Hydrocortisone hemisuccinate
(Synonyms: 氢化可的松琥珀酸酯,Hydrocortisone 21-hemisuccinate) 目录号 : GC60914
Hydrocortisone hemisuccinate (A-hydrocort, Hydrocortisone 21-hemisuccinate), a physiological glucocorticoid with anti-inflammatory properties, is an inhibitor of proinflammatory cytokine with IC50 of 6.7 μM and 21.4 μM for Interleukin-6 (IL-6) and IL-3, respectively.
Cas No.:2203-97-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
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- Purity: >98.00%
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- SDS (Safety Data Sheet)
- Datasheet
Hydrocortisone hemisuccinate (A-hydrocort, Hydrocortisone 21-hemisuccinate), a physiological glucocorticoid with anti-inflammatory properties, is an inhibitor of proinflammatory cytokine with IC50 of 6.7 μM and 21.4 μM for Interleukin-6 (IL-6) and IL-3, respectively.
[1] B S Kang, et al. Biol Pharm Bull. 2001 Jun;24(6):701-3. [2] E Langhoff, et al. Int J Immunopharmacol. 1987;9(4):469-73.
| Cas No. | 2203-97-6 | SDF | |
| 别名 | 氢化可的松琥珀酸酯,Hydrocortisone 21-hemisuccinate | ||
| Canonical SMILES | C[C@@]12[C@](C(COC(CCC(O)=O)=O)=O)(O)CC[C@@]1([H])[C@]3([H])CCC4=CC(CC[C@]4(C)[C@@]3([H])[C@@H](O)C2)=O | ||
| 分子式 | C25H34O8 | 分子量 | 462.53 |
| 溶解度 | DMSO: 250 mg/mL (540.51 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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| 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 | 2.162 mL | 10.8101 mL | 21.6202 mL |
| 5 mM | 0.4324 mL | 2.162 mL | 4.324 mL |
| 10 mM | 0.2162 mL | 1.081 mL | 2.162 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。
Effect of early low-dose hydrocortisone on survival without bronchopulmonary dysplasia in extremely preterm infants (PREMILOC): a double-blind, placebo-controlled, multicentre, randomised trial
Lancet 2016 Apr 30;387(10030):1827-36.PMID:26916176DOI:10.1016/S0140-6736(16)00202-6.
Background: Bronchopulmonary dysplasia, a major complication of extreme prematurity, has few treatment options. Postnatal steroid use is controversial, but low-dose hydrocortisone might prevent the harmful effects of inflammation on the developing lung. In this study, we aimed to assess whether low-dose hydrocortisone improved survival without bronchopulmonary dysplasia in extremely preterm infants. Methods: In this double-blind, placebo-controlled, randomised trial done at 21 French tertiary-care neonatal intensive care units (NICUs), we randomly assigned (1:1), via a secure study website, extremely preterm infants inborn (born in a maternity ward at the same site as the NICU) at less than 28 weeks of gestation to receive either intravenous low-dose hydrocortisone or placebo during the first 10 postnatal days. Infants randomly assigned to the hydrocortisone group received 1 mg/kg of Hydrocortisone hemisuccinate per day divided into two doses per day for 7 days, followed by one dose of 0·5 mg/kg per day for 3 days. Randomisation was stratified by gestational age and all infants were enrolled by 24 h after birth. Study investigators, parents, and patients were masked to treatment allocation. The primary outcome was survival without bronchopulmonary dysplasia at 36 weeks of postmenstrual age. We used a sequential analytical design, based on intention to treat, to avoid prolonging the trial after either efficacy or futility had been established. This trial is registered with ClinicalTrial.gov, number NCT00623740. Findings: 1072 neonates were screened between May 25, 2008, and Jan 31, 2014, of which 523 were randomly assigned (256 hydrocortisone, 267 placebo). 255 infants on hydrocortisone and 266 on placebo were included in analyses after parents withdrew consent for one child in each group. Of the 255 infants assigned to hydrocortisone, 153 (60%) survived without bronchopulmonary dysplasia, compared with 136 (51%) of 266 infants assigned to placebo (odds ratio [OR] adjusted for gestational age group and interim analyses 1·48, 95% CI 1·02-2·16, p=0·04). The number of patients needed to treat to gain one bronchopulmonary dysplasia-free survival was 12 (95% CI 6-200). Sepsis rate was not significantly different in the study population as a whole, but subgroup analyses showed a higher rate only in infants born at 24-25 weeks gestational age who were treated with hydrocortisone (30 [40%] of 83 vs 21 [23%] of 90 infants; sub-hazard ratio 1·87, 95% CI 1·09-3·21, p=0·02). Other potential adverse events, including notably gastrointestinal perforation, did not differ significantly between groups. Interpretation: In extremely preterm infants, the rate of survival without bronchopulmonary dysplasia at 36 weeks of postmenstrual age was significantly increased by prophylactic low-dose hydrocortisone. This strategy, based on a physiological rationale, could lead to substantial improvements in the management of the most premature neonates. Funding: Assistance Publique-Hôpitaux de Paris.
Impact of Hydrocortisone hemisuccinate use on outcome of severe scorpion-envenomed adult patients
Am J Ther 2014 Nov-Dec;21(6):e181-8.PMID:23584312DOI:10.1097/MJT.0b013e3182583bbc.
