O-Desmethyl Lacosamide
(Synonyms: 去甲拉考沙胺) 目录号 : GC49249
A potential impurity found in commercial preparations of lacosamide
Cas No.:175481-38-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >95.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
O-Desmethyl lacosamide is a potential impurity found in commercial preparations of lacosamide).1,2
1.Molleti, S., Rao, V., and Jayaveera, K.N.Stability indicating RP-UPLC method for the determination of lacosamide and its impurities in bulk drugs and its pharmaceutical dosage formsDer Pharma Chemica5(1)81-89(2013) 2.Yang, A., Hu, F., Chen, M., et al.Improved synthesis and impurity identification of (R)-lacosamideOrg. Proc. Res. Dev.23(5)818-824(2019)
| Cas No. | 175481-38-6 | SDF | |
| 别名 | 去甲拉考沙胺 | ||
| Canonical SMILES | O=C(NCC1=CC=CC=C1)[C@@H](CO)NC(C)=O | ||
| 分子式 | C12H16N2O3 | 分子量 | 236.3 |
| 溶解度 | DMSO: soluble,Ethanol: 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.2319 mL | 21.1595 mL | 42.3191 mL |
| 5 mM | 0.8464 mL | 4.2319 mL | 8.4638 mL |
| 10 mM | 0.4232 mL | 2.116 mL | 4.2319 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。
A sensitive and rapid method for quantification of lacosamide and desmethyl lacosamide by LC-MS/MS
Bioanalysis 2014;6(23):3161-8.PMID:25529884DOI:10.4155/bio.14.158.
Background: Monitoring lacosamide (LCM) helps optimize therapeutic dosing in some clinical settings. We developed a novel LC-MS/MS method for measuring serum LCM and O-Desmethyl Lacosamide (ODL). Results/discussion: The sample preparation was protein precipitation with methanol. The total CV was less than 4.7%. Calibration range was 0.95-30.29 µg/ml and 0.95-30.41 µg/ml while the expanded linear range was 0.41-47.49 µg/ml and 0.34-48.17 µg/ml for LCM and ODL, respectively with analytical accuracy of 87.2-106.0%. 45 random serum samples collected from 23 individuals on either 200 mg/day or 400 mg/day of LCM therapy showed concentrations of 2.2-19.8 µg/ml for LCM and up to 2.5 µg/ml for ODL. Conclusion: A simple and sensitive LC-MS/MS assay was validated for quantification of LCM and ODL in human serum.
[Therapeutic drug monitoring of lacosamide]
Therapie 2012 Mar-Apr;67(2):151-5.PMID:22850102DOI:10.2515/therapie/2012012.
Lacosamide is a third generation antiepileptic drug, available in France since 2008. It is indicated in combination therapy for the treatment of inadequately controlled focal seizures, from the age of 16. The bioavailability of lacosamide is 100% and is unaffected by food intake; protein binding is low; it is metabolized by CYP2C19 into inactive O-Desmethyl Lacosamide. It does not inhibit or induce cytochromes; the elimination is renal with a half-life of approximately 13 h. The relationship between dose and plasma concentration is established, but there does not appear to be any clear relationship between concentration and efficacy. However, the main side effects are concentration dependent. The potential for drug-drug interaction of lacosamide is low and variability between individuals is minimal. Accordingly, the level of evidence for the therapeutic drug monitoring has been estimated at "probably of no use".
Tolerability, pharmacokinetics, and bioequivalence of the tablet and syrup formulations of lacosamide in plasma, saliva, and urine: saliva as a surrogate of pharmacokinetics in the central compartment
Epilepsia 2013 Jan;54(1):81-8.PMID:23148731DOI:10.1111/j.1528-1167.2012.03725.x.
Purpose: To test for bioequivalence of 200 mg lacosamide oral tablet and syrup formulations. Additional objectives were to compare the pharmacokinetic profile of lacosamide in saliva and plasma, and to evaluate its tolerability. Methods: This open-label, randomized, two-way crossover trial was conducted in 16 healthy Caucasian male participants in Germany. The bioequivalence of 200 mg lacosamide tablet and syrup was evaluated using plasma to determine maximum measured concentration (C(max)) and area under the curve from zero to the last time point (AUC)(0-tz). Plasma and saliva samples for evaluation of pharmacokinetic parameters of lacosamide and the major metabolite O-Desmethyl Lacosamide (SPM 12809) were taken over 15 time points (0.5-72 h) and used to statistically compare bioavailability of the two. Urine samples were collected predose and over five time points (0-48 h) to evaluate the cumulative amount of unchanged drug and metabolite. Key findings: Lacosamide median time to reach C(max) (t(max)) was 1 h for tablet and 0.5 h for syrup in plasma and saliva. Mean terminal half life (t(½)) for tablet and syrup was 12.5 and 12.4 h in plasma, and 13.1 and 13.3 h in saliva, respectively. Tablet and syrup mean plasma AUC(0-tz) was 84.5 and 83.3 μg/mL*h, respectively. Mean AUC(0-tz) in saliva was 93.2 μg/mL*h for tablet and syrup. Mean C(max) for tablet was 5.26 μg/mL in plasma and 5.63 μg/mL in saliva. Syrup mean C(max) was 5.14 and 8.32 μg/mL in plasma and saliva, respectively. Within 2 h of syrup administration, elevated lacosamide concentration in saliva compared to plasma was observed. The ratio of lacosamide syrup to tablet was 0.98 for C(max) and 0.99 for AUC(0-tz) in plasma, and 1.00 for AUC((0-tz)) in saliva; the 90% confidence intervals (CIs) for these parameters were within the range of 0.80-1.25, which meets accepted bioequivalence criteria. The syrup-to-tablet ratio for C(max) in saliva was 1.48, and the 90% CIs exceeded the accepted upper boundary for bioequivalence (1.32-1.66). Both formulations were well tolerated. Metabolite concentration versus time profiles for saliva were similar to plasma following tablet and syrup administration. Significance: The tablet and syrup formulations of lacosamide 200 mg were bioequivalent and well tolerated. Saliva samples were demonstrated to be a suitable surrogate to evaluate lacosamide tablet pharmacokinetics in the central compartment. Due to residual syrup in the buccal cavity, limitations exist when using saliva to evaluate the pharmacokinetics of lacosamide syrup <2 h after administration.