Tag: M.W=350-400

Maddiboyina, Balaji published the artcilePreparation and evaluation of esomeprazole enteric coated tablets, Safety of Sodium (S)-6-methoxy-2-(((4-methoxy-3,5-dimethylpyridin-2-yl)methyl)sulfinyl)benzo[d]imidazol-1-ide, the publication is International Journal of Pharmacy and Pharmaceutical Research (2020), 18(1), 16-30, database is CAplus.

Esomeprazole sodium is a proton pump inhibitor used to treat peptic ulcer, duodenal ulcer, gastro oesophageal reflux disease by inhibiting the enzyme H⁺/K⁺ATPase. The objective of the revision is to formulate and evaluate the Delayed Release tablets and parallel with that of innovator product. The principal intension is to delay the release of drug which is incapacitated by the stomach contents. Methacrylicacid copolymer (EudragitL30D55) was used as an enteric coating material in the formulation. Eight formulations of enteric coated tablets of Esomeprazole was advanced by preparing core tablets using mannitol as diluent, Crospovidone as super disintegrant, povidone (PVP K-30) as binder in diverse extents and variable the compositions of sub coating and enteric coating using sicovit yellow, titanium dioxide and eudragit.The core tablets were prepared by dry granulation method. Formulation F7 was institute to be acid resistant and invitro drug release was also insightful and akin to the innovator product. Stability study is conceded out for 2 mo at 25°C; 60% RH: and 40°C; 75%RH, bestowing to ICH guidelines. The tablets were tested for acid release through the stability period and inveterate that results were institute within the limits. H⁺/K⁺ATPase, inhibition by the Esomeprazole effect the gastric acid formation progression and is dose-dependent and delivers for exceedingly operative inhibition of both basal acid secretion and stimulated acid secretion, irresp. of the stimulus.

International Journal of Pharmacy and Pharmaceutical Research published new progress about 161796-78-7. 161796-78-7 belongs to imidazoles-derivatives, auxiliary class Membrane Transporter/Ion Channel,Proton Pump, name is Sodium (S)-6-methoxy-2-(((4-methoxy-3,5-dimethylpyridin-2-yl)methyl)sulfinyl)benzo[d]imidazol-1-ide, and the molecular formula is C17H18N3NaO3S, Safety of Sodium (S)-6-methoxy-2-(((4-methoxy-3,5-dimethylpyridin-2-yl)methyl)sulfinyl)benzo[d]imidazol-1-ide.

Referemce:
https://en.wikipedia.org/wiki/Imidazole,
Imidazole | C3H4N2 – PubChem

Bachhav, Rishikesh S. published the artcileAssay Test procedure as a CPP at Bulk-Solution stage – Esomeprazole Sodium Injection 40MG, Category: imidazoles-derivatives, the publication is World Journal of Pharmaceutical Research (2020), 9(5), 1565-1580, database is CAplus.

A review. To develop & validate the anal. Assay Test procedure as a Critical Processing Parameters at the Bulk-Solution stage during manufacturing of Esomeprazole Sodium Injection 40mg. As per current available literature and the references, Esomeprazole active substance is available in market in five forms, i.e. Esomeprazole as Plan active [Tablet]; Esomeprazole Magnesium Trihydrate [Tablet, Capsule Delayed Release]; Esomeprazole Potassium [Tablet & Capsule]; Esomeprazole Strontium [Capsule Delayed Release] and Esomeprazole Sodium [Injectable]. Assay test for Active & other dosage forms [Tablet, Capsule] were available. Available Test procedure are based on either Potentiometory Titration or HPLC basis. Esomeprazole Sodium Injection 40mg Dosage form is not in any pharmacopeia. As per available reference & literature assay test method for intermediate testing & finished product is based on HPLC. Intermediate testing [In-Process Testing] require as Critical Process Parameters [CPP] to ensure the quality i.e. appropriate bulk-solution purity, before to proceed for filling of Bulk-solution in unit dosage form [Vials]. To test the bulk solution purity approx. 5-6 h required. Which leads to hold the Bulk solution, further it impact & may risk bio-burdon of bulk solution Also it impact & reduce the productivity of line by 5-6 h. HPLC testing required special skilled manpower & cost. Considering all above concerns of current available test methods; this article project is selected to develop & validate the anal. Assay Test procedure as a Critical Processing Parameters at the Bulk-Solution stage during manufacturing of Esomeprazole Sodium Injection 40mg.

