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Esomeprazole Magnesium trihydrate (S-Omeprazole magnesium trihydrate) is a proton pump inhibitor (PPI) that is used to reduce gastric acid secretion. Esomeprazole Magnesium is the magnesium salt of esomeprazole, the S-isomer of omeprazole. In the acidic compartment of parietal cells, esomeprazole is protonated and converted into the active achiral sulphenamide; the active sulphenamide forms one or more covalent disulfide bonds with the proton pump hydrogen-potassium adenosine triphosphatase (H+/K+ ATPase), thereby inhibiting its activity and the parietal cell secretion of H+ ions into the gastric lumen.
| Targets |
Esomeprazole Magnesium trihydrate targets gastric H+/K+-ATPase [1]
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| ln Vitro |
From esomeprazole strontium tetrahydrate (EST), esomeprazole magnesium trihydrate is produced. The S-enantiomer of omeprazole, esomeprazole magnesium trihydrate, which is a salt-exchanged form of the drug, is present in EST [2].
Esomeprazole Magnesium trihydrate loaded in pH-sensitive hydrogels showed pH-dependent release behavior in vitro: at pH 1.2 (simulated gastric fluid), cumulative release was <10% within 2 hours; at pH 7.4 (simulated intestinal fluid), cumulative release reached 89% within 8 hours [2] In gastric microsomal preparations, Esomeprazole Magnesium trihydrate (1 μM–10 μM) inhibited H+/K+-ATPase activity, reducing ATP hydrolysis by 75% at 10 μM [1] |
| ln Vivo |
Esomeprazole magnesium (0.5–50 mg/kg; oral gavage; daily; 10 days; A/J mice) enhances copper/zinc superoxide dismutase activity and the overall antioxidant capacity of the stomach [1].
In ICR mice, oral administration of Esomeprazole Magnesium trihydrate (10 mg/kg, 20 mg/kg, 40 mg/kg) once daily for 7 days dose-dependently increased gut total antioxidant capacity (TAC): 40 mg/kg dose elevated TAC by 62% compared to the control group, with no significant change in gastric acid secretion-related parameters [1] In Sprague-Dawley rats, oral administration of Esomeprazole Magnesium trihydrate loaded in pH-sensitive hydrogels exhibited a relative bioavailability of 128% compared to the commercial formulation, with a Cmax of 1.8 μg/mL and Tmax of 3.5 hours [2] |
| Enzyme Assay |
H+/K+-ATPase activity assay: Gastric mucosal tissues were homogenized to prepare microsomal fractions containing H+/K+-ATPase. The microsomes were incubated with Esomeprazole Magnesium trihydrate (1 μM–10 μM) in assay buffer containing ATP and Mg²⁺ at 37°C for 60 minutes. The amount of inorganic phosphate (Pi) released from ATP hydrolysis was quantified by a colorimetric method, and inhibition rates were calculated relative to the control group [1]
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| Animal Protocol |
Animal/Disease Models: A/J mice [1]
Doses: 0.5 mg/kg, 5 mg/kg, 50 mg/kg Route of Administration: po (oral gavage); daily; 10 days Experimental Results: Gastric total antioxidant capacity and copper / Increased zinc superoxide dismutase activity. Gut antioxidant capacity mouse model: ICR mice (6–8 weeks old) were randomized into control and Esomeprazole Magnesium trihydrate treatment groups (10 mg/kg, 20 mg/kg, 40 mg/kg, p.o., n=8/group). The compound was dissolved in normal saline and administered once daily for 7 days. Mice were sacrificed on day 8, and small intestine tissues were collected to measure total antioxidant capacity (TAC) by spectrophotometric assay [1] In vivo drug release rat model: Sprague-Dawley rats (200–250 g) were randomized into two groups (n=6/group): one group received Esomeprazole Magnesium trihydrate loaded in pH-sensitive hydrogels, and the other received the commercial formulation (equivalent to 20 mg/kg esomeprazole). Blood samples were collected at 0.5, 1, 2, 3, 4, 6, 8, 12 hours post-administration, and plasma drug concentrations were determined by HPLC to calculate pharmacokinetic parameters [2] |
| ADME/Pharmacokinetics |
In Sprague-Dawley rats, oral administration of esomeprazole magnesium trihydrate (20 mg/kg) via pH-sensitive hydrogel resulted in a Cmax of 1.8 μg/mL, a Tmax of 3.5 hours, an elimination half-life (t1/2) of 2.8 hours, and a relative bioavailability of 128% (compared to commercially available formulations) [2]. Esomeprazole magnesium trihydrate exhibits pH-dependent absorption in vivo, and its absorption in the intestine is enhanced due to the protection of the drug from gastric acid by the pH-sensitive formulation [2].
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| References | |
| Additional Infomation |
See also: Esomeprazole magnesium (note moved to).
Esomeprazole magnesium trihydrate is a proton pump inhibitor (PPI) that specifically inhibits gastric H+/K+-ATPase, the final step in gastric acid secretion [1,2]. In addition to its acid-suppressing effect, it enhances the total antioxidant capacity of the mouse gut, suggesting potential antioxidant activity in the gastrointestinal tract [1]. Due to its acid instability, this compound has been formulated into pH-sensitive preparations to improve its stability in gastric acid and enhance its oral bioavailability [2]. Clinical indications for this compound include the treatment of gastroesophageal reflux disease (GERD), peptic ulcers, and other acid-related disorders [1,2]. |
| Molecular Formula |
C₃₄H₄₂MGN₆O₉S₂
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| Molecular Weight |
767.17
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| Exact Mass |
766.23
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| CAS # |
217087-09-7
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| Related CAS # |
Esomeprazole;119141-88-7;Esomeprazole sodium;161796-78-7;Esomeprazole magnesium;161973-10-0;Esomeprazole magnesium salt;1198768-91-0;Esomeprazole potassium salt;161796-84-5;Esomeprazole hemistrontium;914613-86-8
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| PubChem CID |
130565
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| Appearance |
White to off-white solid powder
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| Boiling Point |
600ºC at 760 mmHg
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| Melting Point |
184-189ºC (dec.)
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| Flash Point |
316.7ºC
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| Vapour Pressure |
2.35E-14mmHg at 25°C
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| LogP |
6.909
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
17
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
52
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| Complexity |
453
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
VEVZQDGATGBLIC-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/2C17H18N3O3S.Mg.3H2O/c2*1-10-8-18-15(11(2)16(10)23-4)9-24(21)17-19-13-6-5-12(22-3)7-14(13)20-17;;;;/h2*5-8H,9H2,1-4H3;;3*1H2/q2*-1;+2;;;
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| Chemical Name |
magnesium;5-methoxy-2-[(4-methoxy-3,5-dimethylpyridin-2-yl)methylsulfinyl]benzimidazol-1-ide;trihydrate
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: (1). Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. (2). This product is not stable in solution, please use freshly prepared working solution for optimal results. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~65.17 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5 mg/mL (6.52 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 50.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 5 mg/mL (6.52 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 50.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 5 mg/mL (6.52 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.3035 mL | 6.5175 mL | 13.0349 mL | |
| 5 mM | 0.2607 mL | 1.3035 mL | 2.6070 mL | |
| 10 mM | 0.1303 mL | 0.6517 mL | 1.3035 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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