Solodovnyk V. Development of composition, technologies and research of soft medicinal form with piroctone olamine and naphthalanum deresinated for therapy and prophylaxis of seborrheic dermatitis of hairy part of head

Thesis is dedicated to development of scientifically grounded composition and technology of semisolid pharmacotherapeutic drug for external administration – ointment with piroctone olamine and designed pitch-removed naphthalan for topical prevention of seborrheic dermatitis of the scalp zone with high efficacy and stability, based on the investigations of its physico-chemical, biopharmaceutical, rheological, microbiological and pharmaco-technological properties. In view of the foregoing, development of the semisolid dosage form for therapy and prevention of seborrheic dermatitis of the scalp with composition from piroctone olamine and pitch-removed naphthalan is topical issue for pharmaceutical and medical sciences and can allow to widen the pharmacotherapeutic arsenal of the effective domestic medications for dermatologic practice. Successful realization of this project will allow to propose an effective, with good compliance, available for the most population of Ukraine, innovative dermatologic external medication for domestic healthcare and create the real alternative for imported pharmacotherapeutics. It was established that providing the available and effective drugs for therapy and prevention of seborrheic dermatitis of the scalp for Ukrainians is not enough. That fact proves the necessity and substantiation of intensifying the investigations in the field of creation new domestic medications on the base of piroctone olamine and pitch-removed naphthalan that can combine high efficacy and safety with compliance and available for the wide segments of the Ukrainian population price. It was revealed that nature of the base-device haв a significant impact on the releasing of piroctone olamine from the composed ointments for the pathogenic therapy of seborrheic dermatitis of the scalp. Variance analysis allowed to establish that sodium carboxymethylcellulose glycerol gel provided with the optimal values of this important biopharmaceutical parameter for topical dosage forms. It was established that developed topical dosage form with piroctone olamine by the consistent properties has related to systems with dominating of coagulative links («mechanical stability» 2,37). Structural and mechanical characteristics of the proposed medication for external use were located within the optimum of consistency and factors of dynamic flowing of the ointment (Кd1 = 29,3%; Kd2 = 75,4%) could testify to the positive ability to spreadability and equal distribution on the skin surface. According to results of thermogravimetric study the absence of interaction between the active pharmaceutical ingredients of the proposed composed ointment with excipients and its stability at temperatures used in technological process of emulsion systems were proven. Stability of the main physical and chemical characteristics and microbial purity of the ointment for external use with piroctone olamine and pitch-removed naphthalan during 12 months of the experimental storage in the polymeric packs in the cool (8-15ºС) dark place was established. Preclinical studies of the developed semisolid dosage form for the complex therapy of seborrheic dermatitis of the scalp had proved that it belonged to relatively non-hazardous substances (VI class of toxicity) and had not topical irritative and allergic action when used as intended. Wide specter of antimicrobial effect and expressed anti-inflammatory and antioxidant activity much more than the same parameters of the referent medication – ointment “Psorikap” (KMP, Ukraine) were experimentally proven for developed pharmacotherapeutic drug. Obtained data allowed to prognose a high clinical value of proposed medication for practical healthcare. Keywords: technology, piroctone olamine, pitch-removed naphthalan, semisolid dosage forms, topical therapy, antimycotic, antibacterial, anti-inflammatory, antioxidant activity.