Pregabalin

Pregabalin

Pregabalin is a GABAergic anticonvulsant and depressant of the central nervous system (CNS). It is a close structural analogue of the inhibitory neurotransmitter γ-aminobutyric acid (GABA). Pregabalin binds with high affinity to the α2δ subunit-containing voltage-gated calcium channels (VDCC). It increases extracellularGABA concentrations in the brain by producing a dose-dependent increase in L-Glutamic acid decarboxylase (GAD), the enzyme responsible for GABAsynthesis.

Pregabalin (PGB, PGL, PGN), marketed under the brand name Lyrica among others, is a medication used to treat epilepsy, neuropathic pain, fibromyalgia, andgeneralized anxiety disorder. Its use for epilepsy is as an add-on therapy for partial seizures with or without secondary generalization in adults. Some off-label uses of pregabalin include restless leg syndrome, prevention of migraines, social anxiety disorder, and alcohol withdrawal. When used before surgery it does not appear to affect pain after surgery but may decrease the use of opioids.

1 DESCRIPTION A White to off-white crystlline powder
2 IDENTIFICATION
a)IR The IR sprectrum of the sample conform to that of standard
b) HPLC The retention time of the sample peak should conform to that of standard in enantiomeric
3 X-RAY POWDER DIFRACTION PATTERN To match with the working standard
4 ENANTIOMERIC PURITY
PRB-IV :(R-)-(-)3-Aminomethyl-5-methyl hexanoic acid (R-Isomer)
NMT 0.5%
5 RELATED COMPOUNDS
- - Purity
- - Identified impurity
   - PRB-I : (R)-(-)-3- Carbamoylmethyl-5-methyl- hexanoic acid
   - PRB-II : 3-Isobutyl glutaric acid
   - PRB-III : 4 -Isobutyl- pyrrolidin-2-one
   - Largest unidentified impurity
   - Total impurity

NLT 99.0%

NMT 0.15%
NMT 0.15%
NMT 0.15%
NMT0.10%
NMT1.0%
6 ASSAY 98.0% - 102.0% ( on anhydrous basis and solvent free basis)
7 RESIDUAL SOLVENT
a) Ethanol
b) Isopropyl alcohol
c) Isobutyl alcohol
d) Ethyl acetate
e) Chloroform
f) Triethylamine

NMT 5000 PPM
NMT 5000 PPM
NMT 5000 PPM
NMT 5000 PPM
NMT 60 PPM
NMT 320 PPM
8 WATER CONTENT NMT 0.5%
9 RESIDUE ON IGNITION NMT 0.1%
10 HEAVY METALS NMT 20 ppm