Omeprazole sodium
(Synonyms: 奥美拉唑钠,H 16868 sodium) 目录号 : GC61155
An irreversible inhibitor of the gastric proton pump
Cas No.:95510-70-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Omeprazole is a selective and irreversible inhibitor of the gastric H+/K+ ATPase pump (IC50 = 1.1 μM).1 It is a racemic mixture of two enantiomers, (S)-omeprazole and (R)-omeprazole , which are prodrugs of the active sulfonamide formed by acid-stimulated conversion.2,3 Both enantiomers are extensively metabolized by the cytochrome P450 (CYP) isomers CYP2C19 and CYP3A4.3
1.Smolka, A.J., Goldenring, J.R., Gupta, S., et al.Inhibition of gastric H,K-ATPase activity and gastric epithelial cell IL-8 secretion by the pyrrolizine derivative ML 3000BMC Gastroenterol.4(4)(2004) 2.Richardson, P., Hawkey, C.J., and Stack, W.A.Proton pump inhibitors. Pharmacology and rationale for use in gastrointestinal disordersDrugs56(3)307-335(1998) 3.Shi, S., and Klotz, U.Proton pump inhibitors: An update of their clinical use and pharmacokineticsEur. J. Clin. Pharmacol.64(10)935-951(2008)
| Cas No. | 95510-70-6 | SDF | |
| 别名 | 奥美拉唑钠,H 16868 sodium | ||
| Canonical SMILES | O=S(C1=NC2=CC=C(OC)C=C2N1[Na])CC3=NC=C(C)C(OC)=C3C | ||
| 分子式 | C17H18N3NaO3S | 分子量 | 367.4 |
| 溶解度 | DMSO: 250 mg/mL (680.46 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.7218 mL | 13.6091 mL | 27.2183 mL |
| 5 mM | 0.5444 mL | 2.7218 mL | 5.4437 mL |
| 10 mM | 0.2722 mL | 1.3609 mL | 2.7218 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Compatibility studies between mannitol and Omeprazole sodium isomers
J Pharm Biomed Anal 2008 Sep 29;48(2):356-60.PMID:18374534DOI:10.1016/j.jpba.2008.02.009.
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 have been 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) infrared (IR) spectroscopy in a powder mixture and localized thermal analysis (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.
Pharmacokinetics and bioequivalence evaluation of omeprazole and sodium bicarbonate dry suspensions in healthy Chinese volunteers
Sci Rep 2023 Jan 20;13(1):1113.PMID:36670124DOI:10.1038/s41598-022-27286-5.
Omeprazole and sodium bicarbonate dry suspension are effective treatments for acid-related disorders. This study compared the bioequivalence and safety of the two formulations of omeprazole and sodium bicarbonate powder and assessed how CYP2C19 gene polymorphisms affect pharmacokinetics (PK). A single-center, randomized, single-dose, 2-sequence and 2-period crossover method was performed in forty healthy Chinese subjects. Blood samples were collected after a single dose for PK (AUC0-∞, AUC0-t, and Cmax) analysis. The concentrations of Omeprazole in human plasma were determined by HPLC-MS/MS. Besides, the gene polymorphisms of CYP2C19 were assessed by Sanger sequencing. The geometric mean ratios (90% confidence interval) [GMR (95% CI)] of Test/Reference preparation for Cmax: 95.2% (88.48%, 102.43%), AUC0-t: 97.47% (94.4%, 101.02%), AUC0-∞: 97.68% (94.27%, 101.21%) were within the range of 80.00-125.00%. The non-parametric test showed no statistical difference in Tmax between the two groups (p > 0.05). All drugs were well tolerated, no severe adverse reactions occurred, and no significant differences in adverse events between the two drugs. For CYP2C19 gene polymorphisms, the results showed that of 40 subjects, 12 subjects were extensive metabolizers, 24 were intermediate metabolizers, and 4 were poor metabolizers, the frequency of metabolic genotypes were 30%, 60%, and 10%. And the allele distributions for CYP2C19 were *1, *2, and *3 at 60%, 38.75%, and 1.25%. Both the CYP2C19 alleles and metabolic genotypes were consistent with other studies in Chinese. The results of PK parameters showed that different genotypes of CYP2C19 lead to significant differences in t1/2, AUC0-t, AUC0-∞ and Cmax, but no significant differences in Tmax in each group. At the same time, we confirmed that the PK parameters of the test and reference had no differences between the males and females. This study has shown that the pharmacokinetic parameters of the two formulations are not significantly different, which showed bioequivalence and exemplary safety. CYP2C19 gene polymorphism significantly differed in the PK parameters of Omeprazole sodium bicarbonate powder.
Physical and thermal characterisation of chiral Omeprazole sodium salts
J Pharm Biomed Anal 2006 Sep 11;42(1):25-31.PMID:16524682DOI:10.1016/j.jpba.2005.12.039.
The physical properties of drug substances may affect stability, manufacturing, dissolution and bioavailability. Variations in the degree of crystallinity in a pharmaceutical substance may exhibit physicochemical differences that impact at therapeutic, manufacturing, commercial and legal levels, yet no reference has been found on the physical properties of micronised omeprazole. This study reports on the physical and thermal characterisation of the sodium salts of S- and R-omeprazole, using diffuse reflectance infrared Fourier transform spectroscopy (DRIFT), scanning electron microscopy (SEM), differential scanning calorimetry (DSC), microthermal analysis (microTA) and powder X-ray diffraction (XRPD). DSC experiments were performed in order to determine not only their thermal stability, but also the thermal history of both forms. SEM results indicate similar morphology, particle size and shape of powdered drug, while, microTA of processed discs shows different topographical images for S- and R-omeprazole, exhibiting a smoother surface for the S-form, indicative of the smoother particle size not evident in the SEM results. The low level of crystallinity of both enantiomers was confirmed by DRIFT spectroscopy and XRPD. Thermal stability by DSC of S- and R-omeprazole sodium salts was superior to that of the neutral omeprazole. This study has examined the physical and thermal properties of both forms and in highlighting their differences provides an explanation for the potential differences in bioavailability and therapeutic efficacy.