83-45-4 Purity
99%
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Specification
Lamotrigine (LTZ) can be used as monotherapy or adjunctive therapy for the treatment of epilepsy. In this work, a new method for the quantitative determination of LTZ in human plasma and dried plasma spots (DPS) was developed and validated. This method may provide a suitable and low-cost alternative for therapeutic drug monitoring (TDM) sampling of antiepileptic drugs (AEDs).
LTZ was extracted from plasma and DPS using liquid-liquid extraction with diethyl ether and an extraction solution composed of diethyl ether-methyl tert-butyl ether-acetone (50:30:20, v/v/v), respectively.
The internal standard Lamotrigine-13C3, d3 (LTZ-13C3, d3) was utilized, and chromatographic separation was achieved on a Hypurity Advance C18 column (150 × 4.6 mm, 5 μm). Quantitative estimation of LTZ and the internal standard was carried out on a liquid chromatography tandem mass spectrometer with an electrospray ionization interface operating in positive ionization mode.
Calibration curves were shown to be linear (r2 > 0.99) over a concentration range of 10-3020 ng/mL for both plasma and DPS. Statistical analysis revealed no significant difference in LTZ concentration between plasma and DPS samples, indicating that the method is suitable for use in clinical studies and therapeutic monitoring of LTZ.
A novel lamotrigine (LAM)-containing nanocapsule (NC) formulation for nasal administration was developed and its micrometer parameters, in vitro and in vivo formulation properties were determined. The results showed that the NC formulation had a size of approximately 305 nm, a high encapsulation efficiency (58.44%), and exhibited rapid and high release from the NC in vitro, as well as extensive penetration into brain tissue observed in in vivo studies.
Preparation of LAM nanocapsules
· The NCs were created using a solvent displacement method. The various liquid lipid: surfactant ratios were tested at three levels (2:1, 1:1, and 1:2), with the 1:1 ratio proving optimal in terms of particle size, PDI, and surface charge.
· To create the sample, the organic phase was first prepared by mixing an appropriate amount of LAM solution (100 mg/mL DMSO solution), Peceol, and Transcutol with PEGstearate 40 solution (5.33 mg/mL ethanol solution). This solution was then poured over 2 mL of ultrapure water while continuously stirring magnetically to form an o/w emulsion. After 10 minutes, 2 mL of chitosan solution (1 mg/mL) was added to the emulsion under magnetic stirring, resulting in the spontaneous formation of the NCs.
· In addition, in vivo studies involved the use of lamotrigine-13C3,d3 as an internal standard for plasma and brain tissue samples, using 20 µL of 0.4 µg/mL and 0.5 μg/mL internal standard solutions (lamotrigine-13C3,d3, dissolved in methanol-water, 50:50, v/v), respectively.
The molecular formula is C9H7Cl2N5.
Some synonyms include Lamotrigine-13C-d3, HY-B0495S, and DTXSID80849636.
The molecular weight is 262.09 g/mol.
Lamotrigine-13C3,D3 was created on May 22, 2013.
Lamotrigine-13C3,D3 was last modified on October 21, 2023.
The IUPAC name is 6-(2,3-dichloro-4,5,6-trideuteriophenyl)-(3,5,6-13C3)1,2,4-triazine-3,5-diamine.
The InChI is InChI=1S/C9H7Cl2N5/c10-5-3-1-2-4(6(5)11)7-8(12)14-9(13)16-15-7/h1-3H,(H4,12,13,14,16)/i1D,2D,3D,7+1,8+1,9+1.
The InChIKey is PYZRQGJRPPTADH-MKOZQUTQSA-N.
The canonical SMILES is C1=CC(=C(C(=C1)Cl)Cl)C2=C(N=C(N=N2)N).
The CAS number is 1246815-13-3.