产品说明书

Loteprednol Etabonate

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Chemical Structure| 82034-46-6 同义名 : 氯替泼诺
CAS号 : 82034-46-6
货号 : A111407
分子式 : C24H31ClO7
纯度 : 98%
分子量 : 466.952
MDL号 : MFCD00870765
存储条件:

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 105 mg/mL(224.86 mM),配合低频超声助溶,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

动物实验配方:
生物活性
描述 Loteprednol etabonate is a corticosteroid which is the product of 'soft drug' design (synthesis of a compound that undergoes predictable metabolism to inactive metabolites after its therapeutic effects have been expressed at or near the site of application). Loteprednol etabonate can reduce ocular inflammation caused by cataract surgery, seasonal allergic conjunctivitis or contact lens wear. The benign tolerability profile of loteprednol etabonate, in particular its low propensity to cause elevated IOP (when used in the short term) is an attractive characteristic[3]. LE (Loteprednol Etabonate) relieves ocular surface and lacrimal gland inflammation associated with dry eye and is used in combination with ciclosporin A as a treatment of dry eye[4]. In vivo animal studies, loteprednol effectively inhibited allergically induced vascular leakage in the nasal cavity of actively sensitized Brown Norway rats and rhinorrhea in actively sensitized domestic pigs following nasal challenge. In several models of allergic asthma, it was clearly demonstrated that loteprednol was able to suppress the allergically induced late phase eosinophilia in mice, rats and guinea pigs.[5].
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
NCT00905762 Healthy Phase 1 Completed - United States, New York ... 展开 >> Bausch & Lomb Incorporated Rochester, New York, United States, 14609 收起 <<
NCT02163824 Ocular Infections, Irritations... 展开 >> and Inflammations 收起 << Phase 3 Completed - United States, California ... 展开 >> Sall Research Medical Center Artesia, California, United States, 90701 North Valley Eye Medical Group Mission Hills, California, United States, 91345 Martel Eye Medical Group Rancho Cordova, California, United States, 95670 Wolstan & Goldberg Eye Associates Torrance, California, United States, 90505 United States, Georgia Clayton Eye Center Morrow, Georgia, United States, 30260 United States, Indiana Price Vision Group Indianapolis, Indiana, United States, 46260 John-Kenyon American Eye Institute New Albany, Indiana, United States, 47150 United States, Kentucky Taustine Eye Center Louisville, Kentucky, United States, 40217 United States, Missouri Tauber Eye Center Kansas City, Missouri, United States, 64111 Tekwani Vision Center Saint Louis, Missouri, United States, 63128 Ophthalmology Associates Saint Louis, Missouri, United States, 63131 Ophthalmology Consultants Saint Louis, Missouri, United States, 63131 United States, Nevada Las Vegas Physicians Research Group Henderson, Nevada, United States, 89052 United States, New York Raymond Fong, MDPC New York, New York, United States, 10013 Rochester Ophthalmological Group, PC Rochester, New York, United States, 14618 United States, North Carolina Cornerstone Eye Care High Point, North Carolina, United States, 27262 United States, Ohio Cincinnati Eye Institute Cincinnati, Ohio, United States, 45242 The Eye Center of Columbus Columbus, Ohio, United States, 43215 United States, South Carolina Westside Research, LLC Spartanburg, South Carolina, United States, 29306 United States, Texas The Eye Clinic of Texas, Affiliate of Houston Eye Associates League City, Texas, United States, 77573 R&R Eye Research, LLC San Antonio, Texas, United States, 78229 Kozlovsky Delay & Winter Eye Consultants, LLC San Antonio, Texas, United States, 78230 United States, Virginia Virginia Eye Consultants Norfolk, Virginia, United States, 23502 收起 <<
NCT02813265 Dry Eye Syndromes ... 展开 >> Keratoconjunctivitis Sicca 收起 << Phase 3 Completed - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.14mL

0.43mL

0.21mL

10.71mL

2.14mL

1.07mL

21.42mL

4.28mL

2.14mL

参考文献

[1]Buris LF, Bodor N, Buris L. Loteprednol etabonate, a new soft steroid is effective in a rabbit acute experimental model for arthritis. Pharmazie. 1999 Jan;54(1):58-61.

[2]Druzgala P, Hochhaus G, Bodor N. Soft drugs--10. Blanching activity and receptor binding affinity of a new type of glucocorticoid: loteprednol etabonate. J Steroid Biochem Mol Biol. 1991 Feb;38(2):149-54.

[3]Noble S, Goa KL. Loteprednol etabonate: clinical potential in the management of ocular inflammation. BioDrugs. 1998 Oct;10(4):329-39.

[4]Pavesio CE, Decory HH. Treatment of ocular inflammatory conditions with loteprednol etabonate. Br J Ophthalmol. 2008 Apr;92(4):455-9

[5]Szelenyi I, Hochhaus G, Heer S, Kusters S, Marx D, Poppe H, Engel J. Loteprednol etabonate: a soft steroid for the treatment of allergic diseases of the airways. Drugs Today (Barc). 2000 May;36(5):313-20.