Ibuprofen sodium
(Synonyms: (±)-Ibuprofen sodium) 目录号 : GC66211
Ibuprofen ((±)-Ibuprofen) sodium 是一种具有口服活性的 COX-1 选择性抑制剂，IC50 值为 13 μM。Ibuprofen sodium 抑制细胞增殖、血管生成，并诱导细胞凋亡 (apoptosis)。Ibuprofen sodium 是一种非甾体抗炎试剂和一氧化氮 (NO) 供体。Ibuprofen sodium 可用于疼痛、肿胀、炎症、感染、免疫学、癌症的研究。
Cas No.:31121-93-4
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Ibuprofen ((±)-Ibuprofen) sodium is an orally active, selective COX-1 inhibitor with an IC50 value of 13 μM. Ibuprofen sodium inhibits cell proliferation, angiogenesis, and induces cell apoptosis. Ibuprofen sodium is a nonsteroidal anti-inflammatory agent and a nitric oxide (NO) donor. Ibuprofen sodium can be used in the research of pain, swelling, inflammation, infection, immunology, cancers[1][2][5][8].
Ibuprofen sodium (24 h) inhibits COX-1 and COX-2 activity with IC50 values of 13 μM and 370 μM[1].
Ibuprofen sodium (500 μM, 48 h) inhibits cell proliferation and angiogenesis, and induces apoptosis in AGS cells (Adenocarcinoma gastric cell line)[2].
Ibuprofen sodium (500 μM, 48 h) downregulates transcription of Akt, VEGF-A, PCNA, Bcl2, OCT3/4 and CD44 genes, but upregulates RNA levels of wild type P53 and Bax genes in AGS cell[2].
Ibuprofen sodium (500 μM, 24 h) restores microtubule reformation, microtubule-dependent intracellular cholesterol transport, and induces extension of microtubules to the cell periphery in both cystic fibrosis (CF) cell models and primary CF nasal epithelial cells[3].
Ibuprofen sodium (500 μM, 24 h) enhances UV-induced cell death in MCF-7 cells and MDA-MB-231 cells by a photosensitization process[4].
Cell Viability Assay[2]
| Cell Line: | AGS cells |
| Concentration: | 100-1000 μM |
| Incubation Time: | 24 h, 48 h |
| Result: | Inhibited AGS cell viability with IC50 values of 630 μM (trypan blue staining, 24 h), 456 μM (neutral red assay, 24 h), 549 μM (trypan blue staining , 48 h) and 408 μM (neutral red assay, 48 h). |
Ibuprofen sodium (fed in animal feedings, 300 mg/kg, 14 days) reduces overall tumor growth and enhances anti-tumor immune characteristics without adverse autoimmune reactions in a model of postpartum breast cancer[5].
Ibuprofen sodium (subcutaneous injection, 60 mg/kg, every second day for 15 days) reduces the risk of neuropathy in a rat model of chronic Oxaliplatin?induced peripheral neuropathy[6].
Ibuprofen sodium (oral administration, 20 mg/kg, every 12 hours, 5 doses total) decreases muscle growth (average muscle fiber cross-sectional area) without affecting regulation of supraspinatus tendon adaptions to exercise[7].
Ibuprofen sodium (oral administration, 35 mg/kg, twice daily) attenuates the Inflammatory response to pseudomonas aeruginosa in a rat model of chronic pulmonary infection[8].
| Animal Model: | Syngeneic (D2A1) orthotopic Balb/c mouse model of PPBC (postpartum)[5] |
| Dosage: | 300 mg/kg, daily for 14 days |
| Administration: | Fed in animal feedings (added to pulverized standard chow and mixed dry, then mixed with water, made into chow pellets and dried thoroughly) |
| Result: | Suppresed tumor growth, reduced presence of immature monocytes and increased numbers of T cells. Enhanced Th1 associated cytokines as well as promoted tumor border accumulation of T cells. |
| Animal Model: | Oxaliplatin?induced peripheral neuropathy[6] |
| Dosage: | 60 mg/kg, every second day for 15 days |
| Administration: | Subcutaneous injection |
| Result: | Lowered sensory nerve conduction velocity (SNCV). |
| Cas No. | 31121-93-4 | SDF | Download SDF |
| 别名 | (±)-Ibuprofen sodium | ||
| 分子式 | C13H17NaO2 | 分子量 | 228.26 |
| 溶解度 | H2O : ≥ 100 mg/mL (438.10 mM) | 储存条件 | 4°C, away from moisture |
| 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 | 4.381 mL | 21.9048 mL | 43.8097 mL |
| 5 mM | 0.8762 mL | 4.381 mL | 8.7619 mL |
| 10 mM | 0.4381 mL | 2.1905 mL | 4.381 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。
Ibuprofen sodium dihydrate, an ibuprofen formulation with improved absorption characteristics, provides faster and greater pain relief than ibuprofen acid
Int J Clin Pharmacol Ther 2007 Feb;45(2):89-97.PMID:17323788DOI:10.5414/cpp45089.
