Препарат Антарейт – комбинация магалдрата (антацида нового поколения) с симетиконом (противопенным компонентом для уменьшения метеоризма). Антацидный эффект магалдрата развивается быстро (1–2 мин) и сохраняется на протяжении длительного времени (до 3 ч). Магалдрат – антацид мультитаргетного воздействия, проявляющий адсорбирующее, обволакивающее, а также выраженное цитопротективное действие на слизистую оболочку желудка. При растворении магалдрата в соляной кислоте кристаллическая структура этого вещества обусловливает формирование плотноупакованных частиц гексаакваалюминия. Данные частицы обволакивают область изъязвления, причем размер их (2 мкм) таков, что облегчает миграцию эпителиоцитов и фибробластов в процессе репарации стенки желудка. В результате модулируется метаболизм простагландинов, повышаются уровни вазодилататора оксида азота, улучшается микроциркуляция тканей, также проявляются антигистаминные эффекты – важные составляющие мультитаргетного действия магалдрата.
Ключевые слова: антациды, G-белки, магалдрат, Антарейт, фармакокинетика, фармакодинамика, интеллектуальный анализ данных.
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Antareit is a combination of magaldrate (new generation antacid) with simeticone (anti-foaming agent used to reduce bloating). Magaldrate anti-acid effect develops quickly (in 1–2 minutes) and preserves for a long time (up to 3 hours). Magaldrate is a multitarget antacid that has adsorbing, enveloping and significant cytoprotective effect on gastric mucosa. When magaldrate dissolves in hydrochloric acid its crystal structure provides forming of tightly-packed hexaaquaaluminium particles. These particles envelop the ulceration area and their size (2 µm) enables epithelial cells and fibroblasts migration in gastric wall reparation process. As a result prostaglandin metabolism is modulated, nitrogen oxide vasodilatator level increases, tissue microcirculation improves and antihistamine effects manifest. These processes are important components of multitarget magaldrate effect.
Key words: antacids, G-proteins, magaldrate, Antareit, pharmacokinetics, pharmacodynamics, data mining.
1. Patel AV, Santani DD, Goyal RK. Antiulcer activity and the mechanism of action of magaldrate in gastric ulceration models of rat. Indian J Physiol Pharmacol 2000; 44 (3): 350–4.
2. Cousar GD, Gadacz TR. Comparison of antacids on the binding of bile salts. Arch Surg. 1984; 119 (9): 1018–20.
3. Arnold R, Garbe I, Koop H et al. Effect of antacid and H2-receptor blocker treatment on gastric endocrine cells. Scand J Gastroenterol (Suppl.) 1984; 101: 31–7.
4. Громова О.А., Торшин И.Ю., Максимов В.А. Магалдрат как антацид с мультитаргетным воздействием: клинико-фармакологическое эссе. Лечащий врач. 2018; 2: 7. / Gromova O.A., Torshin I.Yu., Maksimov V.A. Magaldrat kak antacid s multitargetnym vozdejstviem: kliniko-farmakologicheskoe esse. Lechashij vrach. 2018; 2: 7. [in Russian]
5. Peterson CL, Perry DL, Masood H et al. Characterization of antacid compounds containing both aluminum and magnesium. I. Crystalline powders. Pharm Res 1993; 10 (7): 998–1004.
6. Winterberg B, Bertram H, Rolf N et al. Differences in plasma and tissue aluminum concentrations due to different aluminum-containing drugs in patients with renal insufficiency and with normal renal function. J Trace Elem Electrolytes Health Dis 1987; 1 (2): 69–72.
7. Wilson GE Jr, Falzone CJ, Johnson R, Lee HK. Action of hydrochloric acid on aluminum hydroxide-magnesium hydroxide gels and magaldrate: 27Al NMR and pH-stat studies. J Pharm Sci 1985; 74 (10): 1075–7.
8. Торшин И.Ю., Громова О.А. Экспертный анализ данных в молекулярной фармакологии. 2012. / Torshin I.Yu., Gromova O.A. Ekspertnyj analiz dannyh v molekulyarnoj farmakologii. 2012. [in Russian]
9. Wessel K, Resch K, Kaever V. Aluminium fluoride enhances phospholipase A2 activity and eicosanoid synthesis in macrophages. Eicosanoids 1989; 2 (4): 223–7.
10. Ong J, Kerr DI. Interactions of N-ethylmaleimide and aluminium fluoride with GABAB receptor function in rat neocortical slices. Eur J Pharmacol 1995; 287 (2): 197–200.
11. Liu P, Wen M, Hayashi J. Guanine nucleotide-binding protein stimulates arachidonic acid metabolism in TEA3A1 thymic epithelial cells by stimulating release and inhibiting incorporation of arachidonic acid. Biochem Mol Biol Int 1993; 31 (4): 613–25.
12. Rawlinson SC, Wheeler-Jones CP, Lanyon LE. Arachidonic acid for loading induced prostacyclin and prostaglandin E (2) release from osteoblasts and osteocytes is derived from the activities of different forms of phospholipase A (2). Bone 2000; 27 (2): 241–7.
