LevodropropizineHistamine receptor inhibitor,cough suppressant CAS# 99291-25-5 |
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Quality Control & MSDS
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| Cas No. | 99291-25-5 | SDF | Download SDF |
| PubChem ID | 65859 | Appearance | Powder |
| Formula | C13H20N2O2 | M.Wt | 236.31 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO : ≥ 50 mg/mL (211.59 mM) H2O : 10 mg/mL (42.32 mM; Need ultrasonic) *"≥" means soluble, but saturation unknown. | ||
| Chemical Name | (2S)-3-(4-phenylpiperazin-1-yl)propane-1,2-diol | ||
| SMILES | C1CN(CCN1CC(CO)O)C2=CC=CC=C2 | ||
| Standard InChIKey | PTVWPYVOOKLBCG-ZDUSSCGKSA-N | ||
| Standard InChI | InChI=1S/C13H20N2O2/c16-11-13(17)10-14-6-8-15(9-7-14)12-4-2-1-3-5-12/h1-5,13,16-17H,6-11H2/t13-/m0/s1 | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
Levodropropizine Dilution Calculator
Levodropropizine Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 4.2317 mL | 21.1586 mL | 42.3173 mL | 84.6346 mL | 105.7932 mL |
| 5 mM | 0.8463 mL | 4.2317 mL | 8.4635 mL | 16.9269 mL | 21.1586 mL |
| 10 mM | 0.4232 mL | 2.1159 mL | 4.2317 mL | 8.4635 mL | 10.5793 mL |
| 50 mM | 0.0846 mL | 0.4232 mL | 0.8463 mL | 1.6927 mL | 2.1159 mL |
| 100 mM | 0.0423 mL | 0.2116 mL | 0.4232 mL | 0.8463 mL | 1.0579 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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Levodropropizine possess anti-allergic and inhibits histamine receptor, reduces cough by interfering with stimulus activation of peripheral endings of sensory nerves and by modulation of neuropeptides involved in the cough reflex.
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Levodropropizine for treating cough in adult and children: a meta-analysis of published studies.[Pubmed:26097707]
Multidiscip Respir Med. 2015 May 31;10(1):19.
BACKGROUND: Cough is one of the most common symptoms for which patients seek medical attention from primary care physicians and lung specialists. About 40% of the population at any one time report cough. Cough is associated with significantly impaired health-related quality of life. Levodropropizine is an effective and very well tolerated peripheral antitussive drug. We want to compare it to central cough suppressants efficacy (opioids and non-opioids) that may be associated with side effects limiting their use. METHODS: After a comprehensive literature search, a meta-analysis of 7 clinical studies of Levodropropizine vs. control, including a total of 1,178 patients, was performed with the aim to evaluate the overall comparative efficacy of Levodropropizine in the pediatric and adult population. Three electronic databases and reference list were used to search for studies that assessed the efficacy of Levodropropizine for treating cough in children and adults using as standardized efficacy parameters the cough frequency and severity, and number of night awakenings as outcome parameters. RESULTS: The meta-analysis of all standardized efficacy parameters showed a highly statistically significant difference in the overall antitussive efficacy in favor of Levodropropizine vs. control treatments (p = 0.0015). The heterogeneity test for the efficacy outcome was not statistically significant (p = 0.0534). Seven studies met out inclusion criteria. A meta-analysis of the eligible ones showed a statistically significant difference in the overall anti-tussive effect of Levodropropizine versus control (p = 0.0015). CONCLUSIONS: This analysis indicates that Levodropropizine is an effective antitussive drug in children and adults, with statistically significant better overall efficacy outcomes vs. central antitussive drugs (codeine, cloperastine, dextromethorphan) in terms of reducing cough intensity and frequency, and nocturnal awakenings. This result further reinforces the favorable benefit/risk profile of Levodropropizine in the management of cough. The efficacy of Levodropropizine in the treatment of cough in children and adults is higher than that of the common centrally-acting anti-tussive.
Levodropropizine-Induced Anaphylaxis: Case Series and Literature Review.[Pubmed:28293935]
Allergy Asthma Immunol Res. 2017 May;9(3):278-280.
