Comparative study of specific activity of the piroctone olamine semisolid dosage form for external use

Abstract

The external treatment of seborrheic dermatitis of the scalp depends on the withdrawal of clinical symptoms and the complaints the patient made to the doctor. At present Ukrainian dermatology has several dozen pharmacotherapeutic products in this direction, with dominating medicines of ketoconazole, zinc pyrition, and their combinations. They are characterized by the short-term or weak effect, associated with the pathogenic microorganisms’ resistance against the background of long-term use of biologically active substances which are their active parts. One way to solve the problem is using the drugs with new highly active pharmaceutical ingredients. Employees of the Department of Technology of Medications of the Zaporizhzhia State Medical University proposed the composition of a new applicate semisolid dosage form of pirocton olamine based on complex physical-chemical, pharmacotechnological, biopharmaceutical, and rheological investigations – topical ointment on the hydrophilic base in combination with resin-free naphthalene for external use in the complex etiotropic treatment of seborrheic dermatitis of the scalp. The aim of this work is to study the specific activity of the combined ointment with pirocton olamine and resin-free naphthalene on a hydrophilic vehicle. Materials and methods. As the object of preclinical studies used experimental ointment containing 1 % piroctone olamine and 5 % resin-free naphthalene on the base of sodium carboxymethylcellulose glycerogel, providing optimum release of active pharmaceutical ingredients from the vehicle, and appropriate placebo semisolid dosage form. The study of the specific activity of the developed ointment under the conditional name “Oktonaf” was carried out by evaluating its antimicrobial, anti-inflammatory, and antioxidant effects given the foreseeable therapeutic focus and the literature on the spectrum of biological activity of active substances. The anti-inflammatory and antioxidant action of the proposed composition was evaluated by the allergic contact dermatitis model. As a reference drug cream “Psoricap” (KMP, Ukraine), which has long been applied in dermatological practice was used. Results of comparative microbiological studies proved that composite anti-seborrheic ointment with piroctone olamine and resin-free naphthalene by the antibacterial effect in relation to the size of the growth delay zones for Staphylococcus aureus and Escherichia coli (gram-positive and gram-negative microorganisms) slightly exceeds the effective dermatological medication reference cream “Psoricap”. At the same time, the antimycotic activity of experimental ointment in relation to Candida albicans practically does not differ from the same reference drug. A study of antioxidant and anti-inflammatory activity of the developed piroctone olamine ointment on a hydrophilic basis using the model of allergic contact dermatitis revealed that its level reliably was exceed the efficacy of topical reference medication “Psoricap”. Conclusions. Obtained data of a spectrum of specific activity of a combined ointment with piroctone olamine and resin-free naphthalene can predict the high clinical value of the proposed drug for practical domestic dermatology.