Salbutamol (hydrochloride)
(Synonyms: 盐酸左旋沙丁胺醇,(R)-Albuterol hydrochloride; (R)-Salbutamol hydrochloride; Levosalbutamol hydrochloride) 目录号 : GC44868
A β2-AR agonist
Cas No.:50293-90-8
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Salbutamol is an agonist of the β2-adrenergic receptor (β2-AR; Kd = 759 nM in a radioligand binding assay using CHO cells expressing the human receptor). It is selective for β2-ARs over β1- and β3-ARs (Kds = 46.8 and 21.9 μM, respectively). Salbutamol (25-50 μg/kg, i.v.) reduces acetylcholine-induced bronchospasm in anesthetized guinea pigs. It also reduces response of bronchial muscle to efferent vagal stimulation in anesthetized cats and dogs when administered at doses ranging from 1 to 2.5 and 10 to 20 μg/kg, respectively. Nebulized salbutamol reduces transpulmonary pressure in recurrent airway obstruction-affected horses (EC50 = 39.7 μg). Formulations containing salbutamol have been used in the treatment of asthma and chronic obstructive pulmonary disease (COPD).
| Cas No. | 50293-90-8 | SDF | |
| 别名 | 盐酸左旋沙丁胺醇,(R)-Albuterol hydrochloride; (R)-Salbutamol hydrochloride; Levosalbutamol hydrochloride | ||
| Canonical SMILES | OCC1=C(O)C=CC([C@@H](O)CNC(C)(C)C)=C1.Cl | ||
| 分子式 | C13H21NO3•HCl | 分子量 | 275.8 |
| 溶解度 | DMF: 25 mg/ml,DMSO: 20 mg/ml,Ethanol: 12 mg/ml,PBS (pH 7.2): 3 mg/ml | 储存条件 | Store at -20°C,protect from light |
| 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 | 3.6258 mL | 18.1291 mL | 36.2582 mL |
| 5 mM | 0.7252 mL | 3.6258 mL | 7.2516 mL |
| 10 mM | 0.3626 mL | 1.8129 mL | 3.6258 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。
Clenbuterol hydrochloride
Profiles Drug Subst Excip Relat Methodol 2017;42:91-123.PMID:28431781DOI:10.1016/bs.podrm.2017.02.002.
Clenbuterol (Broncodil and trade) is a direct-acting sympathomimetic agent with mainly beta-adrenergic activity and a selective action on β2 receptors (a β2 agonist). It has properties similar to those of Salbutamol. It is used as a bronchodilator in the management of reversible airways obstruction, as in asthma and in certain patients with chronic obstructive pulmonary disease. The uses, applications, and the synthetic pathways of this drug are outlined. Physical characteristics including: ionization constant, solubility, X-ray powder diffraction pattern, thermal methods of analysis, UV spectrum, IR spectrum, mass spectrum are all produced. This profile also includes the monograph of British Pharmacopoeia, together with several reported analytical methods including spectrophotometric, electrochemical, chromatographic, immunochemical methods, and capillary electrophoretic methods. The stability, the pharmacokinetic behavior, and the pharmacology of the drug are also provided.
Levalbuterol hydrochloride
Expert Opin Investig Drugs 1998 Dec;7(12):2027-41.PMID:15991945DOI:10.1517/13543784.7.12.2027.
Racemic Salbutamol (racemic albuterol) ameliorates symptoms of asthma by activating beta-adrenoceptors on nerve, smooth muscle and inflammatory cells within the airways. Racemic Salbutamol comprises equal proportions of 2 isomers: (S)-salbutamol and (R)-salbutamol, with the latter being exclusively responsible for activation of beta-adrenoceptors. Accordingly, within racemic Salbutamol it is (R)-salbutamol that efficiently relieves obstruction of asthmatic airways and affords highly effective protection from bronchoconstrictor stimuli, including allergens. During regular use of racemic Salbutamol, there is a progressive decline of protective efficacy and a corresponding intensification of airway responsiveness. This decline is largely absent during regular use of (R)-salbutamol. Consequently, bronchodilator responses to sub-maximal doses of (R)-salbutamol exceed responses to the equivalent dose of (R)-salbutamol given as the racemate. For example, in asthmatics with baseline FEVs
Levalbuterol hydrochloride
Pediatr Pulmonol 2002 Feb;33(2):151-7.PMID:11802253DOI:10.1002/ppul.10027.
