Abstract
Salicylic acid derivatives are well known as effective anti-inflammatory drugs used for the treatment of rheumatic disorders, neuralgia, myalgia, and other diseases. Salicylamide (SA) is a compound structurally close to other salicylates, but this drug is better tolerated by the organism and less frequently leads to side effects [1]. Unfortunately, SA is characterized by a rather poor solubility, which limits the bioaccessibility of this compound and hinders wide use of SA as a drug. The problem of increasing the bioaccessibility of poorly soluble parent substances in ready-to-use medicinal forms is now successfully solved by using the so-called solid dispersion systems involving various biologically inert carriers. The role of such carriers can be played either by water-soluble polymeric matrices based on poly(vinyl pyrrolidone) (PVP), poly(ethylene glycol) (PEG), methylcellulose (MC), etc., or by relatively simple substances such as urea and lactose [2]. Previously [3, 4], we have demonstrated that such mixtures containing the components in a eutectic ratio are characterized by a significant increase in the solubility of a sparingly soluble drug component as compared to that of the parent substance. This paper reports on the results of our investigation of the relationship between the phase diagram and the characteristics of solubility (solubility diagram, solubility rate) in the salicylamide – trisamine (SA – TA) system. In selecting trisamine as a binary system component, we took into consideration the high solubility of this compound in water, the high thermal stability of trisamine in the temperature interval of interest, and the optical transparency of the aqueous trisamine solutions in the UV range used for the spectrophotometric determination of SA. In addition, trisamine has a generally low physiological activity – in particular, it exhibits practically no toxicity – which makes this compound a biocompatible component of the solid dispersion composition.
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