Pantoprazole Sodium
CAS number 138786-67-1
Product Name : PANTOPRAZOLE SODIUM SALT
C.A.S. No: 138786-67-1
Synonyms : Sodium-[5-(Difluoromethoxy)-2-[[(3,4-dimethoxy-2-pyri - dinyl)-methyl]-sulfinyl]-1H-benzimidazolide
Molecular Formula: C16H14F2N3NaO4S1.5 H2O
Formula Weight : 432.4
Product Group: Antiulcerative
Pantoprazole Sodium is a substituted benzimidazole proton-pump inhibitor (PPI) that suppresses gastric acid secretion by inhibiting the gastric (H+,K+)-ATPase enzyme pump. Pantoprazole Sodium forms a covalent bond to two sites of the (H+,K+)-ATPase enzyme system at the secretory surface of the gastric parietal cell; this binding results in antisecretory effects that persists for more than 24 hours. A significant increase in gastric pH and decrease in basal acid output follow oral and IV administration of Pantoprazole Sodium. Pantoprazole Sodium does not antagonize H2 or cholinergic receptors.
Most studies report that gastric acid suppression is dose-related following IV and oral administration of Pantoprazole Sodium, resulting in inhibition of both basal and stimulated gastric acid secretion (irrespective of the stimulus).
Significant in vitro activity against Helicobacter pylori (H. Pylori) has been demonstrated for Pantoprazole Sodium.
Similar to omeprazole and other PPIs, hypergastrinemia can occur during Pantoprazole Sodium therapy. Although prolonged hypergastrinemia has been associated with gastric tumors in rats, long-term studies of proton pump inhibitors do not suggest the development of tumors in humans.
No clinically relevant effects of Pantoprazole Sodium on cardiovascular, respiratory, ophthalmic, or central nervous system function have been detected. A short-term (2-week) evaluation showed that oral Pantoprazole Sodium had no effect on endocrine hormones including: cortisol, testosterone, triiodothyronine (T3), thyroxine (T4), thyroid-stimulating hormone, thyronine-binding protein, parathyroid hormone, insulin, glucagon, renin, aldosterone, follicle-stimulating hormone, luteinizing hormone, prolactin and growth hormone.
HAZARDS IDENTIFICATION
Not considered hazardous when handled under normal conditions with good house keeping
- Systematic (IUPAC) name
- 6-(difluoromethoxy)-2-[(3,4-dimethoxypyridin-2-yl)methylsulfinyl]-1H-benzo[d]imidazole
- Identifiers
- ATC code A02BC02
- PubChem 4679
- DrugBank APRD00073
- ChemSpider 4517
- Chemical data
- Formula C16H15F2N3O4S
- Mol. mass 383.371 g/mol
- SMILES eMolecules & PubChem
- Pharmacokinetic data
- Bioavailability 77%
- Metabolism Hepatic (CYP2C19 and 3A4)
- Half life 1 hour
- Excretion Renal
- Therapeutic considerations
- Pregnancy cat.
- B3(AU) B(US)
- Legal status
- Prescription only
- Routes Oral and intravenous
1. Omeprazole Sodium
CAS number 95510-70-6
CAS NO. 95510-70-6
Molecular Formula: C17H18N3NaO3S ,H2O
Molecular Weight: 367.397890 [g/mol]
Synonyms:
Losec Sodium, Andra, Nexium IV, Esomeprazole Sodium, OMEPRAZOLE SODIUM, Losec sodium (TN),
Nexium IV (TN), H 168/68 sodium, Omeprazole sodium [USAN], Omeprazole sodium (USAN), Esomeprazole
sodium (USAN), LS-33032, D01207, D04056, 1H-Benzimidazole, 5-methoxy-2-(((4-methoxy-3,5-dimethyl-2-
pyridinyl)methyl)sulfinyl)-, sodium salt, 95510-70-6, 5-Methoxy-2-(((4-methoxy-3,5-dimethyl-2-
pyridyl)methyl)sulfinyl)benzimidazole, sodium salt, 161796-78-7
DEFINITION
Sodium 5-methoxy-2-[(RS)-[(4-methoxy-3,5-dimethylpyridin-2-yl)methyl]sulphinyl]-1Hbenzimidazole
monohydrate.
