Pregabalin is a synthetic active pharmaceutical ingredient belonging to the gabapentinoid class. It is the S-enantiomer of 3-(aminomethyl)-5-methylhexanoic acid and is structurally related to gamma-aminobutyric acid (GABA). Pregabalin is used in pharmaceutical formulations for indications including neuropathic pain and certain seizure disorders.
Pregabalin has the CAS Number 148553-50-8, molecular formula C₈H₁₇NO₂, and molecular weight 159.23 g/mol. The FDA Global Substance Registration System identifies Pregabalin with UNII 55JG375S6M.
The current USP monograph specifies 98.0–102.0% Pregabalin, calculated on the dried basis. The pharmacopoeial quality profile also controls residue on ignition, chloride, specified organic impurities, enantiomeric purity and loss on drying.
Pregabalin API is a chiral small-molecule pharmaceutical ingredient supplied for the manufacture of pharmaceutical formulations. The active substance is specifically the S-enantiomer, while the R-enantiomer is controlled as an enantiomeric impurity.
Pregabalin is generally described as a white to off-white crystalline powder. It is freely soluble in water and is used in pharmaceutical products in different oral dosage forms.
For pharmaceutical API quality control, identity is established using infrared spectroscopy and chromatographic retention time. USP assay is performed by liquid chromatography with UV detection at 205 nm.
Pregabalin is a chiral gamma-amino acid derivative with one stereogenic center. Its pharmaceutical activity is associated specifically with the S-enantiomer.
Chemical Name: (S)-3-(Aminomethyl)-5-methylhexanoic acid
CAS Number: 148553-50-8
Molecular Formula: C₈H₁₇NO₂
Molecular Weight: 159.23 g/mol
UNII: 55JG375S6M
ChEBI: CHEBI:64356
DrugBank: DB00230
API Type: Small-Molecule API
Pharmaceutical Class: Gabapentinoid
Therapeutic Class: Anticonvulsant / Neuropathic Pain Agent
Physical Form: White to off-white crystalline powder
Solubility: Freely soluble in water
PubChem confirms the molecular formula, molecular weight, CAS number and S-enantiomer identity of Pregabalin.
Pregabalin API is used in the manufacture of pharmaceutical formulations for several neurological and pain-related applications.
Its pharmaceutical applications include:
Pregabalin binds with high affinity to the α₂δ subunit of voltage-gated calcium channels and is pharmacologically distinct from classical GABA receptor agonists.
Quality control of Pregabalin API requires particular attention to assay, stereochemical purity and related organic impurities because Pregabalin is a chiral active substance.
The USP specification includes:
The USP enantiomeric-purity procedure specifically controls Pregabalin Related Compound A, which is the R-enantiomer.
Pregabalin API manufacturing requires careful control of stereochemistry, impurity formation and final API purity. Because Pregabalin is a chiral active substance, control of the undesired R-enantiomer is an important quality attribute.
A pharmaceutical-quality manufacturing process should incorporate controlled raw materials, validated process parameters, appropriate purification and validated analytical methods for assay, related substances and enantiomeric purity.
Finished Pregabalin API should be released against an established specification appropriate to the applicable pharmacopoeial and regulatory requirements.
Pregabalin should be preserved in tight containers, protected from light and stored at not more than 25°C, according to the USP monograph.
Suitable pharmaceutical-grade packaging should protect the API from moisture, light and other unsuitable environmental exposure during storage and transportation.
Recommended CMS storage wording:
Preserve in tight containers. Protect from light and store at a temperature not exceeding 25°C.
Pregabalin API documentation may include:
Documentation should correspond to the actual manufacturing batch and applicable quality specification.
Pregabalin is a well-established pharmaceutical API requiring strict control of assay, stereochemical purity, organic impurities, moisture and inorganic residue.
A quality-focused Pregabalin API manufacturing program should combine controlled manufacturing processes with validated analytical testing to maintain consistent batch quality. Particular attention to R-enantiomer control and related organic impurities helps ensure compliance with applicable pharmacopoeial requirements.
USP-aligned testing provides defined controls for assay, residue on ignition, related substances, enantiomeric purity and loss on drying, supporting pharmaceutical formulation and development requirements.
| Parameter | Specification |
|---|---|
| Appearance | white to off-white crystalline powder |
| Identification | IR & HPLC compliant |
| Assay (HPLC) | 98.0% – 102.0% |
| Loss on Drying | NMT 0.5% |
| Residue on Ignition | NMT 0.1% |
| Total Impurities | NMT 0.8% |