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Dexamethasone phosphate disodium (Dexamethasone 21-phosphate disodium salt) Sale

(Synonyms: 地塞米松磷酸二钠; Dexamethasone 21-phosphate disodium salt) 目录号 : GC31658

A glucocorticoid

Dexamethasone phosphate disodium (Dexamethasone 21-phosphate disodium salt) Chemical Structure

Cas No.:2392-39-4

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10mM (in 1mL Water)
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实验参考方法

Animal experiment:

Rats: Male Sprague-Dawley rats are used. Dexamethasone-treated rats are injected intraperitoneally once daily with Dexamethasone (1.5 mg/kg body weight) for 5 days and are allowed to feed ad libitum. Control rats receive no treatment and are fed ad libitum. In order to take into account the decrease in food intake induced by Dexamethasone treatment, a third group of pair-fed rats are used. These rats are provided with the same amount of food as Dexamethasone-injected rats and are treated with a daily isovolumic intraperitoneal injection of NaCl (0.9%) for 5 days. After the final injection of Dexamethasone or NaCl, the animals are fasted overnight prior to being killed by decapitation[4].Mice: Female C57Bl/6JBom mice (age 10-12 weeks) are used in all experiments. Dexamethasone is administered as a single injection of 1 or 10 mg/kg. Dexamethasone is dissolved in saline and 400 μL are injected intraperitoneally, either 1 h before or 1 h after LPS exposure. In one experiment, N-acetylcysteine (NAC) (100 and 500 mg/kg) is injected successively every 4-5 h, starting 1 h before challenge (five injections in total). A control group of LPS-exposed animals are injected intraperitoneally with solvent alone (saline). Intratracheal administration is performed by instillation of 100 μL NAC (50, 100 or 500 mg/kg) or Dexamethasone (10 mg/kg) into the lungs of mice anaesthetized with 15 mg/kg Rapinovet (i.v.)[3].

References:

[1]. LaLone CA, et al. Effects of a glucocorticoid receptor agonist, Dexamethasone, on fathead minnow reproduction, growth, and development. Environ Toxicol Chem. 2012 Mar;31(3):611-22.
[2]. Adcock IM, et al. Ligand-induced differentiation of glucocorticoid receptor (GR) trans-repression and transactivation: preferential targetting of NF-kappaB and lack of I-kappaB involvement. Br J Pharmacol. 1999 Jun;127(4):1003-11.
[3]. Rocksén D, et al. Differential anti-inflammatory and anti-oxidative effects of Dexamethasone and N-acetylcysteine in endotoxin-induced lung inflammation. Clin Exp Immunol. 2000 Nov;122(2):249-56.
[4]. Roussel D, et al. Dexamethasone treatment specifically increases the basal proton conductance of rat liver mitochondria. FEBS Lett. 2003 Apr 24;541(1-3):75-9.

产品描述

Dexamethasone phosphate is a glucocorticoid.1 It reduces LPS-induced production of RANTES, TGF-β1, and nitric oxide (NO) in BV-2 microglia when used at concentrations ranging from 1 to 4 ?M. Dexamethasone phosphate reverses LPS-induced decreases in IL-10 levels in, and inhibits LPS-induced migration of, BV-2 microglia when used at a concentration of 4 ?M. In vivo, dexamethasone phosphate decreases motor activity and reduces adrenal weight and plasma corticosterone levels in rats when administered in the drinking water at a concentration of 5 ?g/ml.2 Dexamethasone phosphate (1.6 mg/kg per day) reduces joint swelling in a rat model of collagen-induced arthritis when administered for a minimum of seven days.3 It also reduces pruritis and the clinical lesion score in cats with hypersensitivity dermatitis.4 Formulations containing dexamethasone phosphate have been used in the treatment of various inflammatory diseases, arthritis, and endocrine disorders.

