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Sucralfate

Product Name
Sucralfate
CAS No.
54182-58-0
Chemical Name
Sucralfate
Synonyms
SUCRALPHATE;carafate;Keal;Ulcar;Urbal;Sugast;Venter;Citogel;Succosa;Sucrate
CBNumber
CB6239042
Molecular Formula
C11H52Al16O75S8-16
Formula Weight
2072.71
MOL File
54182-58-0.mol
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Sucralfate Property

Melting point:
>220°C (dec.)
Boiling point:
1990℃ at 101.325kPa
Density 
0.338 at 20℃
vapor pressure 
0Pa at 25℃
storage temp. 
Inert atmosphere,2-8°C
solubility 
Practically insoluble in water, in ethanol (96 per cent) and in methylene chloride. It dissolves in dilute solutions of mineral acids and alkali hydroxides.
pka
pKa = 0.43 to 1.19(at 25℃)
form 
Solid
color 
White
LogP
1.46 at 25℃ and pH7
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Safety

WGK Germany 
2
RTECS 
BD0900000
HS Code 
29400090
Hazardous Substances Data
54182-58-0(Hazardous Substances Data)
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
S0652
Product name
Sucrose octasulfate–aluminum complex
Packaging
1g
Price
$89.4
Updated
2024/03/01
Sigma-Aldrich
Product number
S0652
Product name
Sucrose octasulfate–aluminum complex
Packaging
5g
Price
$310
Updated
2024/03/01
Cayman Chemical
Product number
27882
Product name
Sucralfate
Packaging
500mg
Price
$32
Updated
2024/03/01
Cayman Chemical
Product number
27882
Product name
Sucralfate
Packaging
1g
Price
$61
Updated
2024/03/01
Sigma-Aldrich
Product number
Y0001324
Product name
Sucralfate
Purity
European Pharmacopoeia (EP) Reference Standard
Packaging
y0001324
Price
$220
Updated
2024/03/01
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Sucralfate Chemical Properties,Usage,Production

Description

Sucralfate is a complex of the sulfuric acid ester of sucrose and aluminum hydroxide. Secondary polymerization with aluminum hydroxide forms intermolecular bridges between molecules of sulfate esters with aluminum. Limited dissociation of the complex occurs in gastric acid, but these anionic sulfate esters form insoluble adherent complexes with the proteinaceous exudate at the abraded surface of a crater of the ulcerated area in the stomach. This physical complex protects the ulcer from the erosive action of pepsin and bile salts. Sucralfate also stimulates synthesis and release of prostaglandins, bicarbonate, and epidermal and fibroblast growth factors. Significant ulcer healing effects are noted in placebo-controlled trials. Only small amounts of sucralfate are absorbed systemically. In renal impairment, there is a risk of accumulation of absorbed aluminum from the drug. Sucralfate reduces absorption of other drugs, including H2 antihistamines, quinolone antibiotics, phenytoin, and perhaps, warfarin

Description

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.

Chemical Properties

White Powder

Originator

Antepsin,Baldacci,Italy,1975

Uses

antineoplastic, antileukemia

Uses

An inhibitor of peptic hydrolysis and stomach acidity. Used as an antiulcerative

Uses

Sucralfate, an aluminum salt of sucrose octasulfate, is used as an antacid and antiulcer medication. Bis- and tris-platinum complexes of sucrose show promise as antitumor agents. Sucrose monoesters are used in some pharmaceutical preparations.

Indications

Sucralfate (Carafate) is an aluminum hydroxide–sulfated sucrose complex that is only minimally absorbed from the GI tract. After exposure to gastric acid, the compound becomes negatively charged, creating a viscous adherent complex. This complex is believed to inhibit back-diffusion of H .Other effects are a direct reduction in pepsin activity and a slight rise in tissue prostaglandin levels. Stimulation of a cytoprotection mechanism may therefore assist mucosal healing. The drug has no acid-buffering capacity.

Manufacturing Process

A disaccharide is added to a pyridine SO3 complex solution, which is prepared by reacting 5 to 6 times the molar amount of liquid SO3 as much as that of disaccharide with 5 to 10 times the amount of pyridine as that of the disaccharide at 0°C to 5°C, for sulfation at 50°C to 70°C for 3 to 7 hours. After the completion of sulfation, the greater part of pyridine is removed by decantation. The obtained solution exhibits an acidity that is so strong that it is improper to apply the reaction with aluminum ion and, therefore, sodium hydroxide is added for neutralization. After the remaining pyridine is removed by concentration, 100 unit volumes of water per unit volume of the residue is added thereto. To the solution is then added aluminum ion solution mainly containing aluminum dihydroxychloride, the pH of which is 1.0 to 1.2, in such an amount that the aluminum ion is present in an amount of 4 to 6 molar parts of the amount of disaccharide to provide a pH of 4 to 4.5. The mixture is reacted under stirring at room temperature and the formed disaccharide polysulfate-aluminum compound is allowed to precipitate. After filtration, the residue is washed with water and dried.

brand name

Carafate (Axcan Scandipharm).