Content
98.0 per cent to 101.0 per cent (anhydrous substance).
CHARACTERS
Appearance
White or almost white, hygroscopic powder.
Solubility
Freely soluble in water and in ethanol (96 per cent), soluble in propylene glycol, very slightly
soluble in methylene chloride.
IDENTIFICATION
Ultraviolet and visible absorption spectrophotometry (2.2.25).
Test solution Dissolve 2.0 mg in 0.1 M sodium hydroxide and dilute to 100.0 ml with the
same solvent.
Spectral rangeâ„¢ 230-350 nm.
Spectral range ™±230-350 nm.
Absorption maximam At 276 nm and 305 nm.
Absorption ratio A305 / A276 = 1.6 to 1.8.
â„¢ B. Examine the chromatograms obtained in the test for impurity C.
Resultsâ„¢The principal spot in the chromatogram obtained with test solution (b) is similar in
position and size to the principal spot in the chromatogram obtained with reference solution
(a). Place the plate in a tank saturated with vapour of acetic acid R. The spots rapidly turn
brown.
™±C. Ignite 1 g and cool. Add 1 ml of water R to the residue and neutralise with hydrochloric
acid R. Filter and dilute the filtrate to 4 ml with water R. 0.1 ml of the solution gives reaction
(b) of sodium (2.3.1).
Omeprazole sodium bicarbonateis a combination of omeprazole, a proton-pump inhibitor, and sodium bicarbonate, an antacid. Omeprazole is a substituted benzimidazole, 5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]sulfinyl]-1H-benzimidazole, a racemic mixture of two enantiomers that inhibits gastric acid secretion. Its empirical formula is C17H19N3O3S, with a molecular weight of 345.42.
Omeprazole is a white to off-white crystalline powder which melts with decomposition at about 155 oC. It is a weak base, freely soluble in ethanol and methanol, and slightly soluble in acetone and isopropanol and very slightly soluble in water. The stability of omeprazole is a function of pH; it is rapidly degraded in acid media, but has acceptable stability under alkaline conditions.
Omeprazole is supplied as immediate-release capsules and unit-dose packets as powder for oral suspension. Each capsule contains either 40 mg or 20 mg of omeprazole and 1100 mg of sodium bicarbonate with the following excipients: croscarmellose sodium and sodium stearyl fumarate. Packets of powder for oral suspension contain either 40 mg or 20 mg of omeprazole and 1680 mg of sodium bicarbonate with the following excipients: xylitol, sucrose, sucralose, xanthan gum, and flavorings.
TESTS
Solution S
Dissolve 0.50 g in carbon dioxide-free water R and dilute to 25 ml with the same solvent.
Appearance of solution
Solution S is clear (2.2.1) and not more intensely coloured than reference solution B6 (2.2.2,
Method II).
pH (2.2.3)
10.3 to 11.3 for solution S.
Related substances
Liquid chromatography (2.2.29).
Test solution Dissolve 3.0 mg of the substance to be examined in the mobile phase and
dilute to 25.0 ml with the mobile phase.
Reference solution (a) ™ ±Dissolve 1.0 mg of omeprazole CRS and 1.0 mg of omeprazole
impurity D CRS in the mobile phase and dilute to 10.0 ml with the mobile phase.
Reference solution (b) ±Dilute 1.0 ml of the test solution to 100.0 ml with the mobile phase.
Dilute 1.0 ml of this solution to 10.0 ml with the mobile phase.
Column:
size: l = 0.15 m, = 4 mm;
stationary phase: octylsilyl silica gel for chromatography R (5 ™ ¼m).
