Justification of the gel formers selection in the development of oromucosal drug in the form of troches

Abstract

Introduction. Troches deserve special attention among the existing oromucosal dosage forms. They have good consumer characteristics and an adequate level of bioavailability, which makes it expedient to expand the range of medicines to be used in the form of troches, especially for pediatric use. The purpose of this work is to justify the optimal composition of troches by selecting the most rational gel-forming agent and its concentration. Materials & methods. Gel formers gelatine (250 g/cm², according to Bloom), agar (800 g/cm², according to Bloom) and apple pectin were used as objects of the study. The ratio of the ingredients was investigated in 6 samples. Samples with gelatine and agar were prepared as follows: the calculated amount of gelatine or agar was poured with the calculated amount of purified water and left for swelling. When gelatine/agar swelled, it was melted in a water bath and mixed with concentrate of citric acid, glucose syrup, glycerol, fruit flavouring and food colouring. Samples with apple pectin were prepared as follows: the calculated amount of apple pectin was mixed with half the sugar and heated to (50.0 ± 2.0) °C with water purified with vigorous stirring. After swelling, it was mixed with concentrate of citric acid, glucose syrup, glycerol, fruit flavouring and food colouring. The resulting mass was poured into silicone form and placed in a refrigerator for hardening. Results & discussion. The obtained troches were evaluated by such quality indicators as organoleptic control, uniformity of dosage units, dissolution time. It was found that sample No. 5 shows the best consumer characteristics, while the other samples do not meet the requirements of the studied quality indicators. For example, sample No. 1 was not formed, the texture remained semi-solid; samples No. 2 and No. 3 were formed, but were opaque and easily destroyed when pressed; samples No. 4 and No. 6 contained too much gelatine, some of which remained undissolved, resulting in deterioration of taste characteristics (less pleasant taste, "crunch", sticking during chewing). The critical parameters of the technological process of troches preparation are time of gelatine swelling, temperature of gelatine melting, time of troches hardening. Conclusion. The findings showed that samples of gelatine-based troches with its content of 8.65 mass. % have the best consumer characteristics. The resulting troches are homogenous, with a pleasant fruity aroma and sweet taste. They meet the requirements of SPhU by the quality indicators organoleptic indicators, the uniformity of the dosage units and the dissolution time. The established critical parameters of the technological process and their values were established.