Mosapride API is a gastroprokinetic pharmaceutical active ingredient used in medicines intended to improve gastrointestinal motility. Mosapride is a selective 5-HT4 receptor agonist that promotes the release of acetylcholine from the gastrointestinal nerve plexus, thereby supporting gastrointestinal movement and gastric emptying. Unlike dopamine D2 receptor antagonists, mosapride's pharmacological activity is primarily associated with serotonin 5-HT4 receptor stimulation.
The pharmaceutical substance is commonly used in the form of Mosapride Citrate Hydrate, also described as mosapride citrate dihydrate. The Japanese Pharmacopoeia identifies Mosapride Citrate Hydrate with the chemical formula C₂₁H₂₅ClFN₃O₃·C₆H₈O₇·2H₂O, molecular weight 650.05 g/mol, and CAS number 636582-62-2. The corresponding anhydrous mosapride citrate has a molecular weight of 614.02 g/mol.
Mosapride itself has the molecular formula C₂₁H₂₅ClFN₃O₃, molecular weight 421.89 g/mol, and CAS number 112885-41-3. It is a racemic substance containing equimolar R- and S-mosapride. The chemical name is 4-amino-5-chloro-2-ethoxy-N-[[4-[(4-fluorophenyl)methyl]morpholin-2-yl]methyl]benzamide.
According to the Japanese Pharmacopoeia, Mosapride Citrate Hydrate occurs as a white to yellowish-white crystalline powder. It is freely soluble in N,N-dimethylformamide and acetic acid, sparingly soluble in methanol, slightly soluble in ethanol, and practically insoluble in water. A solution in N,N-dimethylformamide shows no optical rotation.
The JP XVIII monograph establishes a quantitative requirement of 98.5% to 101.0% of mosapride citrate, calculated on the anhydrous basis. It also specifies identification through ultraviolet absorption spectrophotometry, infrared spectrophotometry and a qualitative citrate reaction. These analytical characteristics provide a recognized pharmacopoeial basis for identity and quality assessment of Mosapride Citrate Hydrate.
For purity testing, the Japanese Pharmacopoeia specifies a heavy-metal limit of not more than 20 ppm and provides a liquid-chromatographic procedure for related substances. Under the monograph, the specified impurity at a relative retention time of approximately 0.47 is limited to three times the reference peak response, individual other specified peaks are limited to the reference peak response, and total peaks other than mosapride are limited to five times the reference peak response. These correspond to approximately NMT 0.3%, NMT 0.1% for individual other impurities, and NMT 0.5% total related substances, when interpreted against the monograph's reference-solution dilution.
Mosapride API is therefore relevant to pharmaceutical formulation and manufacturing applications involving gastrointestinal motility products. For API procurement, formulation development and quality control, analytical testing should be performed according to the applicable pharmacopoeial monograph, approved specification and batch-specific Certificate of Analysis.
The water content for Mosapride Citrate Hydrate is specified at 11.0–13.0% in the Japanese Pharmacopoeia, reflecting its hydrated form. Residue on ignition is specified at not more than 0.1%. These values should not be confused with generic specifications for anhydrous mosapride citrate or mosapride free base.
| Parameter | Specification |
|---|---|
| Appearance | White crystalline powder or crystals |
| Identification | IR & HPLC compliant |
| Assay (HPLC) | NLT 98.0% by HPLC |
| Loss on Drying | 11.0–13.0% |
| Residue on Ignition | NMT 0.5% |
| Heavy Metals | NMT 20 ppm |
| Individual Impurity | NMT 0.5% |
| Total Impurities | ≤ 1.5% |
| Water Content | 11.0–13.0% |