Optimization of the composition of a nasal medicine with interleukin-1 antagonist β

Keywords: interleukin-1 β (IL-1ra) receptor antagonist, stability, release, nasal form


In the development of new effective and safe drugs an important place is occupied by the issue of ensuring the stability of the dosage form. In this case, a significant contribution to this problem is made directly by the nature of the active pharmaceutical ingredient. Based on our experimental studies, the composition of the base-carrier of the nasal drug with the receptor antagonist intereleukin-1 (IL-1ra) was determined, and the need to add a preservative was identified. However, focusing on the peptide nature of the biologically active component of IL-1ra, it is necessary to take into account the possible lack of stability during storage of the drug with changes in pH.

The aim of the work is to optimize the composition of a nasal drug with an interleukin antagonist (IL-1ra) to increase its storage stability.

As the active pharmaceutical ingredient used a semi-finished solution of the receptor antagonist of interleukin-1 (IL-1ra). Excipients were: sodium carboxymethylcellulose, tween-80, D-panthenol, trilon B, benzalkonium chloride. To ensure the appropriate pH value used phosphate buffer solutions, which were prepared according to State Pharmacopoeia. The study of some indicators of pharmaceutical availability (kinetic indicators) was performed by studying the release of the active ingredient from the drug composition by equilibrium dialysis in purified water. Equilibrium dialysis was performed through Cuprofan cellophane film at 37 ± 0.5 °C in Franz Diffusion Cell System. The content of IL-1ra in the dialysate was determined spectrophotometrically, at certain intervals.

As a result of pharmaco-technological studies to optimize the composition of the nasal agent with IL-1ra, it was found that the developed nasal agent with IL-1ra requires the addition of stabilizers to the composition of the formulation. It was found that the use as stabilizers: phosphate buffer solution 6.0 and trilon B, provides proper release of the active substance from the dosage form and corrects the stability of the hydrogen index over time. The obtained results of pharmaceutical availability indicators indicate that the release of IL-1ra from the nasal form is subject to the first order equation.


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How to Cite
Burlaka, B. S. (2021). Optimization of the composition of a nasal medicine with interleukin-1 antagonist β. Farmatsevtychnyi Zhurnal, (1), 43-49. https://doi.org/10.32352/0367-3057.1.21.05
Pharmaceutical technology