World Journal of Pharmaceutical Research published new progress about 161796-78-7. 161796-78-7 belongs to imidazoles-derivatives, auxiliary class Membrane Transporter/Ion Channel,Proton Pump, name is Sodium (S)-6-methoxy-2-(((4-methoxy-3,5-dimethylpyridin-2-yl)methyl)sulfinyl)benzo[d]imidazol-1-ide, and the molecular formula is C17H18N3NaO3S, Category: imidazoles-derivatives.

Referemce:
https://en.wikipedia.org/wiki/Imidazole,
Imidazole | C3H4N2 – PubChem

Howard, Philip H. published the artcileIdentifying New Persistent and Bioaccumulative Organics Among Chemicals in Commerce II: Pharmaceuticals, HPLC of Formula: 161796-78-7, the publication is Environmental Science & Technology (2011), 45(16), 6938-6946, database is CAplus and MEDLINE.

The goal was to identify com. pharmaceuticals that might be persistent and bioaccumulative (P&B) and that were not being considered in current wastewater and aquatic environmental measurement programs. We developed a database of 3193 pharmaceuticals from 2 US Food and Drug Administration (FDA) databases and some lists of top ranked or selling drugs. Of the 3193 pharmaceuticals, 275 pharmaceuticals have been found in the environment and 399 pharmaceuticals were, based on production volumes, designated as high production volume (HPV) pharmaceuticals. All pharmaceuticals that had reported chem. structures were evaluated for potential bioaccumulation (B) or persistence (P) using quant. structure property relationships (QSPR) or scientific judgment. Of the 275 drugs detected in the environment, 92 were rated as potentially bioaccumulative, 121 were rated as potentially persistent, and 99 were HPV pharmaceuticals. After removing the 275 pharmaceuticals previously detected in the environment, 58 HPV compounds were identified that were both P&B and 48 were identified as P only. Of the non-HPV compounds, 364 pharmaceuticals were identified that were P&B. This study has yielded some interesting and probable P&B pharmaceuticals that should be considered for further study.

Environmental Science & Technology published new progress about 161796-78-7. 161796-78-7 belongs to imidazoles-derivatives, auxiliary class Membrane Transporter/Ion Channel,Proton Pump, name is Sodium (S)-6-methoxy-2-(((4-methoxy-3,5-dimethylpyridin-2-yl)methyl)sulfinyl)benzo[d]imidazol-1-ide, and the molecular formula is C17H18N3NaO3S, HPLC of Formula: 161796-78-7.

Referemce:
https://en.wikipedia.org/wiki/Imidazole,
Imidazole | C3H4N2 – PubChem

Bi, Yiling published the artcileRepurposing of Proton Pump Inhibitors as first identified small molecule inhibitors of endo-β-N-acetylglucosaminidase (ENGase) for the treatment of NGLY1 deficiency, a rare genetic disease, Name: Sodium (S)-6-methoxy-2-(((4-methoxy-3,5-dimethylpyridin-2-yl)methyl)sulfinyl)benzo[d]imidazol-1-ide, the publication is Bioorganic & Medicinal Chemistry Letters (2017), 27(13), 2962-2966, database is CAplus and MEDLINE.

N-Glycanase deficiency, or NGLY1 deficiency, is an extremely rare human genetic disease. N-Glycanase, encoded by the gene NGLY1, is an important enzyme involved in protein deglycosylation of misfolded proteins. Deglycosylation of misfolded proteins precedes the endoplasmic reticulum (ER)-associated degradation (ERAD) process. NGLY1 patients produce little or no N-glycanase (Ngly1), and the symptoms include global developmental delay, frequent seizures, complex hyperkinetic movement disorder, difficulty in swallowing/aspiration, liver dysfunction, and a lack of tears. Unfortunately, there has not been any therapeutic option available for this rare disease so far. Recently, a proposed mol. mechanism for NGLY1 deficiency suggested that endo-β-N-acetylglucosaminidase (ENGase) inhibitors may be promising therapeutics for NGLY1 patients. Herein, we performed structure-based virtual screening utilizing FDA-approved drug database on this ENGase target to enable repurposing of existing drugs. Several Proton Pump Inhibitors (PPIs), a series of substituted 1H-benzo [d] imidazole, and 1H-imidazo [4,5-b] pyridines, among other scaffolds, have been identified as potent ENGase inhibitors. An electrophoretic mobility shift assay was employed to assess the inhibition of ENGase activity by these PPIs. Our efforts led to the discovery of Rabeprazole Sodium as the most promising hit with an IC₅₀ of 4.47 ± 0.44 μM. This is the first report that describes the discovery of small mol. ENGase inhibitors, which can potentially be used for the treatment of human NGLY1 deficiency.

