Sucralfate, 硫糖铝

Cytoprotective agent. Pepsin inhibitor. Binds to albumin and fibrinogen forming stable insoluble complexes. Creates a physical barrier over gastrointestinal ulcers. Promotes duodenal ulcer healing in vivo. Orally active.

Sucralfate is a basic aluminum sucrose sulfate complex that has gastroprotective activity. It inhibits rat pepsin in a concentration-dependent manner and pepsin activity in isolated human gastric juice. It also inhibits ulcer formation induced by pyloric ligation, indomethacin, or cysteamine in rats. Sucralfate (5,600 mg/animal) is protective against neutral ethanol and acidified taurocholic acid-induced damage in a rat model of hydrochloric acid-induced gastric mucosal damage, increasing the pH and reducing the disappearance of hydrogen ions. Formulations containing sucralfate have been used as antacids in the treatment of duodenal ulcer.

Sucralfate is a locally acting substance that in an acidic environment (pH < 4) reacts with hydrochloric acid in the stomach to form a cross-linking, viscous, paste-like material capable of acting as an acid buffer for as long as 6 to 8 hours after a single dose. It also attaches to proteins on the surface of ulcers, such as albumin and fibrinogen, to form stable insoluble complexes. These complexes serve as protective barriers at the ulcer surface, preventing further damage from acid, pepsin, and bile. In addition, sucralfate prevents back diffusion of hydrogen ions, and adsorbs both pepsin and bile acids. It has been thought that sucralfate also stimulates the production of prostaglandin E2, epidermal growth factors (EGF), bFGF, and gastric mucus.

Sucralfate is a drug that is used to treat and prevent injury-related inflammation by forming a protective barrier on the lining of the stomach and duodenum. Sucralfate has been shown to be effective in the treatment of infectious diseases, such as viral or bacterial infections, and also for radiation enteritis and ulcerative colitis. Sucralfate may interfere with the absorption of other drugs, such as acyclic nucleoside phosphonates, which are used to treat HIV/AIDS. This drug has also been shown to have anti-inflammatory properties through inhibition of prostaglandin synthesis. Sucralfate has been shown to have anti-inflammatory properties through inhibition of prostaglandin synthesis.

Title: Sucralfate

CAS Registry Number: 54182-58-0

CAS Name: Hexadeca-m-hydroxytetracosahydroxy[m8-[1,3,4,6-tetra-O-sulfo-b-D-fructofuranosyl-a-D-glucopyranoside tetrakis(hydrogen sulfato)(8-)]]hexadecaaluminum

Additional Names: b-D-fructofuranosyl-a-D-glucopyranoside octakis(hydrogen sulfate) aluminum complex; sucrose octakis(hydrogen sulfate) aluminum complex

Trademarks: Antepsin (Wyeth); Carafate (Aventis); Citogel (Zyma); Hexagastron (Durascan); Keal (Sinbio); Succosa (Astra HÝsle); Sucralfin (Inverni); Sucrate (Lisapharma); Sugast (Alfa); Sulcrate (Aventis); Ulcar (Houd?; Ulcerlmin (Chugai); Ulcogant (Merck KGaA)

Molecular Formula: C12H54Al16O75S8

Molecular Weight: 2086.74

Percent Composition: C 6.91%, H 2.61%, Al 20.69%, O 57.50%, S 12.29%

Literature References: A basic aluminum sucrose sulfate complex which inhibits peptic hydrolysis and stomach acidity. Prepn: M. Nametaka et al., Yakugaku Zasshi 87, 889 (1967), C.A. 68, 20831d (1968); FR 1500571; N. Yoshihiro et al., US 3432489 (1967, 1969 both to Chugai). Structure and properties: R. Nagashima, N. Yoshida, Arzneim.-Forsch. 29, 1668 (1979). In vitro and in vivo study of antipeptic and antiulcer activity: L. E. Borella, et al., ibid. 793. Series of articles on mode of action: ibid. 30, 73-88 (1980). Pharmacokinetics, metabolism and selective binding studies: K. Steiner et al., ibid. 32, 512 (1982). Clinical studies: J. F. Mayberry et al., Br. J. Clin. Pract. 32, 291 (1978). Symposium on clinical studies: J. Clin. Gastroenterol. 3, Suppl. 2, 103-184 (1981); Scand. J. Gastroenterol. 18, Suppl. 83, 1-82 (1983). Review of pharmacology and clinical studies: R. N. Brogden et al., Drugs 27, 194 (1984). Series of articles on clinical efficacy in peptic ulcer disease and gastritis: Am. J. Med. 79, Suppl. 2C, 1-64 (1985).

Properties: White amorphous powder. Sol in dil HCL and NaOH solns. Practically insol in water, ethanol, CHCl3. pKa = 0.43 to 1.19. Dissolution of aluminum occurs at pH <3; of sucrose sulfate at pH >4.

pKa: pKa = 0.43 to 1.19

Therap-Cat: Antiulcerative.

Keywords: Antiulcerative; Cytoprotectant (Gastric).