Prednisolone hemisuccinate
(Synonyms: 泼尼松龙半琥珀酸酯; Prednisolone 21-hemisuccinate) 目录号 : GC36960
Prednisolone半琥珀酸是一种合成的糖皮质激素，是皮质醇的衍生物，用于治疗多种炎症和自身免疫病。
Cas No.:2920-86-7
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Prednisolone hemisuccinate is a synthetic glucocorticoid, a derivative of cortisol, which is used to treat a variety of inflammatory and auto-immune conditions.
| Cas No. | 2920-86-7 | SDF | |
| 别名 | 泼尼松龙半琥珀酸酯; Prednisolone 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(C=C[C@]4(C)[C@@]3([H])[C@@H](O)C2)=O | ||
| 分子式 | C25H32O8 | 分子量 | 460.52 |
| 溶解度 | DMSO: 250 mg/mL (542.86 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。 |
||
| 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.1715 mL | 10.8573 mL | 21.7146 mL |
| 5 mM | 0.4343 mL | 2.1715 mL | 4.3429 mL |
| 10 mM | 0.2171 mL | 1.0857 mL | 2.1715 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。
Pharmacokinetics of prednisolone after high doses of Prednisolone hemisuccinate
Biopharm Drug Dispos 1985 Oct-Dec;6(4):423-32.PMID:4084667DOI:10.1002/bdd.2510060408.
Prednisolone in the form of its hemisuccinate was given intravenously in two different doses (1200 mg and 75 mg). Plasma levels of the ester and prednisolone were measured and pharmacokinetic parameters were calculated. The results indicate a dose-dependency in the pharmacokinetics of both hemisuccinate and the free alcohol. For the high dose 8 per cent of the administered ester was found unchanged in the urine indicating incomplete conversion of the pro-drug. Comparison with previous studies leads to the conclusion that prednisolone shows doubled non-linear pharmacokinetics with higher total body clearance in the medium dose range than in the low and high dose range. Volume of distribution changes accordingly, but overall elimination rate remains remarkably constant. Saliva levels of prednisolone were low and agree reasonably well with calculated plasma concentrations of free, non-protein-bound prednisolone. No Prednisolone hemisuccinate was found in saliva.
[Pharmacokinetics and pharmacodynamics of prednisolone following extremely high dosage as Prednisolone hemisuccinate]
Arzneimittelforschung 1987 Feb;37(2):194-8.PMID:3580023doi
Plasma levels of prednisolone and Prednisolone hemisuccinate of volunteers were measured with HPLC following i.v. injections of 1200 and 75 mg of prednisolone, given as the water-soluble hemisuccinate ester. The hemisuccinate ester is hydrolyzed relatively quickly with a plasma half-life between 18 and 25 min, and the resulting prednisolone has a plasma half-life of 3.5-3.7 h. The dose dependency of the pharmacokinetic parameters indicates a partial saturation of the metabolizing enzymes as consequence of the application of the high dose of prednisolone. In saliva no hemisuccinate could be detected. The prednisolone saliva concentration corresponds with those of non-protein-bound prednisolone in plasma measured at the same time. Only minor quantities of intact ester (1-8%) or intact prednisolone (2-4%) are excreted in urine. Following the application of 1200 mg prednisolone the endogenous cortisol level is partially suppressed only 24 h after the i.v. injection; 48 h later the difference from the basis value is not statistically significant. Leukocytosis and granulocytosis are at maximum 24 h after the injection of the high dose, and after 48 h normal values are observed. Lymphocytes and monocytes fall below normal levels for a longer time after 1200 mg compared to 75 mg, the minimum is between 4 and 8 h. Glucose levels are enhanced dose-dependently. They are normalized even after the extremely high dose at 24 h. Sodium, potassium, calcium, plasma proteins, urea, creatinine, hematocrit and hemoglobin showed no significant differences within 48 h following the injections.
