PRODUCTS

PANTOPRAZOLE SODIUM SESQUIHYDRATE

Pantoprazole Sodium Sesquihydrate is used in the short term treatment of erosive esophagitis associated with gastroesophageal reflux disease.
Pantoprazole Sodium Sesquihydrate is a proton pump inhibitor used to treat erosive esophagitis, gastric acid hypersecretion, and to promote healing of tissue damage caused by gastric acid.
Pantoprazole Sodium Sesquihydrate is also used to treat Zollinger-Ellison syndrome and other conditions involving excess stomach acid.

CAS Number: 164579-32-2
EC Number (EINECS): 605-368-1
IUPAC Name: sodium bis(5-(difluoromethoxy)-2-[(3,4-dimethoxypyridin-2-yl)methanesulfinyl]-1H-1,3-benzodiazol-1-ide) trihydrate
Empirical Formula: C₁₆H₁₄F₂N₃NaO₄S · 1.5 H₂O
Molecular Weight: ~432.37 g/mol

SYNONYMS:
Pantoprazole sodium sesquihydrate, pantoprazole sodium hydrate, pantoprazole sodium salt hydrate, Pantoprazole sodium sesquihydrate, 164579-32-2, 6-(Difluoromethoxy)-2-[[(3,4-dimethoxy-2-pyridinyl)methyl]sulfinyl]-1H-benzimidazole sodium salt hydrate;6-(Difluoromethoxy)-2-[[(3,4-dimethoxy-2-pyridinyl)methyl]sulfinyl]-1H-benzimidazole sodium salt hydrate, 1H-Benzimidazole, 6-(difluoromethoxy)-2-[[(3,4-dimethoxy-2-pyridinyl)methyl]sulfinyl]-, sodium salt, hydrate (2:2:3), SCHEMBL29389155, Pantoprazole sodium sesquihydrate, pantoprazole sodium hydrate, pantoprazole sodium salt hydrate, Pantoprazole, Protonix, Somac, Tecta, Pantoloc, Controloc, Panprax, Pantecta, Protium, Prazolin, Ppi-40, Neoppi, Sodium 5-(difluoromethoxy)-2-[(RS)-[(3,4-dimethoxypyridin-2-yl)methyl]sulfinyl]benzimidazol-1-ide Sesquihydrate, 1H -Benzimidazole, 5-(difluoromethoxy)-2-[[(3,4-dimethoxy-2-pyridyl)methyl]sulfinyl]-, sodium salt, hydrate (2:3), 5-(Difluoromethoxy)-2-[[(3,4-dimethoxy-2-pyridyl)methyl]sulfinyl]benzimidazole, sodium salt, sesquihydrate (USP)

Pantoprazole Sodium Sesquihydrate is a proton pump inhibitor that suppresses the final step in gastric acid production by covalently binding to the H+/K+ATPase enzyme system at the surface of the gastric parietal cell.
This effect leads to inhibition of both basal and stimulated gastric acid secretion, irrespective of the stimulus that persists longer than 24 hours.

Pantoprazole sodium sesquihydrate is an intermediate used in the production of proton pump inhibitors.
Pantoprazole Sodium Sesquihydrate is crucial in the treatment of gastrointestinal reflux diseases and peptic ulcers.
Pantoprazole Sodium Sesquihydrate is a proton pump inhibitor that decreases the amount of acid produced in the stomach.

The active ingredient in Pantoprazole Sodium Sesquihydrate delayed-release tablets is a substituted benzimidazole, sodium 5-(difluoromethoxy)-2-[[(3,4-dimethoxy-2-pyridinyl)methyl] sulfinyl]-1H-benzimidazole sesquihydrate, a compound that inhibits gastric acid secretion.
Pantoprazole Sodium Sesquihydrate's empirical formula is C16H14F2N3NaO4S x 1.5 H2O, with a molecular weight of 432.4.

