Ilaprazole sodium
(Synonyms: 艾普拉唑钠,IY-81149 sodium) 目录号 : GC60929
A gastric proton pump inhibitor
Cas No.:172152-50-0
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Ilaprazole is a proton pump inhibitor that inhibits H+/K+-ATPase activity in isolated rabbit gastric mucosa (IC50 = 6 ?M).1 In vivo, ilaprazole reduces gastric acid secretion induced by pentagastrin or histamine in anesthetized rats (ED50s = 0.38 and 1.2 mg/kg, respectively). It also reduces histamine-induced gastric acid secretion in Heidenhain pouch dogs. Formulations containing ilaprazole have been used in the treatment of peptic ulcers and gastroesophageal reflux disease (GERD).
1.Kwon, D., Chae, J.B., Park, C.W., et al.Effects of IY-81149, a newly developed proton pump inhibitor, on gastric acid secretion in vitro and in vivoArzneimittelforschung51(3)204-213(2001)
| Cas No. | 172152-50-0 | SDF | |
| 别名 | 艾普拉唑钠,IY-81149 sodium | ||
| Canonical SMILES | O=S(C1=NC2=CC=C(N3C=CC=C3)C=C2[N-]1)CC4=NC=CC(OC)=C4C.[Na+] | ||
| 分子式 | C19H17N4NaO2S | 分子量 | 388.42 |
| 溶解度 | DMSO : 78mg/mL | 储存条件 | 4°C, protect from light |
| 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 | 2.5745 mL | 12.8727 mL | 25.7453 mL |
| 5 mM | 0.5149 mL | 2.5745 mL | 5.1491 mL |
| 10 mM | 0.2575 mL | 1.2873 mL | 2.5745 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。
The study of intestinal absorption and biodistribution in vivo of proton pump inhibitors
Eur J Pharm Biopharm 2020 Apr;149:135-144.PMID:32007590DOI:10.1016/j.ejpb.2020.01.015.
The major therapeutic strategy for acid-related gastrointestinal diseases in clinic is to reduce the excretion of gastric acid by oral administration of proton-pump inhibitors (PPIs). However, it is quite a challenge to study the oral absorption behaviors of PPIs considering their extreme instability under gastrointestinal environment. As a result, little information has been reported on PPI oral absorption so far, hindering the further development of PPI-contained oral preparations. Here, we first investigated the degradation rate of three representative PPIs, including ilaprazole, Ilaprazole sodium and rabeprazole sodium. Then a modified in situ intestine absorption method in rat was established: through the temperature control by the heat exchangers, the perfusate was kept at physiological temperature only when passing through the intestine while it was maintained at 4 °C outside the intestine. Therefore PPIs could maintained sufficiently high stability under proper temperature control. Our data demonstrated that both ilaprazole and Ilaprazole sodium exhibited significantly higher absorption efficiency than rabeprazole sodium did through the comparison of their apparent permeability coefficients and steady-state plasma concentrations after perfusion in the duodenum, jejunum, ileum and colon, mainly attributing to their more suitable oil-water partition coefficient. The duodenum could be the best site for the oral absorption of PPIs. Ilaprazole outperformed its sodium salt form with its stable absorption behavior in tested four intestinal segments. Furthermore, after intravenous or oral administration, ilaprazole exhibited a longer residence time and a higher accumulation in the stomach than in most of other tissues/organs. However, it was also found that the accumulation was heterogeneous and mainly located in mucosa cells of the stomach. Our further study indicated that there was no significant difference on the oral absorption efficiency of ilaprazole between female and male rats but ilaprazole underwent a faster metabolism in male rats after oral absorption. Our study provided a valuable guidance for the design of oral formulation and the optimization of PPI-contained formulations.