Development, Physical-Chemical Characterization and in Vitro Antibacterial Activity Evaluation of a Fixed-Dose Combination Isohydrafural-Methyluracil Hydrophilic Ointment

Abstract

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. RezumatAceastă cercetare s-a axat pe dezvoltarea farmaceutică a unui unguent nou, cu combinații fixe de izohidrafural-metiluracil într-o bază hidrosolubilă -de polietilenglicol. Analiza calorimetrică diferențială (DSC) și spectroscopia în infraroșu cu transformantă Fourier (FTIR) au fost aplicate pentru a determina compatibilitatea dintre substanțele active precum și dintre substanțe active și excipienți. Au fost testate nouă formulări privind: aspectul fizic și omogenitatea, pH-ul, vâscozitatea și activitatea osmotică. Formularea optimă a prezentat concentrațiile de PEG 400 -76,72%, PEG 1500 -19,18% și o combinație de doze fixe de 0,1% izohidrafural și 4% metiluracil. Aceasta a prezentat proprietăți antibacteriene superioare atât pentru bacteriile Gram-pozitive cât și pentru cele Gram-negative, față de unguentul de nitrofural 2% (Furacilin ® , Belarus). În urma studiilor de stabilitate în timp real efectuate asupra formulării optimizate a unguentului cu izohidrafural și metiluracil s-a stabilit termenul de valabilitate de doi ani.

Pharmacotechnical and analytical preformulation studies for cannabidiol orodispersible tablets

“…The SeDeM/SeDeM-ODT tools were used and the following parameters were described: dimension, compressibility, flowability, stability, dosage and, disintegration ability. Before starting the SeDeM-ODT characterization, Differential Scanning Calorimetry (DSC) and Fourier Transform-Infrared (FTIR) spectroscopy studies were conducted to observe the eventual analytical incompatibilities ( Moisei et al, 2014 , Todoran et al, 2018 , Rus et al, 2019 ). To obtain orodispersible tablets, excipients from various classes are needed ( Alejandro et al, 2020 , Tawfeek et al, 2020 ).…”

Structural and Thermal Analysis of Cannabidiol Orodispersible Formulations

“…Likewise, good pharmacotechnical and mechanical properties need to be taken into consideration [1,12]. Usually, TG and DSC are used for the characterization of powder and binary mixtures [15]. This method offers an evaluation of the thermal characteristics, dehydration and could be a tool for describing possible interactions between the API and excipients [6,23].…”

“…This method offers an evaluation of the thermal characteristics, dehydration and could be a tool for describing possible interactions between the API and excipients [6,23]. It can be used also in the evaluation of the absorption or desorption of water [15]. In our study thermal analysis was conducted to acquire the thermal properties of the powders and two CBD-ODFs.…”

Ocular Drug Delivery Systems: A Review

“…Ointments An Ophthalmic ointment is a carrier system for topical application that has demonstrated increased bioavailability and sustained drug release. These are comprised of solid and semisolid hydrocarbon molecules (paraffin) and have a melting point of 34°C, the physiological ocular temperature [1,5,[23][24][25][26][27].…”