USES and APPLICATIONS of PANTOPRAZOLE SODIUM SESQUIHYDRATE:
Pantoprazole Sodium Sesquihydrate is a proton pump inhibitor that inhibits gastric acid secretion and used for short-term treatment of erosive esophagitis associated with gastroesophageal reflux disease.
Pantoprazole Sodium Sesquihydrate suppresses the final step in gastric acid production by covalently binding to the (H+, K+)-ATPase enzyme system at the secretory surface of the gastric parietal cell.

This effect leads to inhibition of both basal and stimulated gastric acid secretion, irrespective of the stimulus.
The binding to the (H+, K+)-ATPase results in a duration of antisecretory effect that persists longer than 24 hours.
Pantoprazole Sodium Sesquihydrate is used for short-term treatment of erosion and ulceration of the esophagus for adults and pediatric patients 5 years of age and older caused by gastroesophageal reflux disease.

It can be used as a maintenance therapy for long-term use after initial response is obtained, but there have not been any controlled studies about the use of Pantoprazole Sodium Sesquihydrate past a duration of 12 months.
Pantoprazole Sodium Sesquihydrate may also be used in combination with antibiotics to treat ulcers caused by Helicobacter pylori.

Use of Pantoprazole Sodium Sesquihydrate may increase the chance of developing infections such as pneumonia, particularly in hospitalized patients.
A proton pump inhibitor drug, Pantoprazole Sodium Sesquihydrate inhibits gastric acid secretion.

Applications of Pantoprazole Sodium Sesquihydrate: Fine Chemicals
Pantoprazole Sodium Sesquihydrate is used to treat erosive esophagitis (damage to the esophagus from stomach acid caused by gastroesophageal reflux disease, or GERD) in adults and children who are at least 5 years old.

Pantoprazole Sodium Sesquihydrate is usually given for up to 8 weeks at a time while your esophagus heals.
Pantoprazole Sodium Sesquihydrate is also used to treat Zollinger-Ellison syndrome and other conditions involving excess stomach acid.

Pantoprazole Sodium Sesquihydrate is a first-generation proton pump inhibitor (PPI) used for the management of gastroesophageal reflux disease (GERD), for gastric protection to prevent recurrence of stomach ulcers or gastric damage from chronic use of NSAIDs, and for the treatment of pathological hypersecretory conditions including Zollinger-Ellison (ZE) Syndrome.

Pantoprazole Sodium Sesquihydrate can also be found in quadruple regimens for the treatment of H. pylori infections along with other antibiotics including amoxicillin, clarithromycin, and metronidazole, for example.
Pantoprazole Sodium Sesquihydrate is an H+/K+ ATPase inhibitor that exhibits antacid, anti-parasitic, and anticancer chemotherapeutic activities.

Pantoprazole Sodium Sesquihydrate is clinically used to treat gastroesophageal reflux disease (GERD), although its inhibition of ROCK-2 causes a decrease in gastroesophageal sphincter muscle tone.
In Trichomonas, Pantoprazole Sodium Sesquihydrate inhibits uridine nucleoside ribohydrolase activity.

Additionally, Pantoprazole Sodium Sesquihydrate increases tumor-associated macrophage recruitment in the tumor microenvironment, inhibiting tumor growth in vivo.
Pantoprazole Sodium Sesquihydrate is a type of medication used to treat stomach and esophageal problems.

Pantoprazole Sodium Sesquihydrate works by reducing the amount of acid produced by the stomach and reducing symptoms such as heartburn, difficulty swallowing, and persistent coughing.
Pantoprazole Sodium Sesquihydrate sodium can help heal acid damage to the stomach and esophagus, prevent ulcer growth, and prevent esophageal cancer.

-Therapeutic Role:
Pantoprazole Sodium Sesquihydrate is a proton pump inhibitor (PPI) used to reduce gastric acid secretion, treating conditions such as GERD, erosive esophagitis, stomach or duodenal ulcers, and Zollinger–Ellison syndrome.
Pantoprazole Sodium Sesquihydrate’s also part of Helicobacter pylori eradication regimens.

