Development of the powder composition with the sorbing, analgesic and antimicrobial activity based on natural zeolite

Abstract

Introduction. An active lifestyle, playing sports, participating in hiking trips and various competitions, as well as performing certain types of physical labor may be accompanied by injury. Damage of the skin requires its immediate treatment. Powders are an alternative to soft dosage forms, which are usually used for this purpose. Powders are used in acute inflammatory skin diseases, with a hygienic purpose in increased sweating and sebum secretion, to protect the skin from external irritations, as well as for better fixation of ointments and pastes on the skin. Aim. To select the composition of active substances and excipients for creating a powder with the sorbing, analgesic and antimicrobial activity based on natural zeolite. Materials & methods. The study objects were model powder compositions containing a filler (natural zeolite), anesthetic (pyromecain), antifriction substances (talc, magnesium oxide, silicon dioxide) and antimicrobial substances (neomycin sulfate and polymyxin B sulfate). The quality of the samples was assessed by indicators of bulk and tapped densities, flowability, the Hausner ratio (H) and the Carr index (C). The osmotic activity was assessed by dialysis through a semipermeable membrane. For performing the tests the methods of the State Pharmacopoeia of Ukraine (SPhU) were used. Results & discussion. Powders with 5 % pyromecain showed the most optimal properties by the time of the start and duration of anesthesia; however, a further increase in its concentration did not give a significant effect. The technological properties of powders depend on both the type and concentration of antifriction substances. The addition of talc and magnesium oxide increased the density of powders by 2-18 %, and silicon dioxide reduced the density by 31-47 %.  The flowability (100 g/s) of samples with talc was 48.4-69.4, with magnesium oxide – 65.7-72.2, and with silicon dioxide – 19.8-40.6. The most significant improvement in flowability occurred after adding silicon dioxide; therefore, this substance in the amount of 5 % was chosen for further research. The adsorption properties of the powder were characterized as moderate. The osmotic activity was 73 %. Conclusions. The studies on selection of active substances and excipients for creating a powder with the sorbing, analgesic and antimicrobial action based on natural zeolite have been conducted. The following composition of the medicinal product has been proposed: natural zeolite (clinoptilolite) – up to 25.0 g, neomycin sulfate – 5000 IU/g, polymyxin B sulfate – 10.000 IU/g, pyromecain – 1.25 g (5 %) and silicon dioxide – 1.25 g (5 %).