Romanian Society of Pharmaceutical Sciences

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DEVELOPMENT, PHYSICAL-CHEMICAL CHARACTERIZATION AND IN VITRO ANTIBACTERIAL ACTIVITY EVALUATION OF A FIXED-DOSE COMBINATION ISOHYDRAFURAL-METHYLURACIL HYDROPHILIC OINTMENT

LUCIA MARIA RUS 1#, ELENA DONICI 2#, VLADIMIR VALICA 2,3, VIOREL PRISACARI 4, IOAN TOMUȚĂ 5, DIANA ȘEPELI 6, SIMONA CODRUȚA HEGHEȘ 1, CRISTINA ADELA IUGA 1,7*, LIVIA UNCU 2,3

1.“Iuliu Hațieganu” University of Medicine and Pharmacy, Faculty of Pharmacy, Department of Pharmaceutical Analysis, 6 Louis Pasteur, 400349 Cluj-Napoca, Romania
2.“Nicolae Testemițanu” State University of Medicine and Pharmacy, Faculty of Pharmacy, Department of Pharmaceutical and Toxicological Chemistry, Chișinău, Republic of Moldova
3“Nicolae Testemițanu” State University of Medicine and Pharmacy, Scientific Center of Medicine, Chișinău, Republic of Moldova
4.“Nicolae Testemițanu” State University of Medicine and Pharmacy, Scientific Laboratory “Hospital infections”, Chișinău, Republic of Moldova
5.“Iuliu Hațieganu” University of Medicine and Pharmacy Cluj-Napoca, Faculty of Pharmacy, Department of Pharmaceutical Technology and Biopharmaceutics, 41 Victor Babeș, 400012 Cluj-Napoca, Romania
6.The Institute of Chemistry of the Academy of Sciences of Moldova, 3 Academiei, Chișinău, Republic of Moldova
7.“Iuliu Hațieganu” University of Medicine and Pharmacy, Department of Proteomics and Metabolomics, MedFuture - Research Centre for Advanced Medicine, 8 Victor Babeș, 400000 Cluj-Napoca, Romania

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This research was focused on the pharmaceutical development of a novel, fixed-dose combination isohydrafural-methyluracil ointment on a water soluble base - polyethylene glycol (PEG). Differential scanning calorimetry (DSC) and Fourier transform infra-red spectroscopy (FTIR) were applied in order to determine the compatibility between active pharmaceutical ingredients (APIs) and between APIs - excipients. Nine formulations (F1 - F9) were tested for: physical appearance and homogeneity, pH, viscosity and osmotic activity. The optimal formulation presented the concentrations of PEG 400 - 76.72%, PEG 1500 - 19.18% and a fixed-dose combination of 0.1% isohydrafural and 4% methyluracil. It showed higher antibacterial properties both to Gram-positive and Gram-negative bacteria than nitrofural 2% ointment (Furacilin®, Belarus). The long-term stability testing of the optimized formulation of isohydrafural and methyluracil revealed the shelf-life of two years.