Effect of glycyrrhizin on the pharmacokinetics of prednisolone following low dosage of Prednisolone hemisuccinate
Endocrinol Jpn 1990 Jun;37(3):331-41.PMID:2253583DOI:10.1507/endocrj1954.37.331.
We investigated the pharmacokinetics of prednisolone (PSL) in six healthy men, with or without glycyrrhizin (GL), to confirm whether GL influences the metabolism of PSL in humans. Each subject received an intravenous administration of 0.096 mg/kg of Prednisolone hemisuccinate (PSL-HS, equivalent to 0.075 mg/kg of PSL), with or without 200 mg of GL. Blood samples were taken from a peripheral vein at 5, 10, 15, 30 and 45 min, and 1, 1.5, 2, 3, 4, 6, 8, 10, 12 and 24 h after PSL-HS infusion. The concentration of total PSL in the plasma was analyzed by high-performance liquid chromatography, and the free PSL was measured by an isocolloidosmolar equilibrium dialysis method. The pharmacokinetic parameters of PSL were determined, using noncompartmental analysis. GL was found to increase significantly the concentration of total PSL at 6, 8 h, and of free PSL at 4, 6, and 8 h after PSL-HS infusion. GL was also found to modify the pharmacokinetics of PSL. After the administration of GL, the area under the curve (AUC) increased, total plasma clearance (CL) decreased, and the mean residence time (MRT) was prolonged. However, only those of AUC, CL, and MRT of free PSL were significantly different. The volume of distribution at a steady-state (Vdss) of both total and free PSL showed no evident change. This suggests that GL increases the plasma PSL concentrations by inhibiting the metabolism of PSL and that it potentiates pharmacological effects of PSL.
Histological study of the effects of hycanthone on the frog's ventricle in the presence of a soluble sodium salt of Prednisolone hemisuccinate
Egypt J Bilharz 1976;3(1):101-5.PMID:1029643doi
The histological picture of the ventricle of frog's heart exposed to the action of Hycanthone in Ringer's solution in concentration of 1:1 was compared with that of the ventricle of frog's heart exposed to Ringer's solution devoid of the drug and with that of frog's heart exposed to Ringer's solution containing Hycanthone in concentration of 1:1 in addition to a soluble sodium salt of Prednisolone hemisuccinate in concentration 1:1. It was found that the structure of the ventricle of the heart exposed to the action of Hycanthone in the presence of the soluble sodium salt of Prednisolone hemisuccinate was close in pattern to the structure of the ventricle of the heart exposed to Ringer's solution alone, while the ventricle of the heart exposed to Hycanthone alone in Ringer's solution in concentration of 1:1 was different in that the muscle fibres swollen, the cytoplasm was paler with less marked striations, the nuclei were swollen and paler, the epicardial cells were swollen and the connective tissue pattern was distorted. This denoted that the morphological changes that occurred in response to Hycanthone in the presence of the soluble sodium salt of Prednisolone hemisuccinate was less marked than those which occurred in its absence.
Effect of corticosteroid binding globulin on the pharmacokinetics of prednisolone in rats
Pharm Res 1995 Jun;12(6):902-4.PMID:7667198DOI:10.1023/a:1016225423795.
Purpose: The effect of exogenous corticosteroid binding globulin (CBG) on the pharmacokinetics of intravenous prednisolone was determined in rats to test the "free hormone hypothesis." Methods: A dose of CBG to yield 95% binding with 1000 ng/ml of prednisolone in vitro in rat plasma or saline was administered before dosing 2 mg/kg of Prednisolone hemisuccinate or methylprednisolone intravenously. Drug concentrations in plasma samples were assayed by HPLC. Results: Single administration of CBG decreased apparent prednisolone clearance by 56% (155 to 66 ml/min/kg) and reduced apparent VSS by 35% (4.1 to 2.7 L/kg) (p < 0.001). Methylprednisolone pharmacokinetics, studied as a negative control because the drug does not bind to CBG, did not change. Conclusions: The corticosteroid bound to CBG does not appear to be available for removal by clearance organs.