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Sucralfate
"Descrizione"
by Al222 (19776 pt)
2024-May-05 10:26

Take only under medical supervision

Sucralfate is an anti-ulcer medication that works by forming a protective barrier over the stomach lining. Upon contact with gastric acid, it transforms into an adherent gel that coats the ulcer and shields the damaged area from acids and digestive enzymes. This allows the mucosa to heal more effectively (1). Sucralfate is used to treat gastric and duodenal ulcers (2), erosive gastritis (3), and can also be used to treat throat irritations caused by gastroesophageal reflux disease (4). It is well tolerated by most patients and is generally not absorbed into the bloodstream, minimizing the risk of systemic side effects.

Chemical Industrial Synthesis Process

  • Synthesis of polyaluminum hydroxide. Aluminum hydroxide is reacted with hydrochloric acid to form aluminum chloride, which is then polymerized to produce polyaluminum hydroxide.
  • Reaction of sucrose and sulfate. Sucrose is reacted with sulfuric acid to produce a sucrose sulfate derivative.
  • Condensation. The sucrose sulfate derivative is condensed with polyaluminum hydroxide in the presence of an acid catalyst to form Sucralfate.
  • Purification. Crude Sucralfate is purified through techniques such as crystallization or precipitation to remove impurities and enhance the purity of the product.
  • Drying. The purified product is dried to remove residual moisture and achieve the final solid form.
  • Quality control. Samples of the final product undergo various quality control tests to ensure they meet purity, stability, and therapeutic activity standards.

Commercial Applications

Recently, it has also been adopted in dermatology and cosmetics for its protective and healing properties on the skin. Here are some of the main uses and benefits of sucralfate in cosmetics.

Healing Properties. Sucralfate helps protect and repair damaged skin by forming a protective barrier that facilitates the healing of wounds, abrasions, and skin irritations.

Protective Effects. This compound forms a film on the skin that protects against external irritants and pollutants, helping to prevent further damage.

Reduction of Inflammation. It has properties that help reduce skin inflammation, making it useful for treating conditions such as dermatitis, eczema, and other skin irritations.

Promotion of Skin Regeneration. It stimulates the skin regeneration process, speeding up healing and improving the appearance of scars.

Use in Post-Procedure Products. It is often included in formulations intended for post-procedure skin care, such as those used after laser treatments or chemical peels, to support skin repair and protection.

Versatile Applications. Sucralfate can be employed in a variety of skincare products, including creams, gels, and lotions, particularly those formulated for sensitive or compromised skin.


Molecular Formula    C12H54Al9O55S8

Molecular Weight  1577.9 g/mol

Synonyms:

  • Carafate
  • Sucralfate
  • Sulfate, Aluminum Sucrose
  • Ulcerban
  • Aluminum Sucrose Sulfate
  • Antepsin
  • Basic Aluminum Sucrose Sulfate
  • Ulcogant
  • Ulsanic

Bibliografia_____________________________________________________________________

(1) Candelli M, Carloni E, Armuzzi A, Cammarota G, Ojetti V, Pignataro G, Santoliquido A, Pola R, Pola E, Gasbarrini G, Gasbarrini A. Role of sucralfate in gastrointestinal diseases. Panminerva Med. 2000 Mar;42(1):55-9. 

Abstract. Sucralfate is a cytoprotective drug widely used in clinical practice to prevent or treat several gastrointestinal diseases such as gastro-esophageal reflux, gastritis, peptic ulcer, stress ulcer and dyspepsia. Sucralfate is a safe and well tolerated drug, as demonstrated by the quite complete lack of side effects and it is, for this reason, one of the most important therapeutic choices in the management of acid related diseases during pregnancy. Moreover, sucralfate has recently been shown to be useful in non-acid related gastrointestinal disease as well. In fact, sucralfate has also been administered topically in patients with radiation-induced mucosal procto-sigmoiditis or ulcerative colitis with surprising results. The drug is actually able to form a physical barrier between epithelium and damaging agents (-bile salts, drugs, refluxate...). Moreover, sucralfate increases the local levels of fibroblast growth factors and induces a rise in the mucosal concentration of prostaglandins which are considered important factors in mucosal healing. The aim of this paper is to describe the current and probably forthcoming uses of sucralfate in the field of gastrointestinal disorders. Moreover, we investigate the role of sucralfate as a reliable means to prevent the occurrence of reflux-like symptoms after Helicobacter pylori eradication and in the management of Helicobacter pylori negative patients affected by non-ulcer dyspepsia.

