Selection of the excipients to create tablets of adamantane-1-ammonium 2-((5-(adamantane-1-yl)-4-phenyl-4h-1,2,4-triazole-3-yl)thio)acetate by the method of wet granulation. Part 1

Abstract

Recently, mental health is one of the most serious problems faced by all countries due to at least every fourth person have such problems at any given period of life. In European region, prevalence of mental disorders is rather high. According to the WHO data, among 870 million of people living in European region, about 100 million feel themselves anxiously and depressed; more than 21 million suffer from disorders associated with alcohol; more than 7 million – with Alzheimer's disease and other dementia types; about 4 million suffer from schizophrenia; 4 million - bipolar affective disorders, and 4 million - panic disorders.

Numerous studies in area of the dosage form influence on therapeutic effect have shown, that the optimal activity of drug substance is achieved only under condition of a rational dosage form appointment. Besides, in this way many side effects of remedies can be avoided.

It is known that most of neuroleptics are used in tablet form. Accordingly, development of technology of adamantane-1-ammonium 2-((5-(adamantane-1-yl)-4-phenyl-4h-1,2,4-triazole-3-yl)thio)acetate tablets is important.

The aim of the present study is selection of the optimal excipients to create tablets of adamantane-1-ammonium 2-((5-(adamantane-1-yl)-4-phenyl-4h-1,2,4-triazole-3-yl)thio)acetate by the method of wet granulation with the content of active substance 70 mg.

Methods. Four groups of the excipients with different physical and technological properties were studied. Experimental work was carried out using modern equipment for determination of tablets’ weight uniformity, abrasion, time for disintegration and receiving.

16 excipients were studied; most of them recently appeared in the market, so there is no information about their use in pharmaceutical technology for creation of tablets.

During study of four qualitative factors one of the variance analysis plans was used – four factorial experiment based on the Hyper-Graeco-Latin square.

Results. Based on pharmaco-technological properties and morphometric experiments, wet granulation method was offered for adamantane-1-ammonium 2-((5-(adamantane-1-yl)-4-phenyl-4h-1,2,4-triazole-3-yl)thio)acetate tablets obtaining. Considering the literature data [3,6,10], relying on the research of the modern outstanding scientists: prof. Groshovui T. A., Kazarinov M. O., Borzunov Ye. E., Shteyngart M. V. and the experience of previous technological research, we offered theoretical composition of the tablets, namely set of factors that are often used in tablets production by wet granulation method