MEGLUMIN AND ITS SALTS: PROPERTIES AND PROSPECTS FOR APPLICATION IN PHARMACY
DOI:
https://doi.org/10.11603/2312-0967.2020.2.11194Keywords:
meglumine-containing drugs, biopharmaceutical factors, solubility, bioavailabilityAbstract
The aim of the work. To analyze the physicochemical and biopharmaceutical properties of meglumine (MGA), to generalize and systematize the data for its functional use in the development of drugs with prescribed pharmacological and technological parameters.
Materials and Methods. Methods of system approach, bibliographic, information search, analysis, comparison and generalization are used.
Results and Discussion. The analysis and generalization of literature and information data on physicochemical and biopharmaceutical properties is carried out MGA and its salts.Due to the characteristic features of the molecular structure, which is characterized by the presence of five hydroxyl groups and a secondary amino group, MGA exhibits salt-forming, solubilizing and stabilizing properties. The biopharmaceutical effects of MGA are due to the ability to form stable complexes of amino alcohol with cell membrane proteins, which reduces the effect of osmotic shock on the cell, reduce the toxicity of drugs. Literature data indicate the formation of real triple complexes of MGA with sulfamerazine and cyclodestrins, which leads to improved dissolution drugs and the release of active pharmaceutical ingredients (APhI) from liposomal compositions. The pharmacokinetic parameters of MGA salts with poorly soluble APIs, such as acridinoacetic, alpha-lipoic, enolic, gadotheric acids and their derivatives, prove the advantages of meglumine-containing compounds, which increase the solubility and bioavailability of APhIs. Of particular relevance is the use of IHA to model the required pharmacological and technological parameters of solid dosage forms having fixed combinations of API with different solubility parameters.
Conclusions. The generalization of the literature data indicates that IHA has unique physicochemical and biopharmaceutical properties, which open up prospects for the use of this compound for the development of drugs with specified pharmacological and technological characteristics.
References
Chernykh VP. (Ed.). Pharmaceutical encyclopedia. [Фармацевтична енциклопедія]. National University of Pharmacy. Kyiv: Morion; 2010. Ukrainian.
Abrantes CG, Duarte D, Reis CP. An overview of pharmaceutical excipients: Safe or not safe? Journal of Pharmaceutical Sciences, 2016;105(7): 2019-26. ISSN 0022-3549. doi:10.1016/j.xphs. 2016.03.019.
Alvarez-Lorenzo C, Concheiro A. (2006) Molecularly imprinted materials as advanced excipients for drug delivery systems. Biotechnology Annual Review.12: 225-68. DOI:10.1016/S1387-2656(06)12007-4. DOI: https://doi.org/10.1016/S1387-2656(06)12007-4
Pertsev IM, Dmytriievskyi DI, Rybachuk VD, Khomenko VM, Hudzenko OP, Kotenko OM, Maslii YuS. Excipients in drug technology: effects on technological, consumer, economic characteristics and therapeutic efficacy [Допоміжні речовини в технології ліків: вплив на технологічні, споживчі, економічні характеристики і терапевтичну ефективніcть] Kharkiv: Zoloti storinky, 2010. Ukrainian.
Kovalenko AL, Shyharova LV, Alekseeva LE. Fyzyko–khymycheskye y farmakolohycheskye svoistva N–metylhliukamyna y eho prymenenye v farmatsevtycheskoi tekhnolohyy. Farmatsiya. 2000;1: 45-7. Russian.
Bіlousov VM, Palchevskaia TA, Ziuzia LA, Yurev VYa, Bohdan VD, inventors; L. V. Pisarzhevsky Institute of Physical Chemistry of National Academy of Sciences of Ukraine. Catalyst for obtaining n – methylglucamine: 1286 (Patent). 1993 Ukrainian.
State Register of Medicines of Ukraine [Державний реєстр лікарських засобів України]. Available at: http://www.drlz.kiev.ua/ Ukrainian.
Paulekuhn GS, Dressman JB, Saal C. Trends in active pharmaceutical ingredient salt selection based on analysis of the Orange Book database. Journal of Medicinal Chemistry. 2007; 50(26): 6665-72 DOI: 10.1021/jm701032y PMID: 18052022.https://europepmc.org/article/med/18052022 DOI: https://doi.org/10.1021/jm701032y
Kovalenko AL. (2005). Pharmacological activity of the original drugs based on 1-deoxy-1 (N-methylamino) -D-glucitol. Doctor’s thesis. St-Petersburg. Institute of Toxicology, scientific and technological pharmaceutical company Polisan. Research Institute of Epidemiology and Microbiology named after N.F. Gamalei RAMS. Russian
Handbook of Pharmaceutical Excipients . Edited by Rowe RC, Sheskey PJ, Quinn ME. Sixth edition. Pharmaceutical Press and American Pharmacists Association, 2009.
