Substantiation of the composition of sublingual tablets for the treatment of CNS disorders
DOI:
https://doi.org/10.24959/nphj.24.145Keywords:
L-tryptophan; glycine; dry peony extract; sublingual tablets; wet granulation, taste correctionAbstract
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.
References
DP «Ukrainskyi naukovyi farmakopeinyi tsentr yakosti likarskykh zasobiv». (2015). Derzhavna farmakopeia Ukrainy: v 3 t. (2-he vyd.). Kharkiv: DP «Ukrainskyi naukovyi farmakopeinyi tsentr yakosti likarskykh zasobiv».
Makwana, S., Kharadi R. (2018). A review on sublingual formulation. World journal of pharmacy and pharmaceutical sciences, 7 (9), 1300-1306.
The British Pharmacopoeia 2011. (2010). (1th ed.). (Vol. 3). London: HMSO.
Metodicheskie ukazaniya po obrabotke rezultatov eksperimenta po tehnologii lekarstv / A. I. Tencova, T. A. Groshovyj, V. A. Golovkin, S. M. Mahkamov. – Tashkent: NII «Uzgiprozem», 1980. – 71.
Davydova, I., Ruban, O., Slipchenko, H., Kovalevska, I. (2023). Doslidzhennia fizyko-khimichnykh ta farmakotekhnolohichnykh pokaznykiv L–tryptofanu, hlitsynu ta sukhoho ekstraktu pivonii pry rozrobtsi tabletok sublinhvalnykh. Fitoterapiia. Chasopys, 1, 100-106.
Kurakula, M., Koteswara, Rao G. S. N. (2020). Pharmaceutical assessment of polyvinylpyrrolidone (PVP): As excipient from conventional to controlled delivery systems with a spotlight on COVID-19 inhibition. Journal of Drug Delivery Science and Technology, 60, 1-24. doi: https://10.1016/j.jddst.2020.102046.
Hordiienko, O. I., Vronska, L. V., Melnyk, O. A., Hroshovyi, T. A. (2015). Suchasnyi stan stvorennia, vyrobnytstva ta doslidzhennia tabletovanykh likarskykh zasobiv. Povidoml. 17. Mukoadheziini tabletky: kharakterystyka likarskoi formy, vymohy, pidkhody do rozrobky, doslidzhennia tabletok, pidbir dopomizhnykh rechovyn. Farmatsevtychnyi chasopys, 1, 126-133.
Ma’ali, A., Naseef, H., Qurt, M., Abukhalil, A. D., Rabba, A. K., Sabri, I. (2023). The Preparation and Evaluation of Cyanocobalamin Mucoadhesive Sublingual Tablets. Pharmaceuticals, 16, 1412. doi: https://10.3390/ph16101412.
Paris, A., Caridade, S., Colomb, E., Bellina, M., Boucard, E., Verrier, B., Monge, C. (2021). Sublingual protein delivery by a mucoadhesive patch made of natural polymers. Acta Biomaterialia, 128, 222-235.
Srisuntorn, P., Bhalang, K., Arirachakaran, P. (2018). HPMC Based Mucoadhesive for Delivery of Triamcinolone Acetonide: Mucoadhesion and Drug Release Properties, An In Vitro Study. J. Dent. Assoc Thai, 68 (2), 121-131. doi: https://10.14456/jdat.2018.17.
Ruiz-Caro, R., Gago-Guillan, M., Otero-Espinar, F., Dolores, Veiga M. (2012). Mucoadhesive Tablets for Controlled Release of Acyclovir. Chemical and Pharmaceutical Bulletin, 60 (10), 1249-1257. doi: 10.1248/cpb.c12-00324.
Chakraborti, C. K., Sahoo, S., Behera, P. K. (2014). Role of different biodegradable polymers on the permeability of ciprofloxacin. J. Adv. Pharm. Technol. Res, 5 (3), 140-146. doi: https://10.4103/2231-4040.137434.
Chowdary, Y. A., Raparla, R., Madhuri, M. (2014). Formulation and Evaluation of Multilayered Tablets of Pioglitazone Hydrochloride and Metformin Hydrochloride. J. Pharm. (Cairo), 12, 848243. doi: https://10.1155/2014/848243.
Chuieshov, V. I., Hladukh, Ye. V., Saiko, I. V., Liapunova, O. O., Sichkar, A. A., Krutskykh, T. V., Ruban, O. A. (2012). Tekhnolohiia likiv promyslovoho vyrobnytstva: pidruch. dlia studentiv VNZ (2-he vyd.). (Ch. 1). Kharkiv: NFaU: Oryhinal.
Downloads
Published
Issue
Section
License
Copyright (c) 2024 National University of Pharmacy
This work is licensed under a Creative Commons Attribution 4.0 International License.
Authors who publish with this journal agree to the following terms:- Authors retain copyright and grant the journal right of first publication with the work simultaneously licensed under a Creative Commons Attribution License that allows others to share the work with an acknowledgement of the work's authorship and initial publication in this journal.
- Authors are able to enter into separate, additional contractual arrangements for the non-exclusive distribution of the journal's published version of the work (e.g., post it to an institutional repository or publish it in a book), with an acknowledgement of its initial publication in this journal.
- Authors are permitted and encouraged to post their work online (e.g., in institutional repositories or on their website) prior to and during the submission process, as it can lead to productive exchanges, as well as earlier and greater citation of published work (See The Effect of Open Access).
