Hydrocortisone acetate (Hydrocortisone 21-acetate)
(Synonyms: 醋酸氢化可的松) 目录号 : GC33849
A synthetic corticosteroid
Cas No.:50-03-3
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Hydrocortisone acetate is a synthetic corticosteroid.1,2 Topical administration of hydrocortisone acetate (0.1% v/v) reduces corneal haze and hydroxyproline levels without reducing the stromal wound healing response in a rabbit model of photorefractive keratectomy.1 Hydrocortisone acetate enhances and reduces cartilage degradation in a mouse model of air pouch cartilage implantation when injected into the air pouch cavity or into the air pouch lining tissue, respectively.2 Formulations containing hydrocortisone acetate have been used in the treatment of joint inflammation and rheumatoid arthritis.
1.Bilgihan, K., Ozdek, S., Ozo?ul, C., et al.Topical vitamin E and hydrocortisone acetate treatment after photorefractive keratectomyEye (Lond)14(Pt 2)231-237(2000) 2.Sedgwick, A.D., Sin, Y.M., Moore, A.R., et al.Effects of local administration of hydrocortisone on cartilage degradation in vivoAnn. Rheum. Dis.43(3)418-420(1984)
| Cas No. | 50-03-3 | SDF | |
| 别名 | 醋酸氢化可的松 | ||
| Canonical SMILES | C[C@@]12[C@](C(COC(C)=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 | C23H32O6 | 分子量 | 404.5 |
| 溶解度 | DMSO : ≥ 38 mg/mL (93.94 mM) | 储存条件 | Store at -20°C, protect from light |
| 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 | 2.4722 mL | 12.3609 mL | 24.7219 mL |
| 5 mM | 0.4944 mL | 2.4722 mL | 4.9444 mL |
| 10 mM | 0.2472 mL | 1.2361 mL | 2.4722 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。
Development and validation of HPLC-DAD and LC-(ESI)/MS methods for the determination of sulfasalazine, mesalazine and Hydrocortisone 21-acetate in tablets and rectal suppositories: In vitro and ex vivo permeability studies
J Chromatogr B Analyt Technol Biomed Life Sci 2022 May 15;1198:123246.PMID:35405570DOI:10.1016/j.jchromb.2022.123246.
Controlled-release tablets and rectal suppositories of sulfasalazine (SLF) and Hydrocortisone 21-acetate (HA) were prepared as recommended dosage forms for the treatment of acute episodes of ulcerative colitis, in patients who do not respond to monotherapy. A High-Performance Liquid Chromatography (HPLC) Diode-array method with a gradient elution mobile phase was developed to evaluate the production quality of both formulations (assay and dissolution profiles in gastric and intestinal fluids). Method's validation was carried out providing good linearity (r ≥ 0.9995), precision (RSD < 1.53%), recovery (96.9% - 103.7%) and limits of detection (LODSLF = 12 ng/mL, LODHA = 15 ng/mL). Experimental design and Plackett-Burman methodology was constructed to study the robustness of the analysis. In all composite substrates, a freezing lipid precipitation approach was used as purification step. The method was optimized by applying Central Composite design mode. The in-vitro/ex-vivo permeability studies of both formulations were evaluated by a Liquid Chromatography-Electron Spray Ionization Mass Spectrometry (LC-ESI/MS) +/- mode. The analysis of sulfamethazine (internal standard, SLM, m/z 279), HA (m/z 449, [M + HCOO]-), SLF (m/z 399) and its active metabolite mesalazine (MSL, m/z 154) was performed using a C18 column and gradient elution. The validation of the method met the requirements of the International Council for Harmonization (ICH) (r ≥ 0.9997, RSD ≤ 4.62%, Recovery > 95%, LODSLF = 1.28 ng/mL, LODHA = 1.07 ng/mL, LODMSL = 3.16 ng/mL). Based on the results, important conclusions were drawn concerning the role of excipients and SLF metabolism.
UVB photolysis of Hydrocortisone 21-acetate
J Pharm Biomed Anal 2008 Aug 5;47(4-5):771-7.PMID:18423938DOI:10.1016/j.jpba.2008.03.008.