13. Schmidt C, Baumeister B, Kipnowski J et al. Magaldrate stimulates endogenous prostaglandin E2 synthesis in human gastric mucosa in vitro and in vivo. Hepatogastroenterol 1998; 45 (24): 2443–6.
14. Berstad K, Vergin H, Postius S et al. Gastric prostaglandin E2 release induced by aluminium hydroxide and aluminium hydroxide-containing antacids in rats. Effect of low doses and citric acid. Scand J Gastroenterol 1987; 22 (7): 884–8.
15. Borella LE, DiJoseph JF, Mir GN. Cytoprotective and antiulcer activities of the antacid magaldrate in the rat. Arzneimittel-Forschung 1989; 39 (7): 786–9.
16. Konturek SJ, Brzozowski T, Majka J et al. Nitric oxide in gastroprotection by aluminium-containing antacids. Eur J Pharmacol 1992; 229 (2–3): 155–62.
17. Evora PR, Pearson PJ, Schaff HV. Impaired endothelium-dependent relaxation after coronary reperfusion injury: evidence for G-protein dysfunction. Ann Thorac Surg 1994; 57 (6): 1550–6.
18. Parkinson LG, Giles NL, Adcroft KF et al. The potential of nanoporous anodic aluminium oxide membranes to influence skin wound repair. Tissue Eng Part A 2009; 15 (12): 3753–63.
19. Guterman LR, Falzone J, Wilson GE Jr. Action of hydrochloric acid on aluminum hydroxide-magnesium hydroxide gels and magaldrate: quasi-elastic light scattering studies. J Pharm Sci 1986; 75 (5): 502–5.
20. Громова О.А., Торшин И.Ю. Магний и «болезни цивилизации». М.: ГЭОТАР-Медиа, 2018. / Gromova O.A., Torshin I.Yu. Magnij i "bolezni civilizacii". M.: GEOTAR-Media, 2018. [in Russian]
21. Swart AC, Klaassen BH, Bloys-van Treslong-de, Hemker HC. The adsorption of blood coagulation factors II, VII, IX and X from human plasma to aluminium hydroxide. Thromb Diath Haemorrh 1972; 27 (3): 490–501.
22. Громова О.А., Торшин И.Ю., Рудаков К.В. и др. Систематический анализ магнийзависимых митохондриальных белков. Кардиология. 2014; 54 (9): 86–92. / Gromova O.A., Torshin I.Yu., Rudakov K.V. i dr. Sistematicheskij analiz magnijzavisimyh mitohondrialnyh belkov. Kardiologiya. 2014; 54 (9): 86–92. [in Russian]
23. Юдина Н.В., Торшин И.Ю., Громова О.А. и др. Обеспеченность ионами калия и магния – фундаментальное условие для поддержания нормального артериального давления. Кардиология. 2016; 56 (10): 80–9. / Yudina N.V., Torshin I.Yu., Gromova O.A. i dr. Obespechennost ionami kaliya i magniya – fundamentalnoe uslovie dlya podderzhaniya normalnogo arterialnogo davleniya. Kardiologiya. 2016; 56 (10): 80–9. [in Russian]
24. Громова О.А., Торшин И.Ю., Юдина Н.В. и др. Дефицит магния и нарушения регуляции тонуса сосудов. Кардиология. 2014; 54 (7): 66–72. / Gromova O.A., Torshin I.Yu., Yudina N.V. i dr. Deficit magniya i narusheniya regulyacii tonusa sosudov. Kardiologiya. 2014; 54 (7): 66–72. [in Russian]
25. Adewoye EO, Salami AT. Anti-ulcerogenic mechanism of magnesium in indomethacin induced gastric ulcer in rats. Niger J Physiol Sci 2013; 28 (2): 193–9.
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1. Patel AV, Santani DD, Goyal RK. Antiulcer activity and the mechanism of action of magaldrate in gastric ulceration models of rat. Indian J Physiol Pharmacol 2000; 44 (3): 350–4.
2. Cousar GD, Gadacz TR. Comparison of antacids on the binding of bile salts. Arch Surg. 1984; 119 (9): 1018–20.
3. Arnold R, Garbe I, Koop H et al. Effect of antacid and H2-receptor blocker treatment on gastric endocrine cells. Scand J Gastroenterol (Suppl.) 1984; 101: 31–7.
4. Gromova O.A., Torshin I.Yu., Maksimov V.A. Magaldrat kak antacid s multitargetnym vozdejstviem: kliniko-farmakologicheskoe esse. Lechashij vrach. 2018; 2: 7. [in Russian]
5. Peterson CL, Perry DL, Masood H et al. Characterization of antacid compounds containing both aluminum and magnesium. I. Crystalline powders. Pharm Res 1993; 10 (7): 998–1004.
6. Winterberg B, Bertram H, Rolf N et al. Differences in plasma and tissue aluminum concentrations due to different aluminum-containing drugs in patients with renal insufficiency and with normal renal function. J Trace Elem Electrolytes Health Dis 1987; 1 (2): 69–72.
