产品说明书

Olopatadine HCl

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Chemical Structure| 140462-76-6 同义名 : KW4679;ALO4943A;Patanase;Pataday;Olopatadine (hydrochloride);Olopatadine hydrochloride
CAS号 : 140462-76-6
货号 : A143866
分子式 : C21H24ClNO3
纯度 : 98%
分子量 : 373.873
MDL号 : MFCD00875716
存储条件：

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(133.74 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

H2O: 6.5 mg/mL(17.39 mM)，配合低频超声助溶
动物实验配方：

PO 0.5% CMC-Na 23 mg/mL suspension

生物活性
靶点

  • Histamine receptor
描述 Olopatadine hydrochloride is an antihistamine and mast cell stabilizer available as oral, intranasal and ocular preparations. It can function both as a viable alternative or addition to first line therapies such as intranasal steroids and oral antihistamines[3]. Compared to ketotifen, olopatadine provided quicker relief of symptoms, and improved symptoms of AC (Allergic conjunctivitis) and QOL (quality of life), with fewer side effects[4]. The rise in skin temperature was inhibited by pretreatment with olopatadine in a dose-dependent manner. Olopatadine also significantly inhibited increases in vascular permeability and nerve growth factor production in the skin induced by topical tacrolimus treatment. The combination application with olopatadine and tacrolimus ointment is useful for improving medication adherence with tacrolimus ointment treatment in patients with atopic dermatitis[5]. Oral administration of olopatadine inhibited passive cutaneous anaphylaxis in rats, experimental allergic rhinitis and bronchial asthmatic responses in actively sensitized guinea pigs. Olopatadine exerted no significant effects on action potential duration in isolated guinea pig myocardium and ventricular myocytes[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
NCT02709538 Perennial Allergic Rhinitis Phase 3 Completed - -
NCT02709538 - Completed - -
NCT03464435 Vernal Keratoconjunctivitis Phase 4 Completed - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.67mL

0.53mL

0.27mL

13.37mL

2.67mL

1.34mL

26.75mL

5.35mL

2.67mL
参考文献

[1]Havle A, Jain V, et al. Olopatadine Hydrochloride and Fluticasone Propionate in Topical Treatment of Allergic Rhinitis: A Single Blind Randomised Study. J Clin Diagn Res. 2016 Dec;10(12):MC04-MC07.

[2]Hampel FC Jr, Ratner PH, et al. Improved quality of life among seasonal allergic rhinitis patients treated with olopatadine HCl nasal spray 0.4% and olopatadine HCl nasal spray 0.6% compared with vehicle placebo. Allergy Asthma Proc. 2006 May-Jun;27(3):202-7.

[3]Gonzalez-Estrada A, Reddy K, Dimov V, Eidelman F. Olopatadine hydrochloride ophthalmic solution for the treatment of allergic conjunctivitis. Expert Opin Pharmacother. 2017 Aug;18(11):1137-1143

[4]Patel D, Sarala N, Datti NP. Topical Olopatadine Hydrochloride versus Ketotifen Fumarate for Allergic Conjunctivitis. J Ophthalmic Vis Res. 2018 Apr-Jun;13(2):119-123

[5]Satake K, Ikeda J, Tamura T, Amano T, Kobayashi K. Olopatadine hydrochloride suppresses hot flashes induced by topical treatment with tacrolimus ointment in rats. Eur J Pharmacol. 2015 Oct 15;765:402-5

[6]Ohmori K, Ikemura T, Kobayashi H, Mukouyama A. [Pharmacological, pharmacokinetic and clinical properties of olopatadine hydrochloride' (olopatadine), an antiallergic drug]. Nihon Yakurigaku Zasshi. 2001 Jul;118(1):51-8. Japanese