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Prednisolone Phosphate (sodium salt) Sale

(Synonyms: 泼尼松龙21-磷酸二钠; Prednisolone 21-phosphate disodium) 目录号 : GC44678

A prodrug form of prednisolone

Prednisolone Phosphate (sodium salt) Chemical Structure

Cas No.:125-02-0

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产品描述

Prednisolone disodium phosphate is a synthetic glucocorticoid with anti-inflammatory and immunomodulating properties.Target: Glucocorticoid ReceptorPrednisolone irreversibly binds with glucocorticoid receptors (GR) alpha and beta for which they have a high affinity. Prednisolone can activate and influence biochemical behaviour of most cells. The steroid/receptor complexes dimerise and interact with cellular DNA in the nucleus, binding to steroid-response elements and modifying gene transcription. They induce synthesis of some proteins, and inhibit synthesis of others. Prednisolone exerted a delayed biphasic effect on the resistant CCRF-CEM leukemic cell line, necrotic at low doses and apoptotic at higher doses. At low doses, prednisolone exerted a pre-dominant mitogenic effect despite its induction on total cell death, while at higher doses, prednisolone's mitogenic and cell death effects were counterbalanced [1, 2].

References:
[1]. Lambrou, G.I., et al., Prednisolone exerts late mitogenic and biphasic effects on resistant acute lymphoblastic leukemia cells: Relation to early gene expression. Leuk Res, 2009. 33(12): p. 1684-95.
[2]. http://en.wikipedia.org/wiki/Prednisolone

Chemical Properties

Cas No. 125-02-0 SDF
别名 泼尼松龙21-磷酸二钠; Prednisolone 21-phosphate disodium
Canonical SMILES O=C1C=C[C@@]2(C)C(CC[C@]3([H])[C@]2([H])[C@@H](O)C[C@@]4(C)[C@@]3([H])CC[C@]4(O)C(COP([O-])([O-])=O)=O)=C1.[Na+].[Na+]
分子式 C21H27O8P•2Na 分子量 484.4
溶解度 PBS (pH 7.2): 10 mg/ml,PBS (pH 7.2): 10 mg/ml 储存条件 Store at -20°C
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1 mM 2.0644 mL 10.322 mL 20.6441 mL
5 mM 0.4129 mL 2.0644 mL 4.1288 mL
10 mM 0.2064 mL 1.0322 mL 2.0644 mL
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Research Update

An in vitro comparison of the permeability of prednisolone, prednisolone sodium phosphate, and prednisolone acetate across the NZW rabbit cornea

J Ocul Pharmacol 1992 Summer;8(2):139-50.PMID:1506755DOI:10.1089/jop.1992.8.139.

Controversy and ambiguity in the literature concerning the corneal penetration of prednisolone acetate over Prednisolone Sodium phosphate in NZW rabbits has recently prompted comparative studies using specific chromatographic assays. In vitro, corneal penetration studies were performed using the Ussing Chambers to compare the permeability and flux of both esters and prednisolone at 0.5% using a reversed phase HPLC-UV assay. Chromatograms of samples from the receiver chambers show primarily the presence of prednisolone from both esters; only Prednisolone Phosphate penetrated the cornea intact. Flux measurements were similar for prednisolone and both salt forms in terms of the metabolite prednisolone. Permeability coefficient calculations give the relative comparison: prednisolone acetate greater than prednisolone greater than prednisolone sodium phosphate.

Prednisolone acetate or Prednisolone Phosphate concurrently administered with ciprofloxacin for the therapy of experimental Pseudomonas aeruginosa keratitis

Curr Eye Res 1993 May;12(5):469-73.PMID:8344070DOI:10.3109/02713689309024629.

This study was conducted to determine the therapeutic efficacy of 3.0 mg/ml ciprofloxacin administered concurrently with one of two salts of prednisolone for the treatment of experimental pseudomonal keratitis. Rabbit corneas were injected intrastromally with Pseudomonas aeruginosa ATCC strain 27853. Sixteen hr after injection, rabbits were randomly divided into four treatment groups (3 rabbits, 6 eyes per group): 1) ciprofloxacin plus prednisolone acetate; 2) ciprofloxacin plus Prednisolone Phosphate; 3) ciprofloxacin only; 4) untreated. Signs of inflammation were graded in a masked fashion by slit lamp examination (SLE) and by estimating polymorphonuclear leukocyte (PMN) numbers in corneas 27 hr after injection. SLE scores and PMN numbers were significantly lower (P < 0.02) in eyes receiving either salt of prednisolone plus ciprofloxacin compared to the untreated controls. In contrast, SLE scores and PMN numbers were not significantly different in eyes treated with ciprofloxacin alone, compared to untreated controls (P > 0.13). No viable bacteria were recovered from any eye treated with ciprofloxacin (groups 1, 2, and 3). Ciprofloxacin concentrations in the aqueous humor of eyes in groups 1, 2, and 3 were greater than 15-fold higher than the MIC for P. aeruginosa 27853. These results suggest that either salt of prednisolone, when combined with ciprofloxacin, reduces ocular inflammation without affecting the antimicrobial efficacy of the antibiotic.

2-Methyl-β-cyclodextrin grafted ammonium chitosan: synergistic effects of cyclodextrin host and polymer backbone in the interaction with amphiphilic Prednisolone Phosphate salt as revealed by NMR spectroscopy

Int J Pharm 2020 Sep 25;587:119698.PMID:32736017DOI:10.1016/j.ijpharm.2020.119698.

Reduced molecular weight chitosan was quaternized with 2-chloro-N,N-diethylethylamine to obtain a water soluble derivative (N+-rCh). Methylated-β-cyclodextrin (MCD), with 0.5 molar substitution, was covalently linked to N+-rCh through 1,6-hexamethylene diisocyanate spacer to give the derivatized ammonium chitosan N+-rCh-MCD. To shed light on the role of the cyclodextrin pendant in guiding binding interactions with amphiphilic active ingredients, corticosteroid Prednisolone Phosphate salt (PN) was considered. The deep inclusion of PN into cyclodextrin in PN/MCD model system was pointed out by analysis of 1H NMR complexation shifts, 1D ROESY spectra, and diffusion measurements (DOSY). By using proton selective relaxation rates measurements as investigation tool, the superior affinity of N+-rCh-MCD towards PN was demonstrated in comparison with parent ammonium chitosan N+-rCh.