Hydrocortisone 21-acetate (HCA) in methanol solution undergoes photodegradation under UVB light, as monitored by HPLC. Five main photoproducts have been isolated and characterized by means of NMR and mass spectroscopy. One of them derives from a Norrish I photoreaction which cleaves the C17-C20 bond of the steroid yielding the andro-derivative, a second product comes from a Yang-type photorearrangement which links C18 to C20 yielding a cyclobutane adduct. The former photoproduct, in turn, undergoes further photolysis giving rise to various photoproducts, of which three have been characterized. The first is a stereoisomer of the andro-derivative, the others arise from the opening of the five-membered ring. HCA also proved photounstable in the solid state and in a commercial formulation for topical use, thus confirming the requirements of the Pharmacopeias for light protection of this drug. Indeed, experiments on LPS-stimulated THP-1 cells demonstrated the loss of anti-inflammatory activity when HCA was UVB-photodegraded. The radical mechanism involved in HCA photolysis seems also responsible for the in vitro photohemolytic effect and lipid peroxidation induced by HCA in combination with UVB light.
Rheumatoid arthritis; experiences with hydrocortisone (free alcohol) and Hydrocortisone acetate
Calif Med 1952 Jul;77(1):1-6.PMID:12978878doi
Recent experimental evidence suggests that hydrocortisone (Kendall's Compound F) is probably the principal glycogenic steroid secreted by the adrenal cortex and that under conditions of stress it may participate more than cortisone in physiologic reactions. Laboratory studies indicate that hydrocortisone has greater physiologic activity, milligram for milligram, than cortisone and with certain assays its potency is twice as great.Two forms of hydrocortisone, the free alcohol preparation and the acetate, were given systemically to patients with rheumatoid arthritis and were observed to possess significant differences in ability to suppress the disease manifestations. When administered orally in large initial doses, hydrocortisone (free alcohol) appeared to produce greater suppressive effects, milligram for milligram, than either Hydrocortisone acetate or cortisone acetate. Comparisons of potency made by determining maintenance dosage requirements for equivalent degrees of clinical control in the same patients indicated that the effectiveness of hydrocortisone (free alcohol) is more than 50 per cent greater than that of either the free or acetated forms of cortisone and approximately twice as great as that of Hydrocortisone acetate. Certain observations suggested that the greater antirheumatic activity of hydrocortisone (free alcohol) is not accompanied by a correspondingly greater tendency toward endocrine complications. If more extensive future investigations support this observation, hydrocortisone (free alcohol), by producing equally efficient results with smaller doses, may prove superior to cortisone as a therapeutic agent.Intra-articular injections of Hydrocortisone acetate appear to have only a limited place in the management of rheumatoid arthritis but may be used for temporary relief under certain conditions. In preliminary studies by the author it was noted that whereas improvement resulted in 80 per cent of the treated joints, the improvement was graded as pronounced or very pronounced in only one-half of the joints so injected. In almost all instances the benefits derived were quite temporary. Results observed in treatment of osteoarthritic joints by this method were decidedly poorer than in rheumatoid arthritis.
Meralgia paraesthetica
J Indian Med Assoc 1989 Jun;87(6):140-1.PMID:2584731doi
Forty-four patients of meralgia paraesthetica presented with combination of symptoms mainly of numbness with loss of superficial sensation on the anterolateral aspect of a thigh were selected for the study. They responded well to local infiltration of Hydrocortisone acetate and lignocaine hydrochloride which not only helped in diagnosis but also prevented the recurrence of symptoms in majority of cases.
Control of transdermal permeation of Hydrocortisone acetate from hydrophilic and lipophilic formulations
AAPS PharmSciTech 2008;9(3):762-8.PMID:18563577DOI:10.1208/s12249-008-9107-z.
The purpose of this research was the preparation of four formulations containing Hydrocortisone acetate (HCA) for topical application, including two aqueous systems (hydrophilic microemulsion and aqueous gel) and two systems with dominant hydrophobicity (hydrophobic microemulsion and ointment). The formulations were tested for the release and permeation of HCA across an animal membrane. The release of HCA was found comparable for the four systems. The two microemulsions promote permeation across an ex-vivo membrane, examined by means of a Franz cell. Hydrophobic microemulsion guarantees the highest solubility (2,370 microg/ml) and flux (133 microg/cm(2).h) of the drug, since it contains almost 40% Transcutol, a permeation enhancer. Gel and ointment provide lower solubility and flux, being the values, related to the ointment, the lowest ones (562 microg/ml and 0.4 microg/cm(2).h). Experimental results allow the conclusion that gel and ointment can be suitable when it is desirable to minimize absorption of topically applied HCA as to keep the drug restricted to the diseased area and prevent side effects of the systemic presence of HCA.