Objective: The objective of this 6-hour study was to compare rate of pain relief, analgesic efficacy and tolerability of a novel ibuprofen formulation, Ibuprofen sodium dihydrate, with that of ibuprofen acid in subjects with postoperative dental pain. Material and methods: The test formulation of Ibuprofen sodium dihydrate (256 mg sodium salt) and the reference product both contain 200 mg ibuprofen. Subjects with moderate-to-severe pain after extraction of third molars were randomized to receive two tablets of either Ibuprofen sodium dihydrate (198 subjects) or ibuprofen (198 subjects) in this double-blind, multicenter trial. Pain was measured using traditional descriptor scales and onset of analgesia assessed using the stop-watch method. Results: Median time to substantial pain relief occurred 14 minutes earlier in the Ibuprofen sodium dihydrate group (p < 0.001). The first sign of pain relief, an increase in relief and time until the pain was half gone occurred significantly earlier and faster in the Ibuprofen sodium dihydrate-treated patients (p < 0.02-0.00003). Corresponding numbers needed to treat were in the range 11. Reduction in pain intensity was evident within 5 minutes (p < 0.01) in the Ibuprofen sodium dihydrate group compared to 15 minutes in the ibuprofen group. Pain intensity was reduced to half after 30 and 57 minutes in the Ibuprofen sodium dihydrate and ibuprofen groups, respectively (p < 0.025). The overall analgesic efficacy in terms of summed pain intensity differences (SPID), total pain relief (TOTPAR) and remedication times in the two groups were similar. Both treatments were well tolerated and no serious events occurred. Conclusion: Ibuprofen sodium dihydrate provides faster and more efficacious pain relief during the first hour after intake when compared to a conventional ibuprofen acid formulation. The tolerability profiles are similar.
Bioavailability of ibuprofen following oral administration of standard ibuprofen, sodium ibuprofen or ibuprofen acid incorporating poloxamer in healthy volunteers
BMC Clin Pharmacol 2009 Dec 4;9:19.PMID:19961574DOI:10.1186/1472-6904-9-19.
Background: The aim of this study was to compare the pharmacokinetic properties of sodium ibuprofen and ibuprofen acid incorporating poloxamer with standard ibuprofen acid tablets. Methods: Twenty-two healthy volunteers were enrolled into this randomised, single-dose, 3-way crossover, open-label, single-centre, pharmacokinetic study. After 14 hours' fasting, participants received a single dose of 2x200 mg ibuprofen acid tablets (standard ibuprofen), 2x256 mg Ibuprofen sodium dihydrate tablets (sodium ibuprofen; each equivalent to 200 mg ibuprofen acid) and 2x200 mg ibuprofen acid incorporating 60 mg poloxamer 407 (ibuprofen/poloxamer). A washout period of 2-7 days separated consecutive dosing days. On each of the 3 treatment days, blood samples were collected post dose for pharmacokinetic analyses and any adverse events recorded. Plasma concentration of ibuprofen was assessed using a liquid chromatographic-mass spectrometry procedure in negative ion mode. A standard statistical ANOVA model, appropriate for bioequivalence studies, was used and ratios of 90% confidence intervals (CIs) were calculated. Results: Tmax for sodium ibuprofen was less than half that of standard ibuprofen (median 35 min vs 90 min, respectively; P=0.0002) and Cmax was significantly higher (41.47 microg/mL vs 31.88 microg/mL; ratio test/reference=130.06%, 90% CI 118.86-142.32%). Ibuprofen/poloxamer was bioequivalent to the standard ibuprofen formulation, despite its Tmax being on average 20 minutes shorter than standard ibuprofen (median 75 mins vs 90 mins, respectively; P=0.1913), as the ratio of test/reference=110.48% (CI 100.96-120.89%), which fell within the 80-125% limit of the CPMP and FDA guidelines for bioequivalence. The overall extent of absorption was similar for the three formulations, which were all well tolerated. Conclusion: In terms of Tmax, ibuprofen formulated as a sodium salt was absorbed twice as quickly as from standard ibuprofen acid. The addition of poloxamer to ibuprofen acid did not significantly affect absorption.
Onset of analgesia with sodium ibuprofen, ibuprofen acid incorporating poloxamer and acetaminophen--a single-dose, double-blind, placebo-controlled study in patients with post-operative dental pain
Eur J Clin Pharmacol 2009 Apr;65(4):343-53.PMID:19252905DOI:10.1007/s00228-009-0614-y.
Objective: To compare the onset of action and efficacy of sodium ibuprofen (Ibuprofen sodium dihydrate) and ibuprofen acid incorporating poloxamer (ibuprofen/poloxamer) with that of acetaminophen and placebo in patients with post-operative dental pain.
Methods: A double-blind, randomised, placebo-controlled, active comparator, two-centre study assessing the analgesic efficacy of sodium ibuprofen (512 mg, equivalent to 400 mg ibuprofen acid), ibuprofen/poloxamer (containing 400 mg ibuprofen acid and 120 mg poloxamer 407), acetaminophen (1000 mg) and placebo in patients with moderate-to-severe pain after third molar extraction (n = 322). Onset of action was assessed using the two-stopwatch technique, and pain intensity and relief were measured using validated traditional descriptor scales.
