Beclometasone Dipropionate

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Chemical Structure| 5534-09-8 同义名 : 二丙酸倍氯米松 ;Beclomethasone dipropionate
CAS号 : 5534-09-8
货号 : A739014
分子式 : C28H37ClO7
纯度 : 98%
分子量 : 521.04
MDL号 : MFCD00135613
存储条件：

Pure form Sealed in dry, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(201.52 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
生物活性
描述 Betamethasone dipropionate, the prodrug of Betamethasone, is an orally active and potent glucocorticoid with anti-inflammatory and immunosuppressive activity. Betamethasone appears to be an effective inhibitor of LPS-induced inflammation and MMP release. When mice were pretreated with betamethasone (5 mg/kg, po), MMP2 and MMP9 activities, TNF-alpha in BAL fluids, and the enhanced neutrophil number of LPS-exposed mice were reduced, whereas the level of IL-10 was increased[3]. Oral BDP (Beclometasone Dipropionate) gave an overall treatment result in patients with active ulcerative colitis without signs of systemic side-effects[4]. Sustained clinical and histological remission was induced with the topical steroid preparation, beclometasone dipropionate (Clipper), with no adverse effects[5]. Beclometasone dipropionate (BDP) is a topically active corticosteroid with low absorption into the systemic circulation, which minimises many of the deleterious side effects associated with systemic corticosteroids[6].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00854360 Seasonal Allergic Rhinitis ... 展开 >> Hayfever 收起 << Phase 2 Completed - -
NCT00854360 - Completed - -
NCT01345916 Asthma Phase 3 Completed - Poland ... 展开 >> GSPZOZ Uniwersytecki Szpital Kliniczny Łódź, Poland, 90-153 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.92mL

0.38mL

0.19mL

9.60mL

1.92mL

0.96mL

19.19mL

3.84mL

1.92mL
参考文献

[1]Ratner PH, Melchior A, et al. Pharmacokinetic profile of beclomethasone dipropionate hydrofluoroalkane after intranasal administration versus oral inhalation in healthy subjects: results of a single-dose, randomized, open-label, 3-period crossover study. Clin Ther. 2012 Jun;34(6):1422-31.

[2]Busse WW, Brazinsky S, et al. Efficacy response of inhaled beclomethasone dipropionate in asthma is proportional to dose and is improved by formulation with a new propellant. J Allergy Clin Immunol. 1999 Dec;104(6):1215-22.

[3]Corbel M, Lagente V, Théret N, Germain N, Clément B, Boichot E. Comparative effects of betamethasone, cyclosporin and nedocromil sodium in acute pulmonary inflammation and metalloproteinase activities in bronchoalveolar lavage fluid from mice exposed to lipopolysaccharide. Pulm Pharmacol Ther. 1999;12(3):165-71

[4]Campieri M, Adamo S, Valpiani D, D'Arienzo A, D'Albasio G, Pitzalis M, Cesari P, Casetti T, Castiglione GN, Rizzello F, Manguso F, Varoli G, Gionchetti P. Oral beclometasone dipropionate in the treatment of extensive and left-sided active ulcerative colitis: a multicentre randomised study. Aliment Pharmacol Ther. 2003 Jun 15;17(12):1471-80

[5]Ibraheim H, Green M, Papa S, Powell N. Topical beclometasone dipropionate in the management of immune checkpoint inhibitor-induced microscopic colitis. BMJ Case Rep. 2019 Apr 3;12(4):e226481

[6]Díez-Campelo M, Sánchez-Guijo FM, Pérez-Simón JA. Beclometasone dipropionate: a topically active corticosteroid for the treatment of gastrointestinal graft-versus-host disease. Expert Opin Investig Drugs. 2008 Sep;17(9):1389-401