BENEFITS of PANTOPRAZOLE SODIUM SESQUIHYDRATE:
Pantoprazole Sodium Sesquihydrate is useful for reducing the amount of acid produced by the stomach.
This type of Pantoprazole Sodium Sesquihydrate is also used to treat heartburn, acid reflux, and esophageal irritation caused by increased stomach acid.

HIGHLIGHTS of PANTOPRAZOLE SODIUM SESQUIHYDRATE:
Pantoprazole Sodium Sesquihydrate oral tablet is available as both a generic and a brand-name drug.
Pantoprazole Sodium Sesquihydrate comes in three forms: a delayed-release oral tablet, a delayed-release oral liquid suspension, and an intravenous (IV) form that’s injected into a vein by a healthcare professional.

Pantoprazole Sodium Sesquihydrate oral tablet is used to reduce the amount of stomach acid your body makes.
Pantoprazole Sodium Sesquihydrate helps treat painful symptoms caused by conditions such as gastroesophageal reflux disease (GERD).

WHAT IS PANTOPRAZOLE SODIUM SESQUIHYDRATE USED FOR?
Pantoprazole Sodium Sesquihydrate is used to treat heartburn and certain other conditions caused by too much acid in the stomach.

*Gastroesophageal reflux disease (GERD), where stomach acid backs up into your esophagus.
*To treat erosive esophagitis (EE).
*Other conditions where your stomach makes too much acid.
*Pantoprazole may also be used for other conditions as determined by your healthcare provider.

CHEMICAL STRUCTURE of PANTOPRAZOLE SODIUM SESQUIHYDRATE:
Pantoprazole Sodium Sesquihydrate is a white to off-white crystalline powder and is racemic.
Pantoprazole Sodium Sesquihydrate has weakly basic and acidic properties.

Pantoprazole Sodium Sesquihydrate is freely soluble in water, very slightly soluble in phosphate buffer at pH 7.4, and practically insoluble in n‑hexane.
The stability of Pantoprazole Sodium Sesquihydrate in aqueous solution is pH-dependent.

The rate of degradation of Pantoprazole Sodium Sesquihydrate increases with decreasing pH.
At ambient temperature, the degradation half-life of Pantoprazole Sodium Sesquihydrate is approximately 2.8 hours at pH 5.0 and approximately 220 hours at pH 7.8.

MECHANISM OF ACTION OF PANTOPRAZOLE SODIUM SESQUIHYDRATE:
Irreversibly inhibits the (H⁺/K⁺)-ATPase enzyme in gastric parietal cells, leading to sustained acid suppression (>24 hours).

DEVELOPMENT BACKGROUND of PANTOPRAZOLE SODIUM SESQUIHYDRATE:
Synthesized in 1986 as the sesquihydrate form; Pantoprazole Sodium Sesquihydrate's stability and compatibility facilitated intravenous formulation development; first marketed in Germany in 1994.

BENEFITS of PANTOPRAZOLE SODIUM SESQUIHYDRATE:
Pantoprazole Sodium Sesquihydrate is indicated where suppression of acid secretion has therapeutic benefit; i.e
*Peptic ulcer diseases
*Gastroesophageal reflux diseases
*Ulcer induced by non-steroidal anti-inflammatory drugs (NSAIDs)
*Eradication of Helicobacter pylori (in combination with antibiotics)
*Zollinger-Ellison Syndrome

CLINICAL PHARMACOLOGY of PANTOPRAZOLE SODIUM SESQUIHYDRATE:
PHARMACOKINETICS
Pantoprazole Sodium Sesquihydrate is prepared as an enteric-coated tablet so that absorption of pantoprazole begins only after the tablet leaves the stomach.

Pantoprazole Sodium Sesquihydrate does not accumulate and its pharmacokinetics are unaltered with multiple daily dosing.
Following oral or intravenous administration, the serum concentration of Pantoprazole Sodium Sesquihydrate declines biexponentially with a terminal elimination half-life of approximately one hour.

