Hydrocortisone cypionate
(Synonyms: 氢化可的松环戊丙酸酯) 目录号 : GC36268Hydrocortisone cypionate是一种合成的糖皮质激素和皮质类固醇酯。
Cas No.:508-99-6
Sample solution is provided at 25 µL, 10mM.
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Hydrocortisone cypionate is a synthetic glucocorticoid corticosteroid and a corticosteroid ester.
Hydrocortisone (50 nM) shows a dose-dependent down-regulation of GR transcript in hCMEC/D3 cells. Hydrocortisone supplementation of the serum-reduced cell differentiation medium leads to a significant increase in TER across the hCMEC/D3 monolayer[1]. Hydrocortisone-treated Dendritic cells (DCs) show a decreased expression of MHC II molecules, the costimulatory molecule CD86, and the DC-specific marker CD83, as well as a strongly reduced IL-12 secretion. Hydrocortisone-treated DCs inhibit production of IFN-γ but induce an increased release of IL-4 and no change in IL-5[2]. Hydrocortisone reduces postischemic oxidative stress, perfusion pressure, and transudate formation. Hydrocortisone inhibits postischemic shedding of syndecan-1, heparan sulfate, and hyaluronan as is release of histamine from resident mast cells[3].
[1]. F•rster C, et al. Differential effects of hydrocortisone and TNFalpha on tight junction proteins in an in vitro model of the human blood-brain barrier. J Physiol. 2008 Apr 1;586(7):1937-49. [2]. Bellinghausen I, et al. Inhibition of human allergic T-cell responses by IL-10-treated dendritic cells: differences from hydrocortisone-treated dendritic cells. J Allergy Clin Immunol. 2001 Aug;108(2):242-9. [3]. Chappell D, et al. Hydrocortisone preserves the vascular barrier by protecting the endothelial glycocalyx. Anesthesiology. 2007 Nov;107(5):776-84.
Cas No. | 508-99-6 | SDF | |
别名 | 氢化可的松环戊丙酸酯 | ||
Canonical SMILES | C[C@@]1([C@@]2(O)C(COC(CCC3CCCC3)=O)=O)[C@](CC2)([H])[C@@](CCC4=CC5=O)([H])[C@]([C@]4(CC5)C)([H])[C@@H](O)C1 | ||
分子式 | C29H42O6 | 分子量 | 486.64 |
溶解度 | DMSO: 125 mg/mL (256.86 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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1 mg | 5 mg | 10 mg | |
1 mM | 2.0549 mL | 10.2745 mL | 20.5491 mL |
5 mM | 0.411 mL | 2.0549 mL | 4.1098 mL |
10 mM | 0.2055 mL | 1.0275 mL | 2.0549 mL |
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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 | |||
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% DMSO % % Tween 80 % saline | ||||||||||
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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。
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High-performance liquid chromatographic determination of Hydrocortisone cypionate: method development and characterization of chromatographic behavior
J Pharm Sci 1981 Feb;70(2):177-81.PMID:7205224DOI:10.1002/jps.2600700216.
A reversed-phase high-performance liquid chromatographic method for Hydrocortisone cypionate bulk drug and oral solution was developed that avoids the use of a heated column as described in USP XX. A study of the effect of the organic modifier concentration on the capacity factor suggests that mixed partition and adsorption phenomena are responsible for the retention of several steroids when acetonitrile is used in the mobile phase. Evidence is presented that hydrogen bonding of the solute molecule with silane hydroxyl groups may be responsible for the adsorption.
Stability of hydrocortisone oral suspensions prepared from tablets and powder
Ann Pharmacother 1995 Oct;29(10):987-90.PMID:8845559DOI:10.1177/106002809502901005.
Objective: To assess the stability, dosage uniformity, and clinical acceptability of hydrocortisone oral suspensions prepared from tablets and powder. Design: Hydrocortisone 2.5 mg/mL oral suspensions were stored in the dark for 91 days at 5, 25, and 40 degrees C. Dosage uniformity was assessed by repeated sampling of the formulation prepared from tablets at 5 and 25 degrees C. The formulation was clinically evaluated in 2 pediatric patients. Setting: A university pharmacy school and affiliated urban teaching hospital. Participants: A brother (4 y old) and sister (1 y old) with congenital adrenal hyperplasia maintained on a commercially available Hydrocortisone cypionate suspension. Main outcome measures: Samples removed at 5 time points were analyzed for hydrocortisone to assess decomposition over 90 days. Dosage uniformity was evaluated by intra- and interday variability. Palatability was examined in the 2 children and urinary cortisol concentrations were measured in the boy before and 5 days after commencing the formulation prepared from tablets. Results: Decomposition of hydrocortisone was not significant except in the formulation that was prepared from tablets and stored at 40 degrees C. Dosage uniformity gave coefficients of variation less than 4.5%. The formulation was well-tolerated and resulted in satisfactory urinary cortisol concentrations in the boy. Conclusions: The hydrocortisone oral suspensions supply a uniform dose and are chemically stable when stored in the dark at 5 and 25 degrees C for at least 30 days. They provide flexible and convenient dosage forms for pediatric patients.