Beclometasone dipropionate
目录号 : GC35485
Beclometasone二丙酸盐是糖皮质素激动剂，为beclometasone游离形式的原药。
Cas No.:5534-09-8
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
Beclometasone dipropionate is a potent glucocorticoid agonist; it is a prodrug of the free form, beclometasone. IC50 Value: 0.2 nM (Inhibiting thymidine incorporation) [1]Target: glucocorticoid receptorin vitro: Cortisol and beclomethasone dipropionate were more potent than salbutamol in inhibiting thymidine incorporation with IC50 values of 5 nM and 0.2 nM respectively. Cortisol 100 nM led to a 16.6 +/- 6.5% reduction and beclomethasone dipropionate 3 nM led to a 17.8 +/- 5.8% reduction in cell number [1]. in vivo: Controlled trials involving 497 adults and children demonstrated similar clinical efficacy between nebulized BDP and either nebulized fluticasone propionate or nebulized budesonide. Meta-analyses show that BDP, like other inhaled corticosteroids, has no major influence on patient height, urinary cortisol concentration, or bone metabolism [2]. Beclometasone dipropionate (BDP) 800 microgday(-1) suspension for nebulization and budesonide (BUD) 750 microg day(-1) given by nebulization in a twice-daily regimen, and when used in addition to the usual maintenance therapy, resulted in comparable clinical efficacy across all parameters [3]. Clinical trial: Efficacy and Tolerability of Beclometasone/Formoterol Single Inhaler in Patients With Moderate to Severe Persistent Asthma. Phase 3
[1]. Young PG, Skinner SJ, Black PN. Effects of glucocorticoids and beta-adrenoceptor agonists on the proliferation of airway smooth muscle. Eur J Pharmacol. 1995 Jan 24;273(1-2):137-43. [2]. Nicolini G, Cremonesi G, Melani AS. Inhaled corticosteroid therapy with nebulized beclometasone dipropionate. Pulm Pharmacol Ther. 2010 Jun;23(3):145-55. [3]. Delacourt C, et al. Comparison of the efficacy and safety of nebulized beclometasone dipropionate and budesonide in severe persistent childhood asthma. Respir Med. 2003 Feb;97 Suppl B:S27-33.
| Cas No. | 5534-09-8 | SDF | |
| Canonical SMILES | C[C@@]12[C@](C[C@H](C)[C@]2(OC(CC)=O)C(COC(CC)=O)=O)([H])[C@]3([H])CCC4=CC(C=C[C@]4(C)[C@@]3(Cl)[C@@H](O)C1)=O | ||
| 分子式 | C28H37ClO7 | 分子量 | 521.04 |
| 溶解度 | DMSO: ≥ 100 mg/mL (191.92 mM); Water: < 0.1 mg/mL (insoluble) | 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 | 1.9192 mL | 9.5962 mL | 19.1924 mL |
| 5 mM | 0.3838 mL | 1.9192 mL | 3.8385 mL |
| 10 mM | 0.1919 mL | 0.9596 mL | 1.9192 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。
Inhaled Beclometasone dipropionate/formoterol fumarate extrafine fixed combination for the treatment of asthma
Expert Rev Respir Med 2016;10(5):481-90.PMID:26938578DOI:10.1586/17476348.2016.1161508.
Inhaled therapy is often considered the cornerstone of asthma management and international guidelines recommend combination therapy of inhaled corticosteroids (ICS) and long-acting-beta2-agonists (LABA) in a large proportion of asthmatic patients. The effectiveness of ICS/LABA is dependent on the correct choice of device and proper inhalation technique, this influences drug delivery and distribution along the bronchial tree, including the most peripheral airways. The fixed combination of Beclometasone dipropionate/formoterol fumarate (BDP/FF) is the only extrafine formulation available in pressurized metered dose inhaler (pMDI) and in dry powder inhaler (DPI). Here, we focus on the recent significant advances regarding BDP/FF fixed combination for the treatment of asthma.
High-dose Beclometasone dipropionate/formoterol fumarate in fixed-dose combination for the treatment of asthma
Ther Adv Respir Dis 2016 Oct;10(5):492-502.PMID:27340255DOI:10.1177/1753465816654442.