Racemic albuterol, a commonly used bronchodilator, is an exact 50:50 mixture of two enantiomers, R- and S-albuterol. Concern regarding increased mortality associated with the use of this beta-2 (beta 2) agonist triggered the study of both of these enantiomers separately. In vitro studies suggest that the two enantiomers have different binding affinities for beta-adrenoreceptors, may exert opposing effects on inflammation, demonstrate different effects on mucocilary transport, and display differing pharmacokinetics. Clinical studies comparing both enantiomers are few, of short duration, and often in small patient populations, and their results vary. R-albuterol has greater bronchodilatory effects than the racemate and may have anti-inflammatory properties. S-albuterol has markedly less affinity for the beta-adrenoreceptor. It was found to cause bronchoconstriction in animal models, but neither bronchoconstrictive nor pro-inflammatory effects have been conclusively demonstrated in human studies. The data available at present, while suggestive, are insufficient to conclusively recommend R-albuterol over the racemate. Further basic research and investigations in humans comparing both enantiomers at increasing doses over longer time periods are required to clarify the precise roles of R- and S-albuterol.
Simultaneous determination of Salbutamol sulphate and bromhexine hydrochloride in tablets by reverse phase liquid chromatography
Indian J Pharm Sci 2009 Jan;71(1):53-5.PMID:20177457DOI:10.4103/0250-474X.51957.
A simple reverse phase liquid chromatographic method has been developed and subsequently validated for simultaneous determination of Salbutamol sulphate and bromhexine hydrochloride. The separation was carried out using a mobile phase consisting of acetonitrile, methanol and phosphate buffer, pH 4 in the ratio 60:20:20 v/v. The column used was SS Wakosil-II C-18 with a flow rate of 1 ml/min and UV detection at 224 nm. The described method was linear over a concentration range of 10-110 mug/ml and 20-140 mug/ml for the assay of Salbutamol sulphate and bromhexine hydrochloride, respectively. The mean recovery was found to be 95-105% for Salbutamol sulphate and 96.2-102.1% for bromhexine hydrochloride when determined at five different levels.
Orally-disintegrating Tablets in Fixed-dose Combination Containing Ambroxol hydrochloride and Salbutamol Sulphate Prepared by Direct Compression: Formulation Design, Development and In Vitro Evaluation
Turk J Pharm Sci 2018 Apr;15(1):29-37.PMID:32454637DOI:10.4274/tjps.24633.
Objectives: To design a formulation and develop ODTs of AMB hydrochloride and Salbutamol sulphate in combination for the treatment of respiratory disorders and perform an in vitro evaluation using superdisintegrants in combination with a suitable binder and excipients. Direct compression was used to prepare the tablets. Materials and methods: In the present research work, different concentrations of SSG as a superdisintegrant were used to optimize the concentration of SSG in the formulation of ODTs. Different concentrations of MCC and PVP K-30 were also studied along with the optimized SSG concentration. The tablets were evaluated for hardness, friability, weight variation, wetting time, in vitro DT, and percentage drug content uniformity. The optimized formulation was further evaluated in an in vitro release study, and drug-excipient compatibility and accelerated stability study. Results: The optimized concentration of SSG was found as 4% on the basis of the lowest DT. The 1% concentration of MCC was selected as the optimum binder concentration on the basis of the lowest DT. ODTs passed all the quality control tests viz., weight variation, hardness, friability, in vitro DT, drug content (%) and wetting time. The formulation satisfied the requirements of the FDA for rapid-dissolving tablets and allowed more than 85% drug to be released within 30 min. The fourier transform infrared spectroscopy study revealed that there was no interaction between the drug and excipients. The accelerated stability study shows that formulation is quite stable at normal temperature and humidity conditions as well as at extreme temperature conditions. Conclusion: By adopting a systematic formulation approach, ODTs of AMB hydrochloride and Salbutamol sulphate in fixed-dose combination can be formulated using superdisintegrants in combination with appropriate binder and excipients; this was found to be economical and industrially feasible.