The aim of this study is to analyze if the infusion of Hydrocortisone hemisuccinate improve outcome in severe scorpion-envenomated adult patients admitted to intensive care unit (ICU). Pairwise retrospective case-control study with 1:1 matching was designed. Patients were defined as cases when they received Hydrocortisone hemisuccinate (as alone steroids) during hospitalization and as controls when they did not received any steroids. Patients were matched according to age, severity factors at admission represented by the presence of pulmonary edema and grades of severity of scorpion envenomation, and scorpion antivenom administration. Eighty-four patients were included as follows: 42 patients in the cases group and 42 patients in the control group. The mean age (±SD) was 40±21 years, ranging from 16 to 90 years. Moreover, 67 (80%) patients have a systemic inflammatory response syndrome on ICU admission. The comparison between cases group and control group showed that age is not significantly different. There were the same proportions of patients with pulmonary edema in 2 groups. Moreover, 23 (54%) patients in case group and 23 (54%) in the control group received scorpion antivenom (P>0.05). The mean temperature on admission was also not significantly different. The presence of systemic inflammatory response syndrome was again not significantly different between 2 groups. The comparison of outcome of the 2 groups showed that the use of mechanical ventilation and its duration, the ICU stay length, and ICU mortality was not significantly different between the 2 groups. Although our study has some limitations, it confirms that the use of Hydrocortisone hemisuccinate in severe scorpion-envenomed patients did not improve their outcome.
High-dose Hydrocortisone hemisuccinate in scorpion envenomation
Ann Emerg Med 1997 Jul;30(1):23-7.PMID:9209220DOI:10.1016/s0196-0644(97)70105-7.
Study objective: Scorpion envenomation is a common life-threatening hazard in tropical and subtropical countries. Standard treatment is not clearly defined. Many therapies, such as steroids, are prescribed without experimental justification. We sought to assess the efficacy of systematic administration of intravenous Hydrocortisone hemisuccinate (50 mg/kg) in scorpion envenomation. Methods: Six hundred consecutive envenomated patients older than 10 years who presented to the ED of a nonteaching secondary hospital in an area of Tunisia endemic for scorpion envenomation were randomly assigned to receive Hydrocortisone hemisuccinate 50 mg/kg (n = 305) or placebo (n = 295) in addition to standard medical care. Patients in the two groups had similar clinical characteristics on initial clinical evaluation. Each was categorized as grade 1 (absence of systemic symptoms) or grade 2 (systemic symptoms of scorpion envenomation). Patients were treated in the ED for up to 4 hours or in the ICU, depending on clinical severity. Steroid and placebo groups were compared according to mortality rate, change of severity grade 4 hours after presentation and treatment, and duration of hospital stay. Results: Distribution of patients with respect to severity grade was similar in the two groups at the 4-hour clinical evaluation. We detected no significant difference at the time of discharge between steroid-and placebo-treated patients with respect to mortality (one patient in each group) or duration of hospital stay. Extra costs incurred through steroid administration totaled US $989,000. Conclusion: Our findings do not support the use of intravenous high-dose steroids in scorpion-envenomated patients. The discontinuation of this practice would reduce costs substantially.
High-performance liquid chromatographic determination of hydrocortisone and methylprednisolone and their hemisuccinate esters in human serum
J Chromatogr 1979 Oct 11;164(2):129-37.PMID:541404DOI:10.1016/s0378-4347(00)81182-2.
A high-performance liquid chromatographic method is described for the simultaneous determination of methylprednisolone (MP) and methylprednisolone hemisuccinate (MPHS), or hydrocortisone (HC) and Hydrocortisone hemisuccinate (HCHS) in human serum. Reversed-phase liquid chromatography was performed on a microparticulate C18 column (Spherisorb, 5 micron) using a mobile phase of 2% glacial acetic acid, 30--35% acetonitrile, 70--65% water with ultraviolet detection (254 nm). The method uses 17 alpha-hydroxyprogesterone as the internal standard for the determination of methylprednisolone and its hemisuccinate ester, or 11-deoxy-17-hydroxycorticosterone as the internal standard for the determination of hydrocortisone and its hemisuccinate ester. The sensitivity is 0.03 microgram/ml for HC, 0.07 microgram/ml for MP, 0.04 microgram/ml for MPHS, and 0.10 microgram/ml for HCHS, with a detection limit of 0.02 microgram/ml for all four steroids. Calibration curves are linear up to 3 micrograms/ml for MP or MPHS (as equivalent MP) and up to 4 micrograms/ml for HC and 7 micrograms/ml (as equivalent HC) for HCHS. The pooled relative standard deviation for replicate for each steroid is less than 7%. Plasma concentration--time curves are reported for MP and MPHS or HC and HCHS of two human subjects following intramuscular administration of 125 mg of methylprednisolone sodium succinate for injection, U.S.P., or 250 mg of hydrocortisone sodium succinate for injection, U.S.P.
Comparison of absorption of cortisone acetate and Hydrocortisone hemisuccinate
J Clin Endocrinol Metab 1978 Nov;47(5):1137-40.PMID:233690DOI:10.1210/jcem-47-5-1137.
In four patients who required maintenance glucocorticoid therapy after bilateral adrenalectomy for Cushing's disease, we compared the effects of im injection and oral ingestion of cortisone acetate and Hydrocortisone hemisuccinate. By the former route of administration, cortisone acetate was not effective in elevating plasma cortisol levels or in suppressing plasma adrenocorticotropin, although hydrocortisone was. When given by mouth, no significant difference was found between the two steroids. Therefore, in the treatment of acute adrenal insufficiency or in the maintenance of patients with chronic adrenal insufficiency and in their preparation for surgery or other stressful situations, we advise against im injection of cortisone acetate. Oral ingestion, however, is appropriate for maintenance.