Xylometazoline base suitable for use in lipophilic drug products: development of production technology and analytical methods for quality control

Abstract

The aim: development of the technology for obtaining the base of xylometazoline, suitable for the development of formulations in combination with essential oils. Development and validation of methods of control of related substances and assay of the obtained base of xylometazoline. Study of the stability of the obtained xylometazoline base under long-term and accelerated conditions. Materials and methods: experimental samples of xylometazoline base were obtained from commercially available xylometazoline hydrochloride and aqueous sodium hydroxide solution. The quality control of the obtained substance was carried out in accordance with the requirements of the internal specification. The analysis of raw materials of xylometazoline hydrochloride was carried out in accordance with the monograph of the European Pharmacopoeia on xylometazoline hydrochloride (Ph. Eur. 10.1, 1162 (01/2008)). Results: a technology for obtaining xylometazoline base from xylometazoline hydrochloride by the action of a 2 % solution of a strong base, namely sodium hydroxide, was developed. Developed and validated methods of quality control of the obtained xylometazoline base according to indicators of related substances and assay. The stability of the substance was studied for 1 year; the results of control under accelerated research conditions meet the requirements of the specification, which allows for establishing a shelf life of 2 years. Conclusions: the technology for obtaining xylometazoline base and quality control methods based on the monograph of the European Pharmacopoeia on xylometazoline hydrochloride was developed. The developed technology ensures the proper quality of the substance in accordance with the requirements of the internal specification. Analytical methods “related substances” and “assay” meet the established criteria during validation. The obtained results were later used to develop a medicine based on xylometazoline and eucalyptus oil – Eukazolin, nasal drops.