本研究评估了体内注射泼尼松龙对大肠杆菌脂多糖内毒素 (LPS) 引起的血浆 RNI 和中性粒细胞 NOS II mRNA 增加以及大鼠 RNI 生成的影响。我们发现，在体内注射亚致死剂量 0.5 mg/kg 静脉注射后 2 小时内，LPS 迅速诱导大鼠中性粒细胞 NOS II mRNA 和 RNI（NO2- 和 NO3- 阴离子）生成。在注射 LPS 前 15 分钟给予药理剂量的泼尼松龙（50 微克/千克，肌肉注射）可减弱中性粒细胞 NO2- 和 NO3- 的生成，并抑制 LPS 刺激的 NOS II mRNA。3-氨基，1,2,4-三嗪可抑制 NO2- 和 NO3- 的生成，但不影响 NOS II 的基因表达。这些数据表明，LPS 可快速诱导 NOS II 的功能性基因表达，而泼尼松龙则通过抑制其 mRNA 转录来阻止 NOS II 活性的诱导。[1]

短期服用大剂量皮质类固醇后，膈肌会萎缩和无力。本研究调查了长期服用中等剂量氟化和非氟化类固醇对大鼠膈肌收缩特性和组织病理学的影响。60 只大鼠每天接受生理盐水、1.0 mg/kg 曲安奈德或 1.25 或 5 mg/kg 肌肉注射 泼尼松龙，持续 4 周。对照组和两个 泼尼松龙 组的呼吸和外周肌肉质量增加相似，而曲安奈德导致严重的肌肉萎缩。对照组的最大强直张力平均为 2.23 +/- 0.54 kg/cm2 (SD)。 5 mg/kg 泼尼松龙组膈肌束数量增加，产生的最大强直张力小于 2.0 kg/cm2（P < 0.05）。此外，该组在力-频率方案期间的疲劳性最明显（P < 0.05）。相反，曲安西龙导致半松弛时间延长和力-频率曲线左移（P < 0.05）。对膈肌的组织学检查显示对照组和 1.25 mg/kg 泼尼松龙组的膈肌模式正常。然而，5 mg/kg 泼尼松龙组发现了肌源性变化，曲安西龙组更明显。后者发现了选择性 IIb 型纤维萎缩，但在泼尼松龙组没有发现。总之，曲安奈德诱导 IIb 型纤维萎缩，导致呼吸肌肌力减弱和力频曲线左移。相比之下，5 mg/kg 泼尼松龙 导致膈肌收缩特性和组织学变化改变，但不导致纤维萎缩。[2]

Absorption, Distribution and Excretion
Prednisolone acetate oral suspension given at a dose equivalent to 15mg prednisolone has a Cmax of 321.1ng/hr, a Tmaxof 1-2 hours, and an AUC of 1999.4ng\*hr/mL. The absorption pharmacokinetics of prednisolone acetate are not significantly different from a comparable dose of prednisolone.
Prednisolone acetate is predominantly excreted in the urine.
The volume of distribution of the active metabolite, prednisolone, is 0.22/0.7L/kg.
Data regarding the clearance of prednisolone acetate is not readily available.

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Metabolism / Metabolites
Prednisolone acetate undergoes ester hydrolysis to [prednisolone]. After this step, the drug undergoes the normal metabolism of prednisolone. Prednisolone can be reversibly metabolized to [prednisone] which is then metabolized to 17α,21-dihydroxy-pregnan-1,4,6-trien-3,11,30-trione (M-XVII), 20α-dihydro-prednisone (M-V), 6βhydroxy-prednisone (M-XII), 6α-hydroxy-prednisone (M-XIII), or 20β-dihydro-prednisone (M-IV). 20β-dihydro-prednisone is metabolized to 17α,20ξ,21-trihydroxy-5ξ-pregn-1-en-3,11-dione(M-XVIII). Prednisolone is metabolized to Δ6-prednisolone (M-XI), 20α-dihydro-prednisolone (M-III), 20β-dihydro-prednisolone (M-II), 6αhydroxy-prednisolone (M-VII), or 6βhydroxy-prednisolone(M-VI). 6αhydroxy-prednisolone is metabolized to 6α,11β,17α,20β,21-pentahydroxypregnan-1,4-diene-3-one (M-X). 6βhydroxy-prednisolone is metabolized to 6β,11β,17α,20β,21-pentahydroxypregnan-1,4-diene-3-one (M-VIII), 6β,11β,17α,20α,21-pentahydroxypregnan-1,4-diene-3-one (M-IX), and 6β,11β,17α,21-tetrahydroxy-5ξ-pregn-1-en-3,20-dione (M-XIV). MVIII is metabolized to 6β,11β,17α,20β,21-pentahydroxy-5ξ-pregn-1-en-3-one (M-XV) and then to MXIV, while MIX is metabolized to 6β,11β,17α,20α,21-pentahydroxy-5ξ-pregn-1-en-3-one (M-XVI) and then to MXIV. These metabolites and their glucuronide conjugates are excreted predominantly in the urine.

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Biological Half-Life
Oral prednisolone acetate has a plasma half life of 2-3 hours.

Protein Binding
The active metabolite, prednisolone, is 70-90% protein bound in plasma.

:Proc Soc Exp Biol Med.1994 Mar;205(3):220-9;J Clin Invest.1993 Sep;92(3):1534-42.