Bioorganic & Medicinal Chemistry Letters published new progress about 161796-78-7. 161796-78-7 belongs to imidazoles-derivatives, auxiliary class Membrane Transporter/Ion Channel,Proton Pump, name is Sodium (S)-6-methoxy-2-(((4-methoxy-3,5-dimethylpyridin-2-yl)methyl)sulfinyl)benzo[d]imidazol-1-ide, and the molecular formula is C17H18N3NaO3S, Name: Sodium (S)-6-methoxy-2-(((4-methoxy-3,5-dimethylpyridin-2-yl)methyl)sulfinyl)benzo[d]imidazol-1-ide.

Referemce:
https://en.wikipedia.org/wiki/Imidazole,
Imidazole | C3H4N2 – PubChem

Agatonovic-Kustrin, S. published the artcileCompatibility studies between mannitol and omeprazole sodium isomers, Recommanded Product: Sodium (S)-6-methoxy-2-(((4-methoxy-3,5-dimethylpyridin-2-yl)methyl)sulfinyl)benzo[d]imidazol-1-ide, the publication is Journal of Pharmaceutical and Biomedical Analysis (2008), 48(2), 356-360, database is CAplus and MEDLINE.

Omeprazole, commonly used in the treatment of various gastrointestinal disorders degrades rapidly in acidic pHs and results in inter-individual variability due to different rates of metabolism amongst patients. Since S-omeprazole shows more predictable bioavailability and excipients were known to interact with active pharmaceutical ingredients to produce altered bioavailability, it was decided to investigate the compatibility of omeprazole sodium isomers with mannitol, the major excipient in omeprazole formulations using differential scanning calorimetry (DSC) for bulk drug, attenuated total reflectance (ATR) IR spectroscopy in a powder mixture and localized thermal anal. (LTA) from a drug disk. DSC results clearly indicate an interaction between mannitol and R-omeprazole sodium due to decreased melting temperatures and broadening peaks. The DSC of S-omeprazole sodium does not show melting temperature although the drug was crystalline Because of the accelerated temperature conditions during DSC experiments applied in this work, ATR-IR was undertaken to determine whether these results occurred at room temperature for the solid dosage form. The ATR-IR results show a difference between R- and S-omeprazole sodium with mannitol by the appearance of both the amino (N-H) and imino (=N-H) stretching frequencies for R-omeprazole and only the N-H for the S-omeprazole sodium. It may thus be concluded that different ratios for the tautomeric forms for S- and R-omeprazole sodium result in changes in the degree of crystallinity and are responsible for the interaction with mannitol, common excipient in formulation. These interactions may be directly related to the difference in terms of bioavailability.

Journal of Pharmaceutical and Biomedical Analysis published new progress about 161796-78-7. 161796-78-7 belongs to imidazoles-derivatives, auxiliary class Membrane Transporter/Ion Channel,Proton Pump, name is Sodium (S)-6-methoxy-2-(((4-methoxy-3,5-dimethylpyridin-2-yl)methyl)sulfinyl)benzo[d]imidazol-1-ide, and the molecular formula is C17H18N3NaO3S, Recommanded Product: Sodium (S)-6-methoxy-2-(((4-methoxy-3,5-dimethylpyridin-2-yl)methyl)sulfinyl)benzo[d]imidazol-1-ide.

Referemce:
https://en.wikipedia.org/wiki/Imidazole,
Imidazole | C3H4N2 – PubChem

Wang, Zhao-Qun published the artcileEnantioseparation characteristics of biselector chiral stationary phases based on derivatives of cellulose and amylose, Related Products of imidazoles-derivatives, the publication is Journal of Chromatography A (2014), 57-68, database is CAplus and MEDLINE.

