Tiagabine Hydrochloride is the hydrochloride salt of tiagabine, a synthetic anticonvulsant and selective gamma-aminobutyric acid (GABA) reuptake inhibitor. It is an important pharmaceutical API used in the development and manufacture of medicines for epilepsy.
Tiagabine Hydrochloride has the molecular formula C20H26ClNO2S2 and a molecular weight of 412.02 g/mol. Its CAS number is 145821-59-6. The free-base active moiety, tiagabine, has CAS number 115103-54-3 and a molecular weight of approximately 375.6 g/mol.
Tiagabine is a nipecotic acid derivative containing two substituted thiophene rings and a piperidine carboxylic acid structure. The hydrochloride salt is the pharmaceutical form recognized by the USP monograph and used in the marketed drug product.
USP specifies Tiagabine Hydrochloride at 97.5–102.5% on an anhydrous basis and includes chromatographic controls for multiple specified impurities and total impurities.
Tiagabine Hydrochloride is chemically identified as (3R)-1-[4,4-bis(3-methylthiophen-2-yl)but-3-enyl]piperidine-3-carboxylic acid hydrochloride.
The molecule contains a stereogenic center corresponding to the R configuration of the active tiagabine molecule. Its hydrochloride form provides the salt form used for pharmaceutical development and manufacture.
FDA's chemistry documentation describes Tiagabine Hydrochloride as a white to off-white powder with no essentially detectable odor. The material has measurable aqueous solubility and is also soluble in several organic solvents.
Tiagabine selectively inhibits the GABA transporter GAT-1, thereby reducing the reuptake of GABA into presynaptic neurons and increasing the availability of GABA in the synaptic cleft.
The resulting increase in GABAergic inhibitory activity contributes to its anticonvulsant pharmacological effect.
Tiagabine Hydrochloride is used as the active pharmaceutical ingredient in anticonvulsant medicines.
The FDA-approved Gabitril formulation contains tiagabine hydrochloride and was developed for adjunctive treatment of partial seizures in appropriate patients. FDA labeling identifies the active ingredient as tiagabine hydrochloride and provides tablet strengths of 2 mg, 4 mg, 12 mg and 16 mg.
The API is therefore relevant to pharmaceutical manufacturing and development programs involving antiepileptic and GABAergic medicines.
Tiagabine Hydrochloride requires comprehensive pharmaceutical quality testing in accordance with applicable pharmacopoeial and regulatory requirements.
Important analytical parameters include:
The USP monograph specifies an assay range of 97.5–102.5% calculated on the anhydrous basis and total impurities of not more than 1.0%. Its chromatographic method controls several named impurities as well as unknown impurities.
Swapnroop Drugs and Pharmaceuticals is a WHO-GMP certified pharmaceutical company engaged in pharmaceutical APIs and pharmaceutical raw materials for domestic and international markets.
Tiagabine Hydrochloride API can be evaluated against USP requirements, customer-specific specifications and applicable regulatory requirements. Product quality documentation and analytical information can be provided according to the intended pharmaceutical application and destination market.
Tiagabine Hydrochloride should be protected from light and stored in appropriately closed pharmaceutical containers.
The USP monograph specifies preservation in tight, light-resistant containers and storage at a temperature not higher than 30°C.
Technical documentation for Tiagabine Hydrochloride API may include:
Swapnroop Drugs and Pharmaceuticals operates as a WHO-GMP certified pharmaceutical company with a portfolio of pharmaceutical APIs and pharmaceutical raw materials.
For Tiagabine Hydrochloride API requirements, customers can request product specifications, analytical documentation, packaging information and commercial details according to their pharmaceutical development, manufacturing and regulatory requirements.
| Parameter | Specification |
|---|---|
| Appearance | white to off-white crystalline powder |
| Identification | IR & HPLC compliant |
| Assay (HPLC) | 97.5–102.5% |
| Loss on Drying | NMT 0.5% |
| Residue on Ignition | NMT 0.2% |
| Individual Impurity | NMT 0.5% |
| Total Impurities | NMT 1.0% |
| Water Content | NMT 0.5% |
| Melting Point | −38° to −42° |