Results: Significantly more patients achieved confirmed perceptible pain relief and meaningful pain relief with sodium ibuprofen (96.3%, P < 0.0001) and ibuprofen/poloxamer (90.0%, P = 0.0005) than with acetaminophen (67.5%). The onset of action of both ibuprofen formulations was comparable with that of acetaminophen up to 45 min post-dose; a marked divergence in onset times in favour of the ibuprofen formulations occurred from 45 min onward. Mean values for the area under the pain relief and pain intensity differences curve (0-6 h) were significantly greater for sodium ibuprofen (3.46) and ibuprofen acid (3.49) than for acetaminophen (2.25) (P < 0.001). Other pain relief and pain intensity endpoints favoured both ibuprofen formulations over acetaminophen. Distractibility from pain (6 h) was significantly greater with the ibuprofen formulations than with acetaminophen (P = 0.008 for sodium ibuprofen; P = 0.03 for ibuprofen/poloxamer). In patients receiving ibuprofen, pain interfered less with daily activities (at 1 and 6 h) than in those receiving acetaminophen (P
Combining Ibuprofen sodium with cellulosic polymers: a deep dive into mechanisms of prolonged supersaturation
Int J Pharm 2014 Nov 20;475(1-2):536-46.PMID:25219860DOI:10.1016/j.ijpharm.2014.09.015.
The combination of a highly soluble salt form of a drug with a polymeric precipitation inhibitor has the potential to prolong drug supersaturation even following salt disproportionation. In this study, dissolution profiles of Ibuprofen sodium in the presence of various cellulosic polymers, including hydroxypropyl methylcellulose (HPMC), methylcellulose (MC), and hydroxypropyl cellulose (HPC), were examined in order to assess degree and duration of supersaturation. In addition, the roles that the polymers played in altering drug solubility, media viscosity, physical form, and particle morphology were also assessed. A deep dive into the mechanisms of supersaturation revealed that intermolecular hydrogen bonding between ibuprofen and HPMC was driving supersaturation through nucleation inhibition and crystal growth modification. Polymer viscosity was proposed as the primary factor prolonging supersaturation of ibuprofen in the presence of MC, while mechanisms other than hydrogen bonding were likely to be attributed to supersaturation with the most hydrophobic polymer evaluated, HPC. Overall, the study suggested that induction of intermolecular interactions between ibuprofen and HPMC were more effective at inhibiting nucleation and maintaining prolonged supersaturation than physical modulation of solution properties, such as viscosity.
Pharmacokinetics of Ibuprofen sodium dihydrate and gastrointestinal tolerability of short-term treatment with a novel, rapidly absorbed formulation
Int J Clin Pharmacol Ther 2005 Mar;43(3):140-9.PMID:15792398DOI:10.5414/cpp43140.
Objective: This paper describes four studies investigating the dissolution, plasma pharmacokinetics and safety of a novel, fast-acting ibuprofen formulation, Ibuprofen sodium dihydrate. Material and method: Four separate studies investigated: the in vitro dissolution rates of Ibuprofen sodium dihydrate (at pH 1.2, 3.5 and 7.2); the bioavailability of Ibuprofen sodium dihydrate (in two pharmacokinetic studies; combined n = 38) compared with conventional ibuprofen, ibuprofen lysinate, ibuprofen arginate and ibuprofen liquagels (all 2 x 200 mg ibuprofen); and the gastroduodenal tolerance of Ibuprofen sodium dihydrate and ibuprofen arginate (both 2 x 200 mg ibuprofen t.i.d.) in an endoscopy safety study, where endoscopy was performed at baseline and at the end of each treatment period using a five-point scale to assess the integrity of the gastric and duodenal mucosa. Results: Ibuprofen sodium dihydrate dissolved significantly more rapidly at pH 1.2, 3.5 and 7.2 than conventional ibuprofen, ibuprofen lysinate and ibuprofen liquagels. Ibuprofen sodium dihydrate had similar C(max) to ibuprofen lysinate and ibuprofen liquagels and significantly higher Cmax than conventional ibuprofen (p = 0.002). The mean plasma concentration for Ibuprofen sodium dihydrate was significantly higher than for conventional ibuprofen (p = 0.028) 10 minutes post-dose and the t(max) for Ibuprofen sodium dihydrate was reached significantly earlier than for conventional ibuprofen (p = 0.018). All three formulations were bioequivalent according to the acceptable boundaries (90% confidence intervals). No statistically significant difference was observed between the ibuprofen formulations in terms of adverse events and specifically with respect to hemorrhagic scores; 41 (46.0%) adverse events (AEs) occurred after administration of Ibuprofen sodium dihydrate, and 46 (52.9%) after ibuprofen arginate. One occurrence of an invasive ulcer was observed after administration of ibuprofen arginate. Conclusions: The new formulation of Ibuprofen sodium dihydrate dissolves quickly in vitro, has the same extent of absorption as other fast-acting ibuprofen formulations, and is absorbed into plasma more rapidly than conventional ibuprofen. In addition, the present studies suggest that the tolerability and safety profile of Ibuprofen sodium dihydrate is comparable to existing ibuprofen formulations.