Loratadine-d5
(Synonyms: 五氘代氯雷他定,Loratidine-d5; SCH 29851-d5) 目录号 : GC47575
An internal standard for the quantification of loratadine
Cas No.:1020719-57-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Loratadine-d5 is intended for use as an internal standard for the quantification of loratadine by GC- or LC-MS. Loratadine is a non-sedating antihistamine that acts as a selective inverse agonist of peripheral histamine H1 receptors (Ki = 35 nM).1,2,3 It has been shown to inhibit the release of leukotriene C4 (IC50 = 8 µM) and histamine (IC50 = 11 µM) from rodent mast cells and to inhibit allergic bronchospasm in guinea pigs with an ED50 value of 0.40 mg/kg.4 Formulations containing loratadine have been used in the treatment of allergic rhinitis and chronic idiopathic urticaria.
1.Ahn, H.S., and Barnett, A.Selective displacement of [3H]mepyramine from peripheral vs. central nervous system receptors by loratadine, a non-sedating antihistamineEur. J. Pharmacol.127(1-2)153-155(1986) 2.Kay, G.G., and Harris, A.G.Loratadine: A non-sedating antihistamine. Review of its effects on cognition, psychomotor performance, mood and sedationClin. Exp. Allergy29(Suppl 3)147-150(1999) 3.Barnett, A., Iorio, L.C., Kreutner, W., et al.Evaluation of the CNS properties of SCH 29851, a potential non-sedating antihistamineAgents Actions43(3-4)149-156(1994) 4.Kreutner, W., Chapman, R.W., Gulbenkian, A., et al.Antiallergic activity of loratadine, a non-sedating antihistamineAllergy42(1)57-63(1987)
| Cas No. | 1020719-57-6 | SDF | |
| 别名 | 五氘代氯雷他定,Loratidine-d5; SCH 29851-d5 | ||
| Canonical SMILES | ClC(C=C1)=CC(CC([2H])([2H])C2=C/3N=C([2H])C([2H])=C2[2H])=C1C3=C4CCN(C(OCC)=O)CC/4 | ||
| 分子式 | C22H18ClD5N2O2 | 分子量 | 387.9 |
| 溶解度 | DMF: 30 mg/ml,DMSO: 25 mg/ml,Ethanol: 30 mg/ml | 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 | 2.578 mL | 12.8899 mL | 25.7798 mL |
| 5 mM | 0.5156 mL | 2.578 mL | 5.156 mL |
| 10 mM | 0.2578 mL | 1.289 mL | 2.578 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。
LC-ESI-MS/MS estimation of loratadine-loaded self-nanoemulsifying drug delivery systems in rat plasma: Pharmacokinetic evaluation and computer simulations by GastroPlus™
J Pharm Biomed Anal 2016 May 30;124:10-21.PMID:26922577DOI:10.1016/j.jpba.2016.02.008
A rapid, sensitive, and accurate bioanalytical method was established for the quantitation and pharmacokinetic investigation of loratadine (LTD) in rat plasma by liquid chromatography-electrospray ionization mass spectrometry (LC-ESI-MS/MS) using Loratadine-d5 as internal standard (ISTD). The analyte and ISTD were extracted by solid-phase extraction and chromatographic separation was achieved on Gemini NX- Reverse Phase C18 (50 × 4.6mm; 5 μ) using mobile phase mixture of 5mM ammonium formate buffer in water (pH 3.5 ± 0.1 with formic acid), and acetonitrile (20:80 v/v), at a flow rate of 0.400 mL/min with injection volume of 10 μL. LTD and ISTD were detected at m/z 383.3 → 337.4 and 388.4 → 337.3 with retention time of 2.62 and 2.59 min, respectively. High sensitivity (1.0 ng/mL) was achieved using small volume of rat plasma (20 μL) and the method was validated over a linearity range of 1.05-405.41 ng/mL with high correlation coefficient (r = 0.9998). The extraction method displayed a mean process efficiency of 63.25 and 65.47% for LTD and ISTD, respectively. The validated method when successfully applied for quantification of LTD in rat plasma revealed enhanced bioavailability of orally administered LTD-loaded self-nanoemulsifying drug delivery system (SNEDDS) (Cmax, 466.65 ± 18.94 ng/mL and AUC0-t 633.00 ± 12.44 ng-h/mL) over LTD-suspension (Cmax, 104.75 ± 2.87 ng/mL and AUC0-t 287.00 ± 9.11 ng-h/mL). The in vivo-in silico prediction by the GastroPlus™ software showed good prediction accuracy for LTD-SNEDDS (fold error < 2). The Loo-Reigelman method (2-compartment) presented best model-fitting indicating adequate in vitro-in vivo correlations. Conclusively, the developed sensitive analytical method displayed enhanced systemic availability of LTD-SNEDDS, and the in vivo in silico approach revealed sufficiently good GI simulation.