When Pantoprazole Sodium Sesquihydrate is given with food, its tmax is highly variable and may increase significantly.
Following intravenous administration of Pantoprazole Sodium Sesquihydrate to extensive metabolizers, its total clearance is 7.6-14.0 L/h and its apparent volume of distribution is 11.0-23.6 L.

ABSORPTION of PANTOPRAZOLE SODIUM SESQUIHYDRATE:
The absorption of Pantoprazole Sodium Sesquihydrate is rapid, with a Cmax of 2.5 μg/mL that occurs approximately 2.5 hours after administration of a single or multiple oral 40-mg doses of pantoprazole sodium delayed-release tablets.

Pantoprazole Sodium Sesquihydrate is well absorbed; it undergoes little first-pass metabolism resulting in an absolute bioavailability of approximately 77%.
Pantoprazole Sodium Sesquihydrate absorption is not affected by concomitant administration of antacids.

Administration of Pantoprazole Sodium Sesquihydrate with food may delay its absorption up to 2 hours or longer; however, the Cmax and the extent of pantoprazole absorption (AUC) are not altered.
Thus, Pantoprazole Sodium Sesquihydrate may be taken without regard to timing of meals.

DISTRIBUTION of PANTOPRAZOLE SODIUM SESQUIHYDRATE:
The apparent volume of distribution of Pantoprazole Sodium Sesquihydrate is approximately 11.0-23.6 L, distributing mainly in extracellular fluid.
The serum protein binding of Pantoprazole Sodium Sesquihydrate is about 98%, primarily to albumin.

METABOLISM of PANTOPRAZOLE SODIUM SESQUIHYDRATE:
Pantoprazole Sodium Sesquihydrate is extensively metabolized in the liver through the cytochrome P450 (CYP) system.
Pantoprazole Sodium Sesquihydrate metabolism is independent of the route of administration (intravenous or oral).
The main metabolic pathway is demethylation, by CYP2C19, with subsequent sulfation; other metabolic pathways include oxidation by CYP3A4.

There is no evidence that any of the Pantoprazole Sodium Sesquihydrate metabolites have significant pharmacologic activity.
Although these sub-populations of slow Pantoprazole Sodium Sesquihydrate metabolizers have elimination half-life values of 3.5 to 10.0 hours, they still have minimal accumulation (≤ 23%) with once daily dosing.

PHYSICAL and CHEMICAL PROPERTIES of PANTOPRAZOLE SODIUM SESQUIHYDRATE:
Physical State & Appearance: Solid (white to light yellow powder or crystals)
Solubility: Readily soluble in water and ethyl alcohol (ethanol)
Stability: Structurally unstable;
sensitive when selecting excipients for formulations—HPLC is the preferred analytical method
Physicochemical Characterization: Pantoprazole exhibits multiple hydrate forms—Form B is the most physically stable;
Form A is the least stable
CAS / EC Number: 164579-32-2 / 605-368-1
Formula / M.W.: C16H14F2N3NaO4S · 1.5 H2O / ~432.37 g/mol
Appearance: Solid (white to light yellow powder or crystals)
Solubility: Readily soluble in water and ethanol

Stability: Sensitive; most stable hydrate form is B
Therapeutic Use: Proton pump inhibitor for acid-related GI conditions
Mechanism: Inhibition of gastric H⁺/K⁺-ATPase enzyme
Molecular Weight: 424.4 g/mol
Hydrogen Bond Donor Count: 2
Hydrogen Bond Acceptor Count: 10
Rotatable Bond Count: 7
Exact Mass: 424.07546743 Da
Monoisotopic Mass: 424.07546743 Da
Topological Polar Surface Area: 107 Å²