Therapeutic Function

Antiulcer

General Description

Sucralfate, 3,4,5,6-tetra-(polyhydroxyaluminum)-α-D-glucopyranosyl sulfate-2,3,4,5-tetra-(polyhydroxyaluminum)-β-D-fructofuranoside sulfate (Carafate), isthe aluminum hydroxide complex of the octasulfate ester ofsucrose. It is practically insoluble in water and soluble instrong acids and bases. It has a pKa value between 0.43 and1.19.
Sucralfate is minimally absorbed from the GI tract by design,and thus exerts its antiulcer effect through local ratherthan systemic action. It has negligible acid-neutralizing orbuffering capacity in therapeutic doses. Although its mechanismof action has not been established, studies suggestthat sucralfate binds preferentially to the ulcer site to form aprotective barrier that prevents exposure of the lesion to acidand pepsin. In addition, it adsorbs pepsin and bile salts.Either would be very desirable modes of action.
The simultaneous administration of sucralfate may reducethe bioavailability of certain agents (e.g., tetracycline, phenytoin,digoxin, or cimetidine). It further recommends restorationof bioavailability by separating administration of theseagents from that of sucralfate by 2 hours. Presumably, sucralfatebinds these agents in the GI tract. The most frequentlyreported adverse reaction to sucralfate is constipation (2.2%).Antacids may be prescribed as needed but should not be takenwithin 0.5 hour before or after sucralfate.

Clinical Use

Sucralfate is frequently used for prophylaxis of stress-induced gastritis in patients in intensive care units. It has also been successfully used in small numbers of patients as a suspension enema to treat radiation proctitis.

Veterinary Drugs and Treatments

Sucralfate has been used in the treatment of oral, esophageal, gastric, and duodenal ulcers. It has also been employed to prevent drug-induced (e.g., aspirin) gastric erosions, but efficacy for this is somewhat sporadic. Sucralfate has been used in human patients with hyperphosphatemia secondary to renal failure and potentially could be useful for this in animals as well.

Drug interactions

Potentially hazardous interactions with other drugs
Reduced absorption of digoxin, tetracyclines, quinolones, coumarins, fosphenytoin and phenytoin - give 2 hours after sucralfate.

Metabolism

Sucralfate is only slightly absorbed from the gastrointestinal tract after oral doses. However, there can be some release of aluminium ions and of sucrose sulphate; small quantities of sucrose sulphate may then be absorbed and excreted, mainly in the urine; some absorption of aluminium may also occur.

Sucralfate Preparation Products And Raw materials

Raw materials

Preparation Products

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Sucralfate Suppliers

Shenzhen Regent Biochemical Technology Co., Ltd.
Tel
0755-0755-85201366 18938635012
Fax
0755-85201366
Email
sales@regentsciences.com
Country
China
ProdList
9355
Advantage
58
Macheng jinxin biotechnology co., LTD
Tel
18271582018
Email
1126319697@qq.com
Country
China
ProdList
1525
Advantage
58
Hubei Weideli Chemical Reagent Co.,Ltd.
Tel
027-59222918 13385289472
Email
Z13385289472@163.com
Country
China
ProdList
4574
Advantage
58
J & K SCIENTIFIC LTD.
Tel
010-82848833 400-666-7788
Fax
86-10-82849933
Email
jkinfo@jkchemical.com
Country
China
ProdList
96815
Advantage
76
Chembest Research Laboratories Limited
Tel
+86-21-20908456
Fax
021-58180499
Email
sales@BioChemBest.com
Country
China
ProdList
6005
Advantage
61
Beijing HwrkChemical Technology Co., Ltd
Tel
010-89508211 18501085097
Fax
010-89508210
Email
sales.bj@hwrkchemical.com
Country
China
ProdList
8418
Advantage
55
LGM Pharma
Tel
1-(800)-881-8210
Fax
615-250-9817
Email
inquiries@lgmpharma.com
Country
United States
ProdList
2123
Advantage
70
Chemsky(shanghai)International Co.,Ltd.
Tel
021-50135380
Email
shchemsky@sina.com
Country
China
ProdList
32321
Advantage
50
XiaoGan ShenYuan ChemPharm co,ltd
Tel
15527768850
Email
1791901229@qq.com
Country
China
ProdList
8843
Advantage
52
Hunan Hui Bai Shi Biotechnology Co., Ltd.
Tel
0731-85526065 13308475853
Email
ivy@hnhbsj.com
Country
China
ProdList
4552
Advantage
62
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View Lastest Price from Sucralfate manufacturers

WUHAN FORTUNA CHEMICAL CO., LTD
Product
Sucralfate 54182-58-0
Price
US $0.00/Kg/Drum
Min. Order
1KG
Purity
30%-38%
Supply Ability
10 TONS
Release date
2021-07-23
Apeloa production Co.,Limited
Product
Sucralfate 54182-58-0
Price
US $1.00/g
Min. Order
1g
Purity
98%
Supply Ability
1000
Release date
2024-05-22
Hebei Weibang Biotechnology Co., Ltd
Product
Sucralfate 54182-58-0
Price
US $10.00/kg
Min. Order
1kg
Purity
99.5%
Supply Ability
100
Release date
2024-10-31

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