Prednisolone acetate is a corticosteroid hormone.
Prednisolone acetate is a [prednisolone] molecule bound to an acetate functional group by an ester bond. Prednisolone acetate was granted FDA approval in 1955.
Prednisolone acetate has been reported in Rehmannia glutinosa with data available.
Prednisolone Acetate is the acetate salt form of prednisolone, a synthetic glucocorticoid with anti-inflammatory and immunomodulating properties. As a glucocorticoid receptor agonist, prednisolone acetate binds to specific intracellular glucocorticoid receptors, and causes the ligand-receptor complex to be translocated to the nucleus where it initiates the transcription of glucocorticoid-responsive genes such as various cytokines and lipocortins. Lipocortins inhibit phospholipase A2, thereby blocking the release of arachidonic acid from membrane phospholipids and preventing the synthesis of prostaglandins and leukotrienes, both potent mediators of inflammation. This agent also decreases the number of circulating lymphocytes, induces cell differentiation, and stimulates apoptosis in sensitive tumor cell populations.
See also: Prednisolone (has active moiety); Prednisolone acetate; sulfacetamide sodium (component of); Neomycin Sulfate; Prednisolone Acetate (component of) ... View More ...

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Drug Indication
Prednisolone acetate is indicated as an anti-inflammatory or immunosuppressive agent for allergic, dermatologic, gastrointestinal, hematologic, ophthalmologic, nervous system, renal, respiratory, rheumatologic, or infectious conditions. Prednisolone acetate is also indicated in organ transplant patients, as well as endocrine or neoplastic conditions.

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Mechanism of Action
The short term effects of corticosteroids are decreased vasodilation and permeability of capillaries, as well as decreased leukocyte migration to sites of inflammation. Corticosteroids binding to the glucocorticoid receptor mediates changes in gene expression that lead to multiple downstream effects over hours to days. Glucocorticoids inhibit neutrophil apoptosis and demargination; they inhibit phospholipase A2, which decreases the formation of arachidonic acid derivatives; they inhibit NF-Kappa B and other inflammatory transcription factors; they promote anti-inflammatory genes like interleukin-10. Lower doses of corticosteroids provide an anti-inflammatory effect, while higher doses are immunosuppressive. High doses of glucocorticoids for an extended period bind to the mineralocorticoid receptor, raising sodium levels and decreasing potassium levels.

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Pharmacodynamics
Corticosteroids bind to the glucocorticoid receptor, inhibiting pro-inflammatory signals, and promoting anti-inflammatory signals. Prednisolone acetate has a short duration of action as the half life is 2-3 hours. Corticosteroids have a wide therapeutic window as patients make require doses that are multiples of what the body naturally produces. Patients taking corticosteroids should be counselled regarding the risk of hypothalamic-pituitary-adrenal axis suppression and increased susceptibility to infections.

C23H30O6

402.48

402.204

52-21-1

Prednisolone;50-24-8;Prednisolone disodium phosphate;125-02-0;Prednisolone hemisuccinate;2920-86-7;Prednisolone acetate-d8

5834

White to off-white solid powder

1.3±0.1 g/cm3

579.8±50.0 °C at 760 mmHg

240-244 °C

198.4±23.6 °C

0.0±3.7 mmHg at 25°C

1.587

2.58

100.9

2

6

4

29

827

7

CC(=O)OCC(=O)[C@]1(CC[C@@H]2[C@@]1(C[C@@H]([C@H]3[C@H]2CCC4=CC(=O)C=C[C@]34C)O)C)O

LRJOMUJRLNCICJ-JZYPGELDSA-N

InChI=1S/C23H30O6/c1-13(24)29-12-19(27)23(28)9-7-17-16-5-4-14-10-15(25)6-8-21(14,2)20(16)18(26)11-22(17,23)3/h6,8,10,16-18,20,26,28H,4-5,7,9,11-12H2,1-3H3/t16-,17-,18-,20+,21-,22-,23-/m0/s1

[2-[(8S,9S,10R,11S,13S,14S,17R)-11,17-dihydroxy-10,13-dimethyl-3-oxo-7,8,9,11,12,14,15,16-octahydro-6H-cyclopenta[a]phenanthren-17-yl]-2-oxoethyl] acetate

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

配方 1 中的溶解度: ≥ 3 mg/mL (7.45 mM) (饱和度未知) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将100 μL 30.0 mg/mL 澄清的 DMSO 储备液加入到400 μL PEG300中，混匀；再向上述溶液中加入50 μL Tween-80，混匀；然后加入450 μL 生理盐水定容至1 mL。
*生理盐水的制备：将 0.9 g 氯化钠溶解在 100 mL ddH₂O中，得到澄清溶液。

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配方 2 中的溶解度: ≥ 3 mg/mL (7.45 mM) (饱和度未知) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 30.0 mg/mL澄清DMSO储备液加入900 μL 20% SBE-β-CD生理盐水溶液中，混匀。
*20% SBE-β-CD 生理盐水溶液的制备（4°C，1 周）：将 2 g SBE-β-CD 溶解于 10 mL 生理盐水中，得到澄清溶液。

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配方 3 中的溶解度: ≥ 3 mg/mL (7.45 mM) (饱和度未知) in 10% DMSO + 90% Corn Oil (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 30.0 mg/mL 澄清 DMSO 储备液加入到 900 μL 玉米油中并混合均匀。

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配方 4 中的溶解度: 20 mg/mL (49.69 mM) in 50% PEG300 50% Saline (这些助溶剂从左到右依次添加，逐一添加), 悬浊液; 超声助溶。
*生理盐水的制备：将 0.9 g 氯化钠溶解在 100 mL ddH₂O中，得到澄清溶液。

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请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。