Ambroxol-d5
(Synonyms: 盐酸氨溴索D5) 目录号 : GC48611An internal standard for the quantification of ambroxol
Cas No.:1246818-80-3
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Ambroxol-d5 is intended for use as an internal standard for the quantification of ambroxol by GC- or LC-MS. Ambroxol is an expectorant and active metabolite of bromhexine.1 It decreases short-circuit currents in electrically stimulated isolated canine tracheal epithelial cells when applied submucosally (IC50 = 60 nM).2 Ambroxol (100 µM) decreases IL-13-induced production of mucin 5AC (MUC5AC) in primary human airway epithelial cells and inhibits IL-13-induced decreases in the mucociliary transport rate of endogenous particles in the same cells.3 Ambroxol increases phenol red secretion, a marker of expectorant activity, in mice when administered at doses of 30, 60, or 120 mg/kg.4 Formulations containing ambroxol have been used in the treatment of acute or chronic respiratory conditions.
1.Malerba, M., and Ragnoli, B.Ambroxol in the 21st century: Pharmacological and clinical updateExpert Opin. Drug Metab. Toxicol.4(8)1119-1129(2008) 2.Tamaoki, J., Chiyotani, A., Yamauchi, F., et al.Ambroxol inhibits Na+ absorption by canine airway epithelial cells in cultureJ. Pharm. Pharmacol.43(12)841-843(1991) 3.Seagrave, J., Albrecht, H.H., Hill, D.B., et al.Effects of guaifenesin, N-acetylcysteine, and ambroxol on MUC5AC and mucociliary transport in primary differentiated human tracheal-bronchial cellsRespir. Res.13(1)98(2012) 4.Menezes, P.M.N., Brito, M.C., Sousa de SÁ, P.G., et al.Analytical and pharmacological validation of the quantification of phenol red in a mouse model: An optimized method to evaluate expectorant drugsJ. Pharmacol. Toxicol. Methods98106586(2019)
Cas No. | 1246818-80-3 | SDF | |
别名 | 盐酸氨溴索D5 | ||
Canonical SMILES | O[C@@](C([2H])([2H])C1)([2H])C([2H])([2H])C[C@@H]1NCC2=C(C(Br)=CC(Br)=C2)N | ||
分子式 | C13H13Br2D5N2O | 分子量 | 383.1 |
溶解度 | Acetonitrile: soluble,DMSO: soluble,Methanol: soluble,Water: soluble | 储存条件 | -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 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 2.6103 mL | 13.0514 mL | 26.1028 mL |
5 mM | 0.5221 mL | 2.6103 mL | 5.2206 mL |
10 mM | 0.261 mL | 1.3051 mL | 2.6103 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 | |||
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% DMSO % % Tween 80 % saline | ||||||||||
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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。
[Determination of ambroxol hydrochloride in human plasma by ultra high performance liquid chromatography-tandem mass spectrometry and bioequivalence evaluation of its preparation]
Se Pu 2018 Nov 1;36(11):1099-1104.PMID:30378372DOI:10.3724/SP.J.1123.2018.07021
A rapid, simple and sensitive ultra high performance liquid chromatography-tandem mass spectrometry (UHPLC-MS/MS) method was developed for the determination of ambroxol hydrochloride in human plasma, and bioequivalence of its preparation was evaluated. The 50 μL-plasma sample was treated with methanol for protein precipitation, while Ambroxol-d5 was used as an internal standard (IS). The separation was carried out on a Waters XBridge BEH C18 column (50 mm×2.1 mm, 2.5 μm) by gradient elution at a flow rate of 0.4 mL/min, with 0.1% (v/v) formic acid aqueous solution and methanol containing 0.1% (v/v) formic acid as the mobile phases. The analyte was detected using an electrospray ionization source in positive ion multiple reaction monitoring (MRM) mode. The calibration curves were linear in the range of 2-400 ng/mL (r=0.998). The intra- and inter-run accuracies were 97.1%-108.7%, the intra- and inter-run precisions were 1.0%-5.6%. The method was applied to the determination of the plasma concentration of the six healthy subjects after the oral administration of 30 mg of test and reference preparations. The bioavailability was (102.3±14.8)%. The 90% confidence intervals of the test preparation's pharmacokinetic parameters were 80.0%-125.0% of the reference preparation's corresponding parameters. Thus, it is proved that the test preparation and reference preparation are bioequivalent.