1.Hui, B., Yao, X., Zhang, L., et al.Dexamethasone sodium phosphate attenuates lipopolysaccharide-induced neuroinflammation in microglia BV2 cellsNaunyn Schmiedebergs Arch. Pharmacol.393(9)1761-1768(2020) 2.Katz, R.J., and Carroll, B.J.Endocrine control of psychomotor activity in the rat: Effects of chronic dexamethasone upon general activityPhysiol. Behav.20(1)25-30(1978) 3.Rauchhaus, U., Schwaiger, F.W., and Panzner, S.Separating therapeutic efficacy from glucocorticoid side-effects in rodent arthritis using novel, liposomal delivery of dexamethasone phosphate: Long-term suppression of arthritis facilitates interval treatmentArthritis Res. Ther.11(6)R190(2009) 4.McClintock, D., Austel, M., Gogal, R.M., Jr., et al.Oral dexamethasone sodium phosphate solution significantly reduces pruritus and clinical lesions in feline hypersensitivity dermatitis: An open-label studyVet. Dermatol.32(5)497-e137(2021)

Chemical Properties

Cas No. 2392-39-4 SDF
别名 地塞米松磷酸二钠; Dexamethasone 21-phosphate disodium salt
Canonical SMILES O=C1C=C[C@@]2(C)C(CC[C@]3([H])[C@]2(F)[C@@H](O)C[C@@]4(C)[C@@]3([H])C[C@@H](C)[C@]4(O)C(COP([O-])([O-])=O)=O)=C1.[Na+].[Na+]
分子式 C22H28FNa2O8P 分子量 516.4
溶解度 Water : ≥ 106.67 mg/mL (206.56 mM) 储存条件 Store at -20°C,protect from light
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Research Update

The effect of intense, short-term topical dexamethasone disodium phosphate eyedrops on blood glucose level in diabetic patients

Aim: To evaluate the influence of an intensive course of topical (ophthalmic drops) steroid (dexamethasone disodium phosphate) application on blood glucose levels in diabetic patients. Methods: Fifty-five diabetic (type 2) patients were randomly assigned to receive either corticosteroid (study group: 30 patients, 1 drop of 0.1% dexamethasone disodium phosphate) or balanced salt solution (BSS; control group: 25 patients) eyedrops, every 2 h for 7 days (8 drops/day). Blood glucose monitoring (venous blood sample) was performed at the same time every day (10:00 a.m.). Results: During the study no side effects (such as hypoglycemic/hyperglycemic crises) were observed in either study or control group. No statistically significant alterations in blood glucose levels were found (p = 0.19, paired t test) in either group. In the corticosteroid group, when we separately examined patients with controlled diabetes mellitus (initial glucose level <or=135 mg/dl), a statistically significant increase in blood glucose levels was found at the start of dexamethasone treatment (p = 0.003), but which returned to the pretreatment levels after discontinuation of dexamethasone drops. In contrast, similar results were not found for patients with uncontrolled diabetes mellitus (initial glucose level >or=135 mg/dl), while for control patients we did not find any statistically significant differences in any group. Conclusions: Intensive application of topical corticosteroids (drops) for a short period of time (7 days) seems to statistically raise the blood glucose levels in patients with controlled diabetes mellitus, which, however, return to pretreatment levels after discontinuation of eyedrops without any side effects.

Thymus and meat physicochemical measurements to discriminate calves treated with anabolic and therapeutic doses of dexamethasone

To preserve the Europe consumers' health, the use of glucocorticoids as growth promoters is prohibited in cattle fattening. In 2008, the Italian Ministry of Health associated to the official control a national monitoring plan based on the histological thymus analysis to identify animals illegally treated with corticosteroids. However, since corticosteroids are authorized and widely used for therapeutic purposes, it is necessary to verify whether the thymus histological test and some physicochemical traits in meat are able to discriminate doped calves from dexamethasone therapeutic treated ones. The aims of this study were (i) to establish whether the therapeutic and illicit corticosteroid treatments of calves could be differentiated through histological evaluation of thymus and by physicochemical meat traits; (ii) to identify a restricted number of physicochemical traits that could differentiate dexamethasone treated from untreated calves. Three groups of 15 calves each were included in this study: group dexamethasone therapeutic treatment treated with dexamethasone 21-phosphate disodium salt at a therapeutic dose (2 mg/kg of live weight for three consecutive days); group dexamethasone anabolic treatment orally treated with dexamethasone 21-phosphate disodium salt according to a presumed anabolic protocol (0.4 mg/day per animal for 20 days); group placebo control treated with a placebo served as control. Results demonstrated that groups could be easily discriminated by thymus microscopy as well as by two meat markers, namely, cooking loss and shear firmness or Warner-Bratzler shear force. The combination of thymus microscopic features and meat physicochemical traits could be used as a practical, economic and accurate screening strategy to discriminate between meat from illegally and therapeutically treated calves. This new reliable and simple tool could contribute to identify animals treated with dexamethasone in those countries where glucocorticoids are illegally used as growth promoters. More in general, this system could be included in the framework of official controls, and applied to verify suppliers' reliability by the meat industry.