The high-strength formulation of extrafine Beclometasone dipropionate/formoterol fumarate (BDP/Form) 200/6 µg has been developed to step up inhaled corticosteroid treatment, without increasing the dose of the bronchodilator, in patients who are not controlled with previous therapies. Two clinical studies have evaluated efficacy of high-strength BDP/Form as compared with another high-dose fixed combination and BDP monotherapy. Overall, data show that BDP/Form 200/6 μg improves lung function and has beneficial effects on symptoms, use of rescue medication and asthma control, with an acceptable safety profile comparable with that of high-dose fluticasone propionate/salmeterol. Therefore, BDP/Form 200/6 μg could be considered as an effective and safe treatment for patients with asthma who are not adequately controlled with high doses of inhaled corticosteroid monotherapy or medium doses of inhaled corticosteroid/long-acting β2-agonist combinations.
Inhaled Beclometasone dipropionate/formoterol extra-fine fixed combination in the treatment of asthma: evidence and future perspectives
Expert Opin Pharmacother 2008 Feb;9(3):479-90.PMID:18220498DOI:10.1517/14656566.9.3.479.
Background: Combinations of a long-acting beta(2)-agonist (LABA) and an inhaled corticosteroid (ICS) are effective and safe options in asthma management. Objective: To review available data on a recently developed combination of Beclometasone dipropionate (BDP) and formoterol (F) given via a pressurized metered-dose inhaler. Methods: Published data on preclinical and clinical studies were reviewed. Results/conclusion: In the treatment of asthma, BDP/F was shown to be at least as effective and well-tolerated as other available combinations of ICS and LABA with the advantage of a better cost effectiveness, and more effective in improving asthma control than BDP and formoterol given via separate inhalers. The extra-fine BDP/F combination appears to be a valuable therapeutic option in the management of asthma.
Pharmacokinetic and pharmacodynamic properties of inhaled Beclometasone dipropionate delivered via hydrofluoroalkane-containing devices
Clin Pharmacokinet 2005;44(8):815-36.PMID:16029067DOI:10.2165/00003088-200544080-00004.
Inhaled corticosteroids have a key role in the treatment of asthma and chronic obstructive pulmonary disease. In recent times, Beclometasone dipropionate has been reformulated in pressurised metered dose inhalers (pMDIs), using hydrofluoroalkanes (HFAs) as a propellant. Extensive toxicological testing has shown that HFA-propellants are well tolerated. Among the reformulated beclometasone dipropionate-containing pMDIs, only the characteristics of the two Qvar formulations have been thoroughly explored. Compared to the reference Beclometasone dipropionate formulation, the mass median aerodynamic diameter of the Qvar formulations are substantially smaller (1.1 vs 4.0 microm), whereas that of Modulite averages 2.6 microm. Scintigraphic and pharmacokinetic studies indicate a higher lung deposition for both the Qvar and the Beclazone formulations, compared with reference Beclometasone dipropionate formulation. Since the 2- to 3-fold increase in pulmonary deposition results in a 2.6- to 3-fold difference in relative efficacy for Qvar, half the dose of the reference Beclometasone dipropionate formulation has been currently recommended in adult patients with asthma, a recommendation that is supported by a large number of clinical trials. Conversely, the design of the studies conducted to compare the efficacy of Qvar with fluticasone propionate and budesonide does not allow establishing their equivalence on a milligram per milligram basis. Good studies on the bioequivalence between the reference Beclometasone dipropionate formulation and the Modulite or Beclazone formulations are not available.
The role of oral Beclometasone dipropionate in the treatment of gastrointestinal Graft-versus-Host Disease
Drugs 2009 Jul 9;69(10):1339-50.PMID:19583452DOI:10.2165/00003495-200969100-00004.
Graft-versus-host disease (GVHD) after allogeneic stem-cell transplantation causes significant morbidity and mortality. An important site of GVHD is the gastrointestinal (GI) tract because development of acute GI GVHD is prognostic of overall survival. The standard of care to treat acute GI GVHD is systemic corticosteroids and immunosuppressants; however, the use of these therapies can cause life-threatening opportunistic infections. To limit the adverse effects of systemic immunosuppression, the topically active corticosteroid Beclometasone dipropionate has been investigated in case studies and in randomized placebo-controlled trials for the treatment of acute GI GVHD. In this review, we appraise these studies with Beclometasone dipropionate, and discuss future randomized studies to clarify the role of Beclometasone dipropionate for the treatment and prevention of acute GVHD. At present, more data are required before the addition of Beclometasone dipropionate to systemic corticosteroids for the treatment of acute GVHD can be considered the standard of care.