Heavy Atom Count: 28
Formal Charge: 0
Complexity: 490
Isotope Atom Count: 0
Defined Atom Stereocenter Count: 0
Undefined Atom Stereocenter Count: 1
Defined Bond Stereocenter Count: 0
Undefined Bond Stereocenter Count: 0
Covalently-Bonded Unit Count: 3
Compound Is Canonicalized: Yes

Physical state: solid
Color: No data available
Odor: No data available
Melting point/freezing point: No data available
Initial boiling point and boiling range: No data available
Flammability (solid, gas): No data available
Upper/lower flammability or explosive limits: No data available
Flash point: No data available

Autoignition temperature: No data available
Decomposition temperature: No data available
pH: No data available
Viscosity, kinematic: No data available
Viscosity, dynamic: No data available
Water solubility: No data available
Partition coefficient: n-octanol/water
Partition coefficient: No data available
Vapor pressure: No data available

Density: No data available
Relative density: No data available
Relative vapor density: No data available
Particle characteristics: No data available
Explosive properties: No data available
Oxidizing properties: No data available
Other safety information: No data available

Formula: C16H14F2N3NaO4S • 3/2 H2O
Formula Wt.: 432.37
Chemical Name: 5-(Difluoromethoxy)-2-[[(3,4-dimethoxy-2-pyridinyl)-methyl]sulfinyl]-1H-benzimidazole sodium salt
IUPAC Name: sodium;5-(difluoromethoxy)-2-[(3,4-dimethoxypyridin-2-yl)methylsulfinyl]benzimidazol-1-ide
Synonym: Eupantol, Pantozol, Protonix, Somac
Melting Point: >30°C (dec)
Solubility: Soluble in water or ethanol.
Appearance: Almost white or white crystalline powder

FIRST AID MEASURES of PANTOPRAZOLE SODIUM SESQUIHYDRATE:
-Description of first-aid measures
*General advice:
Show this material safety data sheet to the doctor in attendance.
*If inhaled:
After inhalation:
Fresh air.
*In case of skin contact:
Take off immediately all contaminated clothing.
Rinse skin with
water/ shower.
*In case of eye contact:
After eye contact:
Rinse out with plenty of water.
Call in ophthalmologist.
Remove contact lenses.
*If swallowed:
After swallowing:
Immediately make victim drink water (two glasses at most).
Consult a physician.
-Indication of any immediate medical attention and special treatment needed.
No data available

ACCIDENTAL RELEASE MEASURES of PANTOPRAZOLE SODIUM SESQUIHYDRATE:
-Environmental precautions:
Do not let product enter drains.
-Methods and materials for containment and cleaning up:
Cover drains.
Collect, bind, and pump off spills.
Observe possible material restrictions.
Take up dry.
Dispose of properly.
Clean up affected area.

FIRE FIGHTING MEASURES of PANTOPRAZOLE SODIUM SESQUIHYDRATE:
-Extinguishing media:
*Suitable extinguishing media:
Carbon dioxide (CO2)
Foam
Dry powder
*Unsuitable extinguishing media:
For this substance/mixture no limitations of extinguishing agents are given.
-Further information:
Prevent fire extinguishing water from contaminating surface water or the ground water system.

EXPOSURE CONTROLS/PERSONAL PROTECTION of PANTOPRAZOLE SODIUM SESQUIHYDRATE:
-Control parameters:
--Ingredients with workplace control parameters:
-Exposure controls:
--Personal protective equipment:
*Eye/face protection:
Use equipment for eye protection.
Safety glasses
*Body Protection:
protective clothing
*Respiratory protection:
Recommended Filter type: Filter A
-Control of environmental exposure:
Do not let product enter drains.

HANDLING and STORAGE of PANTOPRAZOLE SODIUM SESQUIHYDRATE:
-Conditions for safe storage, including any incompatibilities:
*Storage conditions:
Tightly closed.
Dry.

STABILITY and REACTIVITY of PANTOPRAZOLE SODIUM SESQUIHYDRATE:
-Chemical stability:
The product is chemically stable under standard ambient conditions (room temperature).
-Possibility of hazardous reactions:
No data available