Levodropropizine is commonly used as an antitussive drug for acute and chronic cough. It is a non-opioid agent with peripheral antitussive action via the modulation of sensory neuropeptide levels in the airways. Thus, Levodropropizine has a more tolerable profile than opioid antitussives. However, we experienced 3 cases of Levodropropizine-induced anaphylaxis. Three patients commonly presented with generalized urticaria, dyspnea, and collapse after taking cold medication including Levodropropizine. To find out the culprit drug, we performed skin tests, oral provocation tests (OPTs), and basophil activation tests (BATs). Two patients were confirmed as having Levodropropizine-induced anaphylaxis by OPTs, and one of them showed positive to skin prick tests (SPTs). The other patient was confirmed by skin tests and BATs. When we analyzed pharmacovigilance data related to Levodropropizine collected for 5 years, most cases (78.9%) had allergic reactions, such as rash, urticaria, angioedema, and anaphylaxis. Therefore, physicians should consider that Levodropropizine can be a culprit drug, when anaphylaxis occurs after taking anti-cough or common cold medication.
Design, in vitro release characterization and pharmacokinetics of novel controlled release pellets containing levodropropizine.[Pubmed:23509871]
Pharm Dev Technol. 2014 May;19(3):296-303.
This study was performed to investigate the in vitro release characteristics of Levodropropizine (LDP) from novel dual-coated sustained release (SR) pellets, and evaluate the pharmacokinetics of a novel controlled release (CR) preparation composed of the dual-coated SR pellets and immediate release (IR) LDP pellets. The dual-coated SR pellets composed of a drug-loaded nonpareil core, a sub-coating layer (HPMC 6cps) and an SR-coating layer (Aquacoat(R) ECD, Eudragit(R) RS 30D or Kollicoat(R) SR 30D) were prepared by a bottom-spray fluidized bed-coating method. The drug release from the dual-coated SR pellets coated with Aquacoat(R) ECD followed a zero-order profile in water, and the drug release was not affected by the coating level of the sub-coating layer and stable under the accelerated storage condition (40 degrees C, 75% RH) for 6 months. The CR preparation showed significantly decreased values of maximum drug concentration (Cmax) and elimination rate (K) than the reference product (LEVOTUS(R) SYR) but the similar bioavailability (F = 95.43%). The novel CR preparation presents promising delivery of LDP with an immediate and sustained release manner, with similar clinical effect as the commercial IR product.
Development and Validation of a Stability-Indicating LC-Method for the Simultaneous Estimation of Levodropropizine, Chloropheniramine, Methylparaben, Propylparaben, and Levodropropizine Impurities.[Pubmed:23641334]
Sci Pharm. 2013 Jan-Mar;81(1):139-50.
A simple, fast, and efficient RP-HPLC method has been developed and validated for the simultaneous estimation of Levodropropizine, Chloropheniramine, Methylparaben, Propylparaben, and the quantification of Levodropropizine impurities in the Reswas syrup dosage form. A gradient elution method was used for the separation of all the actives and Levodropropizine impurities by using the X-Bridge C18, 150 mm x 4.6 mm, 3.5 mum column with a flow rate of 1.0 mL/min and detector wavelength at 223 nm. The mobile phase consisted of a potassium dihydrogen orthophosphate buffer and acetonitrile. All the peaks were symmetrical and well-resolved (resolution was greater than 2.5 for any pair of components) with a shorter run time. The limit of detection for Levodropropizine and its Impurity B was 0.07 mug/ml & 0.05 mug/ml, whereas the limit of quantification was 0.19 mug/ml & 0.15 mug/ml respectively. The method was validated in terms of precision, accuracy, linearity, robustness, and specificity. Degradation products resulting from the stress studies were well-resolved and did not interfere with the detection of Levodropropizine, Chloropheniramine, Methylparaben, Propylparaben, and Levodropropizine Impurity B, thus the test method is stability-indicating. Validation of the method was carried out as per International Conference on Harmonization (ICH) guidelines.
