Flunisolide
(Synonyms: 氟尼缩松) 目录号 : GC31747
A fluorinated corticosteroid receptor agonist
Cas No.:3385-03-3
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Flunisolide is a fluorinated corticosteroid receptor agonist that induces reversible pyloric hyalinization in CD-1 mice following oral administration at a dose of 200 μg/kg per day.1 Formulations containing flunisolide have been used for the treatment of asthma.2
1.McKevitt, T.P., Giffen, P., Woodfine, J.A., et al.Hyalinization of the pyloric stomach in CD-1 mice following oral (dietary) administration of the corticosteroid agonists mometasone furoate, budesonide, and flunisolideToxicol. Pathol.39(6)958-968(2011) 2.O'Callaghan, C., White, J.A., and Kantar, A.Nebulization of corticosteroids to asthmatic children: Large variation in dose inhaledRespirology19(2)276-279(2014)
| Cas No. | 3385-03-3 | SDF | |
| 别名 | 氟尼缩松 | ||
| Canonical SMILES | C[C@@]12[C@@]3(C(CO)=O)[C@@](OC(C)(O3)C)([H])C[C@@]1([H])[C@]4([H])C[C@H](F)C5=CC(C=C[C@]5(C)[C@@]4([H])[C@@H](O)C2)=O | ||
| 分子式 | C24H31FO6 | 分子量 | 434.5 |
| 溶解度 | 30mg/ml in ethanol or DMSO, or DMF | 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 | 2.3015 mL | 11.5075 mL | 23.015 mL |
| 5 mM | 0.4603 mL | 2.3015 mL | 4.603 mL |
| 10 mM | 0.2301 mL | 1.1507 mL | 2.3015 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。
Flunisolide
Although not measured, the amounts of inhaled corticosteroids absorbed into the maternal bloodstream and excreted into breastmilk are probably too small to affect a breastfed infant. Reviewers and an expert panel consider inhaled and oral corticosteroids acceptable to use during breastfeeding.[1][2][3]
Flunisolide for the treatment of asthma
Inhaled corticosteroids (ICSs) are recommended for treatment of persistent asthma. Several ICSs are available and delivered by a variety of devices. After the banning of chlorofluorocarbon (CFC), a formulation of hydrofluoroalkane (HFA)-flunisolide marketed with an in-built spacer has been developed, complying with the request of efficacy and safety for children and adults. It delivers an aerosol with mass median aerodynamic diameter smaller than that of the CFC-formulation (1.2 vs 3.8 m). The extrafine aerosol and the add-on spacer are peculiarities of HFA-flunisolide with respect to the traditional ICSs, assuring larger lung deposition, lower oro-pharyngeal dose and targeting small airways. HFA-flunisolide with the spacer is effective at one-third the dose of CFC-flunisolide delivered without spacer. HFA-flunisolide may be considered an effective alternative to currently available ICSs for asthma management of adult and pediatric patients 6 years of age and older.
Flunisolide hydrofluoroalkane with integrated spacer for treating asthma: an updated review
Flunisolide hydrofluoroalkane (HFA) with integrated spacer is the most recent reformulated inhaled corticosteroid (ICS) for asthma available in the United States. It is the only product that combines a corticosteroid extrafine aerosol with a built-in spacer. The potential clinical benefit of the flunisolide HFA formulation and its integrated spacer for treating persistent asthma was assessed through a comprehensive review of the published literature and data from the past 10 years focusing on (1) flunisolide, the molecule, and the impact of the HFA reformulation; (2) updated information on the anti-inflammatory response to flunisolide HFA, particularly in the distal airways; and (3) the usefulness of an integrated spacer. Flunisolide HFA was found effective and safe in clinical studies and comparable with the chlorofluorocarbon (CFC) formulation, but at about one-third the dose of flunisolide CFC, likely reflecting both the device and the particle size of the reformulated product. Compared with the CFC formulation, the extrafine aerosol and smaller particle size of flunisolide HFA substantially increased pulmonary deposition and decreased oropharyngeal deposition. The integrated spacer further enhanced the pulmonary/oropharyngeal deposition ratio. Examination of lung biopsy specimens indicated a favorable anti-inflammatory response to flunisolide HFA in peripheral airways. Pediatric studies showed no significant effects on growth. The data indicate that flunisolide HFA is a safe and effective maintenance therapy for asthma patients. The integrated spacer may provide an added advantage for patients, especially those who may be more likely to experience adverse effects of ICSs, both local and systemic, including children susceptible to adverse effects on growth.
Evaluation of efficacy and safety of flunisolide hydrofluoroalkane for the treatment of asthma
Background: Inhaled corticosteroids are currently recommended as first-line therapy for the long-term control and management of persistent asthma. Flunisolide hydrofluoroalkane (HFA) is a new formulation of the corticosteroid flunisolide that is delivered by a metered-dose inhaler containing an HFA propellant. HFA replaces the chlorofluorocarbon (CFC) propellant of the previous formulation, producing aerosols of smaller average particle size.
Objective: This article reviews the physical and pharmacologic properties, deposition profile, and potential clinical benefits of flunisolide HFA for the treatment of asthma.
Methods: Data included in this review were found via MEDLINE (search term, flunisolide HFA).
Results: Flunisolide HFA has a mass median aerodynamic diameter (MMAD) of 1.2 microm, smaller than the 3.8 microm MMAD of the CFC formulation. Compared with flunisolide CFC, more of each flunisolide HFA dose reaches the lungs and less is deposited in the oropharynx. In addition, scintigraphic studies have found that the extra-fine particle size of flunisolide HFA gives it better access to small airways. In short- and long-term clinical studies, flunisolide HFA has been found to significantly increase pulmonary function relative to placebo. Although not statistically superior to the previous CFC formulation, flunisolide HFA exhibited small improvements in secondary efficacy measures, such as as-needed albuterol use and asthma symptoms, relative to flunisolide CFC. Furthermore, research suggests that the new HFA formulation has a low risk of systemic corticosteroid effects (eg, hypothalamic-pituitary-adrenal axis suppression, growth inhibition in children). Also, lower levels of oropharyngeal deposition, such as those seen with flunisolide HFA, are associated with lower incidence of local effects (eg, candidiasis).
Conclusion: Flunisolide HFA offers effective asthma control with a high level of tolerability in an extra-fine particle formulation that distributes corticosteroid to all areas of the lung, including small airways.