Drotaverine is a pharmaceutical active pharmaceutical ingredient (API) belonging to the antispasmodic class. It is a selective smooth-muscle relaxant used in pharmaceutical formulations for the management of painful spasms associated with various gastrointestinal, biliary and urinary tract conditions.
Drotaverine is a synthetic antispasmodic compound structurally related to papaverine. It produces smooth-muscle relaxation primarily through inhibition of phosphodiesterase type 4 (PDE4), resulting in increased intracellular cyclic AMP and reduced smooth-muscle contraction.
Drotaverine is a small-molecule pharmaceutical API used in the manufacture of oral and injectable formulations. It is commonly formulated as Drotaverine Hydrochloride for pharmaceutical applications.
Drotaverine acts primarily through inhibition of phosphodiesterase-4 (PDE4). This increases cyclic AMP levels in smooth-muscle cells and reduces calcium-dependent contraction, resulting in relaxation of spasmodic smooth muscle.
Drotaverine API is used in pharmaceutical formulations for symptomatic relief of smooth-muscle spasms associated with:
The exact indications depend on the approved pharmaceutical formulation and applicable regulatory labeling.
Drotaverine is generally described as a yellow to pale-yellow crystalline powder. It has limited water solubility, while its hydrochloride salt is more suitable for pharmaceutical formulation applications.
Drotaverine API intended for pharmaceutical manufacturing should be produced under appropriate GMP controls and tested according to applicable quality and regulatory requirements. Quality evaluation may include identification, assay, related substances, loss on drying, residual solvents, elemental impurities and other relevant quality attributes.
Drotaverine is an established pharmaceutical antispasmodic API used in the manufacture of formulations intended for the management of smooth-muscle spasms. Pharmaceutical manufacturers and formulation developers can evaluate Drotaverine based on applicable regulatory requirements, analytical documentation, quality specifications and batch-specific Certificate of Analysis.
| Parameter | Specification |
|---|---|
| Appearance | White to off-white crystalline powder |
| Identification | IR & HPLC compliant |
| Assay (HPLC) | 98.0% – 102.0% |
| Loss on Drying | NMT 1.0% |
| Residue on Ignition | NMT 0.5% |
| Heavy Metals | NMT 20 ppm |
| pH (1% Solution) | 2.0 – 4.0 |
| Individual Impurity | NMT 0.5% |
| Total Impurities | NMT 2.0% |
| Water Content | NMT 1.0% |
| Melting Point | 168°C – 172°C |
| Solubility | Practically insoluble in water; soluble in organic solvents |