSN 2383-5427
    J Korean Soc Clin Pharmacol Ther. 2013 Jun;21(1):26-33. Korean.
    Published online Jun 30, 2013.
    https://doi.org/10.12793/jkscpt.2013.21.1.26
    Copyright © 2013 Korean Society for Clinical Pharmacology and Therapeutics
    Original Article

    Comparison of the Population Pharmacokinetics and Safety Between Please Orally Soluble Film and VIAGRA® in Healthy Male Volunteers

    Taegon Hong,1 Jongtae Lee,1 Sangil Jeon,1 Jeongki Paek,1 Hyun Il Kim,2 Seong Shin Kwak,2 Su Jun Park,2 Seunghoon Han,1 and Dong-Seok Yim1
      • 1Department of Pharmacology, College of Medicine, the Catholic University of Korea and Department of Clinical Pharmacology and Therapeutics, Seoul St. Mary's Hospital, Seoul, Republic of Korea.
      • 2CTC BIO Corporation, 93, Ogeum-dong, Songpa-gu, Seoul, Korea.
    • Corresponding author (Email: waystolove@catholic.ac.kr )
    Received May 20, 2013; Revised June 24, 2013; Accepted June 25, 2013.

    Abstract

    Background

    The objective of this study was to compare the pharmacokinetics and safety between newly developed sildenafil (Please Orally Soluble Film) and sildenafil citrate (VIAGRA®) after single oral administration in healthy Korean male subjects.

    Methods

    A randomized, open-label, single dose, 2-way crossover study was conducted in 50 healthy male subjects. Each sequence group consisted of 25 subjects, received a single oral 50 mg dose of Please Orally Soluble Film (test formulation) or VIAGRA® (reference formulation) by study period. Blood samples were obtained during a 24-hour period after dosing. Sildenafil and its metabolite concentrations were determined using validated LC-MS/MS. A non-compartmental pharmacokinetic analysis was performed. Safety was assessed through monitoring of adverse events, vital sign check-up, physical examination, laboratory tests and electrocardiography.

    Results

    All enrolled participants completed the study. The point estimates and 90% confidence intervals of log transformed Cmax and AUClast of the test formulation in comparison to those of reference formulation were 0.9294(0.8353 - 1.0341) and 0.9415 (0.8869 - 0.9994) respectively. The analysis of variance showed no significant influences of formulation, sequence and period on the pharmacokinetic parameters. The frequencies of adverse events were not statistically different between the formulations. No serious adverse event was observed or reported.

    Conclusion

    Please Orally Soluble Film could be considered bioequivalent to VIAGRA® and had similar safety properties in healthy Korean male subjects.

    Keywords
    Sildenafil; Pharmacokinetics; Safety; Healthy subjects

    Figures

    Figure 1
    Mean (standard deviation) plasma concentration-time profile of reference (VIAGRA®) and test (Please Orally Soluble Film) formulation after a single oral administration.

    Tables

    Table 1
    Subject demographics

    Table 2
    Pharmacokinetic parameters of sildenafil and N-desmethyl sildenafil in reference (VIAGRA®) and test (Please Orally Soluble Film) formulation

    Table 3
    Geometric mean ratio and 90% confidence interval for Cmax and AUClast of sildenafil and N-desmethyl sildenafil in test (Please Orally Soluble Film) and reference (VIAGRA®) formulations in healthy male volunteers

    Table 4
    Analysis of variance for pharmacokinetic parameters of sildenafil between reference (VIAGRA®) and test (Please Orally Soluble Film) formulations

    Table 5
    Analysis of variance for pharmacokinetic parameters of N-desmethyl sildenafil between reference (VIAGRA®) and test (Please Orally Soluble Film) formulations

    References

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    MeSH Terms
    Administration, Oral
    Citric Acid
    Cross-Over Studies
    Humans
    Male
    Physical Examination
    Piperazines
    Purines
    Sildenafil Citratea
    Sulfones
    Vital Signs
    Metrics
    Share
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