54182-58-0 Usage
Description
Sucralfate is a complex of the sulfuric acid ester of sucrose and aluminum hydroxide, which is practically insoluble in water and soluble in strong acids and bases. It has a pKa value between 0.43 and 1.19 and is minimally absorbed from the gastrointestinal tract, exerting its effects through local rather than systemic action. Sucralfate forms a protective barrier at the ulcer site, preventing exposure to acid and pepsin, and also adsorbs pepsin and bile salts. It stimulates the synthesis and release of prostaglandins, bicarbonate, and growth factors, contributing to significant ulcer healing effects.
Uses
1. Used in Pharmaceutical Industry:
a. Sucralfate is used as an antacid and antiulcer medication for the treatment of duodenal ulcers and other gastrointestinal disorders. It forms a protective barrier at the ulcer site, reducing the erosive action of pepsin and bile salts, and stimulates the synthesis and release of prostaglandins, bicarbonate, and growth factors, promoting ulcer healing.
b. Sucralfate is used as an inhibitor of peptic hydrolysis and stomach acidity, helping to reduce the severity of gastrointestinal ulcers and promote healing.
2. Used in Antineoplastic and Antileukemia Applications:
a. Sucralfate's bisand tris-platinum complexes show promise as antitumor agents, potentially offering new treatment options for cancer patients.
3. Used in Drug Delivery Systems:
a. Sucralfate's sulfate esters can form insoluble adherent complexes with the proteinaceous exudate at the abraded surface of a crater of the ulcerated area in the stomach, making it a potential candidate for targeted drug delivery systems in the treatment of gastrointestinal disorders.
Chemical Properties:
Sucralfate is a white powder with 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 various factors in rats.
Brand Name:
Carafate (Axcan Scandipharm) is a brand name for Sucralfate, which is used as an antacid and antiulcer medication.
Originator
Antepsin,Baldacci,Italy,1975
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.
Therapeutic Function
Antiulcer
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.
Check Digit Verification of cas no
The CAS Registry Mumber 54182-58-0 includes 8 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 5 digits, 5,4,1,8 and 2 respectively; the second part has 2 digits, 5 and 8 respectively.
Calculate Digit Verification of CAS Registry Number 54182-58:
(7*5)+(6*4)+(5*1)+(4*8)+(3*2)+(2*5)+(1*8)=120
120 % 10 = 0
So 54182-58-0 is a valid CAS Registry Number.
InChI:InChI=1/C12H22O35S8/c13-48(14,15)37-1-4-6(43-51(22,23)24)8(45-53(28,29)30)9(46-54(31,32)33)11(40-4)42-12(3-39-50(19,20)21)10(47-55(34,35)36)7(44-52(25,26)27)5(41-12)2-38-49(16,17)18/h4-11H,1-3H2,(H,13,14,15)(H,16,17,18)(H,19,20,21)(H,22,23,24)(H,25,26,27)(H,28,29,30)(H,31,32,33)(H,34,35,36)/p-8/t4-,5-,6-,7-,8+,9-,10+,11-,12+/m1/s1