Mobile phase Mix 27 volumes of acetonitrile R and 73 volumes of a 1.4 g/l solution of
disodium hydrogen phosphate R, previously adjusted to pH 7.6 with phosphoric acid R.
Flow rate ±1 ml/min.
Detection Spectrophotometer at 280 nm.
Injection ±40 ¼l.
Run time ±3 times the retention time of omeprazole.
Relative retention ±With reference to omeprazole (retention time = about 9 min): impurity D =
about 0.8.
System suitability Reference solution (a):
™ ½ resolution: minimum 3 between the peaks due to impurity D and omeprazole; if
necessary adjust the pH of the mobile phase or the concentration of acetonitrile R; an
increase in the pH will improve the resolution.
Limit:
™ ½ any impurity: for each impurity, not more than the area of the principal peak in the
chromatogram obtained with reference solution (b) (0.1 per cent).
Heavy metals (2.4.8)
Maximum 20 ppm.
1.0 g complies with test C. Prepare the reference solution using 2 ml of lead standard solution
(10 ppm Pb) R.
2. Rabeprazole Sodium
CAS Number 117976-89-3
Systematic (IUPAC) name
2-([4-(3-methoxypropoxy)-3-methylpyridin-2-yl]methylsulfinyl)-1H-benzo[d]imidazole
Chemical Name: Sodium 2-[[4-(3-methoxypropoxy)-3-methyl-pyridin-
yl]methylsulfinyl]benzoimidazole
Molecular Formula: C18H20N3NaO3S
Molecular Weight: 381.43
Specifications: Rabeprazole Sodium is available as per In house specifications
Packing: Export worthy packing
Application: ANTI ULCERATIVES (Proton pump inhibitors)
Availability: For your requirements of evaluation, Pilots and Commercial procurement
Description: White or almost white colour powder, hygroscopic
Solubility: Freely soluble in Water, soluble in Chloroform, Methanol and Ethyl acetate
Melting point: Rabeprazole sodium melts at about 140 °C with decomposition
Identification: IR spectrum of the sample dispersed in KBr should exhibit maxima only at the
same wave lengths
a) IR as that of similar preparation of the working standard
b) Test for sodium 0.1mL of the neutralized filtrate of the ignited residue gives reaction (b) of
sodium
Water: Between 3.0% and 7.0% w/w
pH: Between 10.0 and 12.0
Chromatographic purity
a) Any known Impurity Not more than 0.15%
b)other unknown individual
impurity Not more than 0.10%
c) Total impurities Not more than 1.0%
Assay: Not less than 99.0% w/w and not more than 101.0% w/w on anhydrous basis
Stability and Reactivity:
Materials to avoid: Strong oxidizing agents.
Conditions to Avoid: Incompatible materials, light.
Hazardous Decomposition Products:
Carbon monoxide, carbon dioxide, nitrogen oxides,sulfur dioxide.
General Information: As in any fire, wear a self-contained breathing apparatus, MSHA/NIOSH (approved or equivalent) and protective clothing to prevent contact with skin and eyes.
Extinguishing Media: Use water spray, dry chemical, carbon dioxide, or appropriate foam.
Pharmacokinetic data
Bioavailability 52%
Metabolism Hepatic
Half life 1 - 1.5 hours
Excretion Renal
Inactive ingredients of the 20 mg tablet are carnauba wax, crospovidone, diacetylated monoglycerides, ethylcellulose, hydroxypropyl cellulose, hypromellose phthalate, magnesium stearate, mannitol, propylene glycol, sodium hydroxide, sodium stearyl fumarate, talc, and titanium dioxide. Iron oxide yellow is the coloring agent for the tablet coating. Iron oxide red is the ink pigment
Indication of Danger: Irritant
Risk Phrases:
R 22 Harmful if swallowed.
Safety Phrases:
S 26 In case of contact with eyes, rinse immediately with plenty
water and seek medical advice.
WGK (Water Danger/Protection)