Supercritical impregnation and optical characterization of loaded foldable intraocular lenses using supercritical fluids

Purpose: To prepare drug-loaded intraocular lenses (IOLs) used to combine cataract surgery with postoperative complication treatment through supercritical impregnation while preserving their optical properties.
Setting: Aix-Marseille Université, CNRS, Centrale Marseille, Laboratoire de Mécanique, Modélisation & Procédés Propres, Marseille, France, and He University Eye Hospital, Liaoning Province, China.
Design: Experimental study.
Methods: Supercritical impregnations of commercial foldable IOLs used in cataract surgery with ciprofloxacin (an antibiotic) and dexamethasone 21-phosphate disodium salt (an antiinflammatory drug) were performed in a noncontinuous mode. Impregnation amounts were determined through drug-release kinetic studies. The optical characterizations of IOLs were determined by evaluating the dioptric power and the imaging quality by determining the modulating transfer function (MTF) at a specified spatial frequency according to the International Organization for Standardization (ISO 11979-2:2014).
Results: Transparent IOLs presenting an effective impregnation were obtained with a prolonged drug delivery during approximately 10 days. Optical characterizations (dioptric powers and MTF values) show preserved optical properties after supercritical treatment/impregnation.
Conclusion: Supercritical treatments/impregnations do not damage the optical properties of IOLs and are therefore adequate for the preparation of delivery devices used for cataract surgery.

Mucoadhesivity and release properties of quaternary ammonium-chitosan conjugates and their nanoparticulate supramolecular aggregates: an NMR investigation

Selective relaxation rate measurements effectively proved the affinity of dexamethasone 21-phosphate disodium salt for quaternary ammonium-chitosan conjugates, their thiolated derivatives and the corresponding nanostructured aggregates. Affinity was also probed by dynamic dialysis. The release profile of dexamethasone loaded nanoparticles was defined by quantitative NMR and interrupted dialysis experiments, and mucoadhesivity of empty nanoparticles was effectively probed by selective relaxation rate measurements.

[Quantitative interpretation of dexamethasone pharmacokinetics in human inner ear perilymph using computer simulations]

Objective: To study the dexamethasone pharmacokinetics of human inner ear perilymph under different drug administration using computer simulations.
Method: The dexamethasone pharmacokinetics in guinea pigs inner ear perilymph under an intratympanic application with high-performance liquid chromatography. Dexamethasone pharmacokinetics in the guinea pigs cochlear fluid were simulated with a computer model, the Washington University Cochlear Fluids Simulator, version 1.6 and the best Simulations parameters to the experimental data could be obtain. With best Simulations parameters based on the experimental data, seven kinds application protocols were designed for human inner ear perilymph.
Result: After an intratympanic application dose of 0.5% dexamethasone 150 ml in guinea pigs, the T(1/2K) was (2.918 +/- 0.089) h, and Cmax was (231.25 +/- 6.89) microg/L. The best Simulations parameters were that concentration of the dexamethasone 21-Phosphate disodium salt was 0.5% and the formula weight was 516, as well as drug diffusion coefficient was 0.6939 x 10(-5) cm2/s and round window permeability was 2.2 x 10(-11) cm/s while drug clearance half time was 175 minutes and scala tympaniscala vestibuli communication was 45 minutes. After an intratympanic application dose of 0.5% dexamethasone 500 mL, which the applied drug stayed in contact with the round window membrane for 15, 30, 60 and 120 minutes, the Cmax was 32.8, 64.3, 122.6 and 203.3 microg/L and the AUC was 116.5, 229.1, 423.6 and 759.2 microg/(h x L), respectively. After an intratympanic application dose of 0.5%, 1%, 2% and 4% dexamethasone 500 ml, which the applied drug stayed in contact with the round window membrane for 30 minutes respectively, the Cmax was 64.3, 127.3, 255.4 and 575.6 microg/L respectively and the AUC was 229.1, 462.8, 920.59 and 1525.2 microg/(h x L), respectively.
Conclusion: The dexamethasone pharmacokinetics in human inner ear perilymph by computer simulations was reported. As the time contact with the round window membrane increased, the inner ear perilymph concentration of dexamethasone increased. As the concentration of dexamethasone increased, the inner ear perilymph concentration of drug increased.