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.