Cellulose tris(4-methylphenylcarbamate) (CMPC) and cellulose tris(4-chlorophenylcarbamate) (CCPC) are known for their powerful chiral recognition capability, and the chiral columns prepared from these two polymers were commercialized. However, the chiral stationary phases (CSPs) can be only used in the mobile phases containing �0% ethanol (referring to CMPC) or cannot be used in ethanol-containing mobile phases (referring to CCPC). To overcome the defect and to study the enantioseparation characteristics of biselector CSPs, CMPC, cellulose tris(phenylcarbamate) (CPC) and CCPC were, resp., mixed with amylose tris(3,5-dimethylphenylcarbamte) (ADMPC) at a ratio of 1:1 (mol/mol) of glucose unit, and three new CSPs were prepared by coating the resulting blends on 3-aminopropyl silica gel. For the purpose of enantioseparation comparison, the corresponding single selector CSPs were also prepared with the individual derivatives of cellulose and amylose. The enantioseparation evaluation indicated that the biselector CSPs still bear excellent enantioseparation capability. The interaction between two polymers in each blend was studied by using CD spectroscopy. Owing to the interaction, the durability of the biselector CSP derived from CMPC and ADMPC was significantly improved. The CSP could be analyzed with a mobile phase of 100% ethanol. And the biselector CSP derived from CCPC and ADMPC could safely work in a normal phase containing 30% ethanol. Therefore, the workable ranges of the mobile phases were broadened. The elution order on the biselector CSPs was generally dominated by the one on the corresponding single selector CSPs that provided a higher resolution The suprastructure variation caused by the interaction between the individual polymers might also affect the enantioseparation of the biselector CSPs. The trends of the retention factors and the resolutions of partially racemic mixtures are discussed.

Journal of Chromatography A published new progress about 161796-78-7. 161796-78-7 belongs to imidazoles-derivatives, auxiliary class Membrane Transporter/Ion Channel,Proton Pump, name is Sodium (S)-6-methoxy-2-(((4-methoxy-3,5-dimethylpyridin-2-yl)methyl)sulfinyl)benzo[d]imidazol-1-ide, and the molecular formula is C6H3ClFNO2, Related Products of imidazoles-derivatives.

Referemce:
https://en.wikipedia.org/wiki/Imidazole,
Imidazole | C3H4N2 – PubChem

Tang, Sheng published the artcilePerformance comparison of chiral separation materials derived from N-cyclohexylcarbonyl and N-hexanoyl chitosans, Related Products of imidazoles-derivatives, the publication is Journal of Chromatography A (2018), 112-123, database is CAplus and MEDLINE.

Chitosan bis(phenylcarbamate)-(N-cyclohexylformamide)s and chitosan bis(phenylcarbamate)-(N-hexanamide)s were synthesized as chiral selectors for enantiomeric separation Since two types of substituents with different structures were, resp., introduced onto the 2-position and the 3-/6-positions of the glucose skeleton in the chitosans through a heterogeneous modification pathway, the enantioseparation performances of the chiral selectors could be improved. Influence and position of the substituents on chiral recognition and enantioseparation abilities was studied in detail, and the structural dependence on enantioseparation performance was particularly demonstrated. Me- and chloro-substituted chitosan bis(phenylcarbamate)-(N-hexanamide)s possessed comparable enantioseparation performances, whereas chloro-substituted chitosan bis(phenylcarbamate)-(N-cyclohexylformamide)s exhibited much more powerful chiral recognition and enantioseparation abilities than the Me-substituted ones. Among all the prepared chiral selectors, those with the combination of the cyclohexyl group at the 2-position of the glucose skeleton in the chitosan derivatives and the chlorophenyl group at the 3-/6-positions seemed to be more preferable for enantiomeric separation As a result, the chitosan bis(3,4-dichlorophenylcarbamate)-(N-cyclohexylformamide) possessed the best enantioseparation performance. The solvent tolerability of the prepared chiral selectors was also studied. Compared with the classical coated-type chiral separation materials derived from cellulose/amylose derivatives, the N-cyclohexylcarbonyl and N-hexanoyl chitosans based chiral stationary phases possess more favorable solvent tolerability, thus possibly widening their applications for various practical enantioseparations

Journal of Chromatography A published new progress about 161796-78-7. 161796-78-7 belongs to imidazoles-derivatives, auxiliary class Membrane Transporter/Ion Channel,Proton Pump, name is Sodium (S)-6-methoxy-2-(((4-methoxy-3,5-dimethylpyridin-2-yl)methyl)sulfinyl)benzo[d]imidazol-1-ide, and the molecular formula is C7H8BBrO3, Related Products of imidazoles-derivatives.

Referemce:
https://en.wikipedia.org/wiki/Imidazole,
Imidazole | C3H4N2 – PubChem

Lin, Shu-yu published the artcileStudy on compatible stability of esomeprazole sodium for injection with six kinds of common solvents, Computed Properties of 161796-78-7, the publication is Yiyao Daobao (2012), 31(9), 1210-1213, database is CAplus.

