Substantiation of the composition of sublingual tablets for the treatment of CNS disorders

Aim. To develop the composition of sublingual tablets with L-tryptophan, glycine and a dry peony extract. Materials and methods. L-tryptophan, glycine and a dry peony extract were used as active pharmaceutical ingredients; Lactose GranuLac 200, MCC 102, HPMC methocel K4M CR Premium, HPMC methocel E4M CR Premium, aspartame, maltodextrin, sorbitol, sucralose, Mint cloroph FLV PDR, Strawberry FLV PDR, Apple FLV PDR, Plasdone K-25, crospovidone XL-10, nonessylin and calcium stearate were used as excipients. The pharmacotechnological studies were conducted in accordance with the methods of the State Pharmacopoeia of Ukraine. Results and discussion. The studies of the pharmacotechnological properties of APIs showed unsatisfactory results (poor fluidity, poor cohesive properties; high hygroscopicity of the peony extract), so it was decided to improve the technological properties of the active substances by wet granulation. Plasdone K-25 (15% aqueous solution) was chosen as a binder. The next step was to select a flour adhesive to improve the bioavailability of the active ingredients. According to the literature, HPMC was included in the composition of the test samples: HPMC methocel E4M CR Premium and HPMC methocel K4M CR Premium. According to the research results, HPMC methocel K4M CR Premium was included in the composition. The tablets developed had a bitter taste due to the presence of tryptophan and the peony extract. To correct the taste and odor, aspartame and Mint cloroph FLV PDR were used. Their optimal content in the formulation was experimentally determined. Conclusions. As a result of the studies conducted, the following substances have been selected: the binder for granulating the tablet mixture – Plasdone K-25; the flour adhesive to improve bioavailability – HPMC methocel K4M CR Premium; flavors for taste and odor to mask the bitter taste of sublingual tablets – aspartame and Mint cloroph FLV PDR.