7. Wilson GE Jr, Falzone CJ, Johnson R, Lee HK. Action of hydrochloric acid on aluminum hydroxide-magnesium hydroxide gels and magaldrate: 27Al NMR and pH-stat studies. J Pharm Sci 1985; 74 (10): 1075–7.
8. Torshin I.Yu., Gromova O.A. Ekspertnyj analiz dannyh v molekulyarnoj farmakologii. 2012. [in Russian]
9. Wessel K, Resch K, Kaever V. Aluminium fluoride enhances phospholipase A2 activity and eicosanoid synthesis in macrophages. Eicosanoids 1989; 2 (4): 223–7.
10. Ong J, Kerr DI. Interactions of N-ethylmaleimide and aluminium fluoride with GABAB receptor function in rat neocortical slices. Eur J Pharmacol 1995; 287 (2): 197–200.
11. Liu P, Wen M, Hayashi J. Guanine nucleotide-binding protein stimulates arachidonic acid metabolism in TEA3A1 thymic epithelial cells by stimulating release and inhibiting incorporation of arachidonic acid. Biochem Mol Biol Int 1993; 31 (4): 613–25.
12. Rawlinson SC, Wheeler-Jones CP, Lanyon LE. Arachidonic acid for loading induced prostacyclin and prostaglandin E (2) release from osteoblasts and osteocytes is derived from the activities of different forms of phospholipase A (2). Bone 2000; 27 (2): 241–7.
13. Schmidt C, Baumeister B, Kipnowski J et al. Magaldrate stimulates endogenous prostaglandin E2 synthesis in human gastric mucosa in vitro and in vivo. Hepatogastroenterol 1998; 45 (24): 2443–6.
14. Berstad K, Vergin H, Postius S et al. Gastric prostaglandin E2 release induced by aluminium hydroxide and aluminium hydroxide-containing antacids in rats. Effect of low doses and citric acid. Scand J Gastroenterol 1987; 22 (7): 884–8.
15. Borella LE, DiJoseph JF, Mir GN. Cytoprotective and antiulcer activities of the antacid magaldrate in the rat. Arzneimittel-Forschung 1989; 39 (7): 786–9.
16. Konturek SJ, Brzozowski T, Majka J et al. Nitric oxide in gastroprotection by aluminium-containing antacids. Eur J Pharmacol 1992; 229 (2–3): 155–62.
17. Evora PR, Pearson PJ, Schaff HV. Impaired endothelium-dependent relaxation after coronary reperfusion injury: evidence for G-protein dysfunction. Ann Thorac Surg 1994; 57 (6): 1550–6.
18. Parkinson LG, Giles NL, Adcroft KF et al. The potential of nanoporous anodic aluminium oxide membranes to influence skin wound repair. Tissue Eng Part A 2009; 15 (12): 3753–63.
19. Guterman LR, Falzone J, Wilson GE Jr. Action of hydrochloric acid on aluminum hydroxide-magnesium hydroxide gels and magaldrate: quasi-elastic light scattering studies. J Pharm Sci 1986; 75 (5): 502–5.
20. Gromova O.A., Torshin I.Yu. Magnij i "bolezni civilizacii". M.: GEOTAR-Media, 2018. [in Russian]
21. Swart AC, Klaassen BH, Bloys-van Treslong-de, Hemker HC. The adsorption of blood coagulation factors II, VII, IX and X from human plasma to aluminium hydroxide. Thromb Diath Haemorrh 1972; 27 (3): 490–501.
22. Gromova O.A., Torshin I.Yu., Rudakov K.V. i dr. Sistematicheskij analiz magnijzavisimyh mitohondrialnyh belkov. Kardiologiya. 2014; 54 (9): 86–92. [in Russian]
23. Yudina N.V., Torshin I.Yu., Gromova O.A. i dr. Obespechennost ionami kaliya i magniya – fundamentalnoe uslovie dlya podderzhaniya normalnogo arterialnogo davleniya. Kardiologiya. 2016; 56 (10): 80–9. [in Russian]
24. Gromova O.A., Torshin I.Yu., Yudina N.V. i dr. Deficit magniya i narusheniya regulyacii tonusa sosudov. Kardiologiya. 2014; 54 (7): 66–72. [in Russian]
25. Adewoye EO, Salami AT. Anti-ulcerogenic mechanism of magnesium in indomethacin induced gastric ulcer in rats. Niger J Physiol Sci 2013; 28 (2): 193–9.
Авторы
О.А.Громова *1, И.Ю.Торшин1, В.А.Максимов2
1 ФГБУ «Федеральный исследовательский центр "Информатика и управление"» РАН. 119333, Россия, Москва, ул. Вавилова, д. 40;
2 ФГБОУ ДПО «Российская медицинская академия непрерывного профессионального образования» Минздрава России. 125993, Россия, Москва, ул. Баррикадная, д. 2/1
1 Federal Research Centre "Information and Management" of the Russian Academy of Sciences. 119333, Russian Federation, Moscow, ul. Vavilova, d. 40;
2 Russian Medical Academy of Continuous Professional Education of the Ministry of Health of the Russian Federation. 125993, Russian Federation, Moscow, ul. Barrikadnaia, d. 2/1
*unesco.gromova@gmail.com