The appropriate HPLC detection for studying the stability of esomeprazole (Eso) sodium for injection with six kinds of common solvents was investigated, and thus provided an evidence for using reasonable compound preparation in clin. use. The Eso sodium for injection was compatible with 100 mL six kinds of common solvents resp., and the pH value was detected. The content of Eso sodium in the compatible solution was analyzed by HPLC. The color and clarity were observed at regular time. Eso showed a good linear relationship within the range of 0.05-1.60 mg·mL^-1 (R²=0.9999). There were no significant changes on pH value, color, clarity and content within 24 h after being mixed with 0.9% sodium chloride injection and xylitol one. No distinct changes appeared 12 h, 8 h and 6 h after being mixed with 10% GS, 5% GS, 5% GNS injection, and the Eso solutions of which were relatively stable. While, the situation was different for Eso mixed with fructose injection. Eso was incompatible with fructose injection and showed better compatibility with 0.9% NS or 5% xylitol injection. The drip of admixture should be finished within 12 h, 8 h and 6 h when mixing with 10% GS, 5% GS, 5% GNS, resp.

Yiyao Daobao published new progress about 161796-78-7. 161796-78-7 belongs to imidazoles-derivatives, auxiliary class Membrane Transporter/Ion Channel,Proton Pump, name is Sodium (S)-6-methoxy-2-(((4-methoxy-3,5-dimethylpyridin-2-yl)methyl)sulfinyl)benzo[d]imidazol-1-ide, and the molecular formula is C17H18N3NaO3S, Computed Properties of 161796-78-7.

Referemce:
https://en.wikipedia.org/wiki/Imidazole,
Imidazole | C3H4N2 – PubChem

Yu, Yong published the artcileSynthesis of sodium esomeprazole, SDS of cas: 161796-78-7, the publication is Huaxue Yanjiu Yu Yingyong (2014), 26(4), 591-595, database is CAplus.

Esomeprazole sodium was synthesized through asym. oxidation reaction, and the synthesis process route was optimized. The ufiprazole was prepared firstly, which was then oxidized to form esomeprazole. Finally, the esomeprazole sodium was prepared by reaction of esomeprazole with sodium hydroxide. The overall yield was 57.2%. The structures of target compounds were characterized by IR, ¹H NMR and MS.

Huaxue Yanjiu Yu Yingyong published new progress about 161796-78-7. 161796-78-7 belongs to imidazoles-derivatives, auxiliary class Membrane Transporter/Ion Channel,Proton Pump, name is Sodium (S)-6-methoxy-2-(((4-methoxy-3,5-dimethylpyridin-2-yl)methyl)sulfinyl)benzo[d]imidazol-1-ide, and the molecular formula is C19H21N3O3S, SDS of cas: 161796-78-7.

Referemce:
https://en.wikipedia.org/wiki/Imidazole,
Imidazole | C3H4N2 – PubChem

Anonymous published the artcilePreparation of 5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]sulfinyl]-1H-benzimidazole zinc salt, Related Products of imidazoles-derivatives, the publication is Research Disclosure (2002), 462(Oct.), P1835, database is CAplus.

A method for the preparing the Zn salt of (S)-5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]sulfinyl]-1H-benzimidazole is described. The compound was prepared by dissolving 0.185 g of 1.36 mmol Zn chloride in a 25 mL of H₂O. The formed solution is then added dropwise to 50mL aqueous solution of 1g, 2.7 mmol 5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]sulfinyl]-1H-benzimidazole Na salt while stirring at room temperature The mixture is stirred for an hour and the resulting precipitate is filtered off. The filter cake was washed with a mixture of ether and 25mL acetone. The product is then suspended in an EtOH and thereafter dried at reduced pressure. A 0.70 g of the Zn salt can be obtained with a Zn content of 8.8%.

Research Disclosure published new progress about 161796-78-7. 161796-78-7 belongs to imidazoles-derivatives, auxiliary class Membrane Transporter/Ion Channel,Proton Pump, name is Sodium (S)-6-methoxy-2-(((4-methoxy-3,5-dimethylpyridin-2-yl)methyl)sulfinyl)benzo[d]imidazol-1-ide, and the molecular formula is C17H18N3NaO3S, Related Products of imidazoles-derivatives.

Referemce:
https://en.wikipedia.org/wiki/Imidazole,
Imidazole | C3H4N2 – PubChem