Palchevska TA, Baula OP, Salii OO, Bessarabov VI, Tarasenko HV, Kuryshko HH. [Marketing research on the assortment of contrating drugs repreazedtovary on the pharmaceutical market of Ukraine]. Farm. chasop. 2020;1: 66-74. DOI:10.11603/2312-0967.2020.1.10980. Ukrainian. DOI: https://doi.org/10.11603/2312-0967.2020.1.10980
Non-tissue Specific Extracellular MRI Contrast Media. In: Thomsen H.S. (Ed). Contrast Media. Medical Radiology (Diagnostic Imaging). Springer, Berlin, Heidelberg. 2006. DOI:10.1007/3-540-27742-0_16. DOI: https://doi.org/10.1007/3-540-27742-0_16
Ysakov VA, Ysakov DV. [Cycloferon: mechanisms of action and new prospects for use in clinical practice] . Klin. med. 2015; 93(9): 46-51. Russian
Plotnikova MA, Klotchenko SA, Kiselev AA, Gorshkov AN, Shurygina A-PS, Vasilyev KA, Uciechowska-Kaczmarzyk U, Samsonov SA, Kovalenko AL & Vasin AV [Meglumine acridone acetate, the ionic salt of CMA and N-methylglucamine, induces apoptosis in human PBMCs via the mitochondrial pathway]. Sci Rep. 2019;9. 18240. DOI:10.1038/s41598-019-54208-9. Russian DOI: https://doi.org/10.1038/s41598-019-54208-9
Almakaieva LH, Naumenok LH, Biehunova NV. [Development of the formulation of drug for paranteral use based on thioctic acid] Farmatsevtychnyi zhurnal. 2011; 4: 67-72. Retrieved from: http://nbuv.gov.ua/UJRN/pharmazh_2011_4_14. pdf Ukrainian. DOI: https://doi.org/10.18108/jeer.2011.14.6.67
Zhebrovska FI, Borshchevska MI, Borshchevskyi HI, Kostiuk HV, inventors; PJSC Farmak. The method of obtaining an injectable form of the drug based on alpha-lipoic acid. UA 96239 С2 (pat.) 2011. Ukrainian.
Chernykh VP, Zahaiko AL, Kotvitska AA, Danylchenko SYu, Vedernikova IO Promising scientific developments of the National University of Pharmacy. Medicines: A handbook. [Перспективні наукові розробки Національного фармацевтичного університету. Лікарські засоби: довідник] Chernykh VP (Ed.). Kh.: NFaU; 2015. Ukrainian.
Almakaieva LH, Naumenok LH, Biehunova NV, Dolia VH, Almakaiev MS. [Development of the composition of the drug based on meloxicam] Visnyk farmatsii. 2013;3: 31-5. Available at: http://nbuv.gov.ua/UJRN/VPhC_2013_3_12. pdf. Ukrainian.
Dobrelia NV, Hula NS, Bohatyrova OV, Khromov OS.
[Liposomes: not only "lipo-"]. Farmakolohiia ta likarska toksykolohiia. 2017;3(54): 16-31. Ukrainian.
Aloisio C, Antimisiaris SG, Longhi MR. Liposomes containing cyclodextrins or meglumine to solubilize and improve the bioavailability of poorly soluble drugs. Journal of Molecular Liquids. 2017; 229:106-13. ISSN 0167-7322. DOI:10.1016/j.molliq.2016.12.035. DOI: https://doi.org/10.1016/j.molliq.2016.12.035
Aloisio C, De Oliveirа AG, Longhi M. Solubility and release modulation effect of sulfamerazine ternary complexes with cyclodextrins and meglumine. Journal of Pharmaceutical and Biomedical Analysis. 2014; 100: 64-73. DOI: 10.1016/j.jpba.2014.07.008 DOI: https://doi.org/10.1016/j.jpba.2014.07.008
Hazhir N, Kiani F, Tahermansouri H, Ghorbani A, Saraei H, Koohyar F. Prediction of thermodynamic and structural properties of sulfamerazine and sulfamethazine in water using DFT and ab initio methods. J Mex Chem Soc. 2018;62(1): 1-13. Sociedad Química de México ISSN-e 2594 – 0317 ISSN 1870 - 249X DOI:10.29356/jmcs.v62i1.575 DOI: https://doi.org/10.29356/jmcs.v62i1.575
Manabu N, Toshimitsu O, Sawada T, Kenzo T, inventors; Boringer Ingelheim International Gmbh. Pharmaceutical formulation comprising telmisartan, process for preparing thereof (variants), bilayer pharmaceutical tablet and process for preparing thereof UA 81781 С2 (pat.) 2008. Ukrainian.
Kalepu S, Nekkanti V. Insoluble drug delivery strategies: review of recent advances and business prospects. Acta Pharm Sin B. 2015;5(5): 442‐53. DOI:10.1016/j.apsb.2015.07.003. DOI: https://doi.org/10.1016/j.apsb.2015.07.003
Podzolkov VI, Tarzimanova AI. [Telmisartan in the treatment of arterial hypertension. Case study]. Ratsionalnaya farmakoterapiya v kardiologii. 2012;8(2): 201-4. Russian DOI: https://doi.org/10.20996/1819-6446-2012-8-2-201-204
LY Chkhol Voo, MIuN Chaikhiuk, KKhYM Chu Von, NAM Kkhiun Van. Inventors; Boriun Farmasiutykal Ko., LTD. Pharmaceutical combination drug. No. 217.015.F86F (Patent). Korea; 2017. Retrieved from: https://edrid.ru/rid/217.015.f86f.html
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