(2) Lam SK. Treatment of duodenal ulcer with sucralfate. Scand J Gastroenterol Suppl. 1991;185:22-8. doi: 10.3109/00365529109093216. PMID: 1683491.

Abstract. Sucralfate attains a healing rate of about 79% for duodenal ulcer in 4 weeks, which is similar to the effects of cimetidine and ranitidine. Whereas cigarette smoking significantly affects duodenal ulcer healing by acid-reducing agents, the healing rates of smokers and non-smokers treated with sucralfate or colloidal bismuth are indistinguishable, suggesting an inherent advantage through the cytoprotective mechanisms of these agents. The 12-month relapse curves for duodenal ulcers initially healed with sucralfate and colloidal bismuth subcitrate closely overlap each other and are significantly lower than the curves for the histamine H2-receptor antagonists. These findings cannot be accounted for by clearance of Helicobacter pylori, on which sucralfate has little effect. Preliminary evidence suggests that the use of acid-reducing agents results in up-regulation of the parietal cells and may help to explain the differences in relapse rates. Sucralfate is superior to placebo and comparable to H2 antagonists in the prevention of duodenal ulcer recurrence.

(3) Rees WD. Mechanisms of gastroduodenal protection by sucralfate. Am J Med. 1991 Aug 8;91(2A):58S-63S. doi: 10.1016/0002-9343(91)90452-4. PMID: 1715673.

Abstract. Over the past 5-10 years, a number of studies have shown that topical sucralfate enhances a number of gastric and duodenal mechanisms, e.g., the "mucus-bicarbonate barrier," mucosal hydrophobicity, mucosal blood flow, cell viability, and local production of prostaglandins, as well as endogenous mediators of tissue injury and repair. It seems likely that the complex actions of sucralfate are in part related to direct interaction between the drug or its components (aluminum, sucrose, and sulfate) and gastric mucosal tissues, and in part related to effects of the drug on the various mucosal mediators of tissue injury and repair. Local actions may play a role in accelerating healing of ulcer-damaged mucosa, but this does not explain the protective actions of sucralfate on normal mucosa. Thus sucralfate appears to enhance the protective function of the "mucus-bicarbonate" barrier by actions on both components. This may depend in part on an interaction with the unstirred layer overlying gastric epithelium. Sucralfate has also been shown to increase the hydrophobicity of mucus gel. There is little doubt that sucralfate increases local production and release of protective prostaglandins (PGs), but the precise role played by these agents in mediating mucosal protection and in chronic ulcer healing remains uncertain. Currently, the mechanism of action of sucralfate on vascular integrity remains unknown and the role of PGs in this protective function is unclear. There is little evidence that epidermal growth factor plays any role in mediating mucosal protection by sucralfate, but it may be important in its ulcer-healing action. Sucralfate has been shown to be truly "cytoprotective" in that it protects isolated epithelial cells from damage by noxious agents. In animals treated with sucralfate, the surface epithelial cells were disrupted, but necrotic lesions in the deep proliferative zone were virtually absent. It seems likely that investigations of the actions of sucralfate and its components will move ever closer to defining the target cells, the intracellular events, and the mediators that bring about its protective and ulcer-healing activity.

(4) Dağlı Ü, Kalkan İH. Treatment of reflux disease during pregnancy and lactation. Turk J Gastroenterol. 2017 Dec;28(Suppl 1):S53-S56. doi: 10.5152/tjg.2017.14. PMID: 29199169.

Abstract. Gastroesophageal reflux disease (GERD) is frequently seen during pregnancy. In the medical treatment of pregnant women with GERD, alginic acid and sucralfate can be used. Calcium- and magnesium-based antacids can also be used, particularly for patients with preeclampsia. In particular, ranitidine -a histamine-2 receptor blocker- is preferred. In the case of non-responsiveness to the abovementioned treatments, proton pump inhibitors (PPIs), except omeprazole, can be given considering the benefit-harm ratio for the mother and fetus after the first trimester. In cases with GERD during the lactation period, drugs having minimum systemic absorption, such as sucralfate and alginic acid, are preferable but there is no data.

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