Revaprazan is a synthetic gastric acid-suppressing active pharmaceutical ingredient belonging to the potassium-competitive acid blocker (P-CAB) / reversible proton pump inhibitor class. It acts on the gastric H⁺/K⁺-ATPase and was developed for conditions associated with excessive gastric acid secretion. Revaprazan hydrochloride is the pharmaceutical salt form identified by FDA's substance registration system.
The free base Revaprazan has CAS Number 199463-33-7, molecular formula C22H23FN4, and molecular weight approximately 362.45 g/mol.
For pharmaceutical applications, Revaprazan Hydrochloride is particularly important. FDA identifies the hydrochloride as CAS 178307-42-1, formula C22H24ClFN4, and molecular weight 398.90 g/mol.
Revaprazan is chemically related to reversible acid-pump inhibition and differs mechanistically from conventional proton-pump inhibitors by competitively interacting with the potassium-binding site of the gastric H⁺/K⁺-ATPase. Revaprazan hydrochloride is also known by development code YH-1885.
Revaprazan hydrochloride is a crystalline material with documented polymorphism. Patent literature describes five crystalline forms, demonstrating that solid-state form is an important quality attribute for the hydrochloride API. Reported melting ranges differ among polymorphs, with crystalline Form I reported at 221–226°C and Form V at 210–218°C.
| Parameter | Revaprazan |
|---|---|
| Product Name | Revaprazan |
| Pharmaceutical Form | Revaprazan Hydrochloride |
| Synonym | YH-1885 |
| Free Base CAS Number | 199463-33-7 |
| Hydrochloride CAS Number | 178307-42-1 |
| Free Base Formula | C22H23FN4 |
| Hydrochloride Formula | C22H24ClFN4 |
| Hydrochloride Molecular Weight | 398.90 g/mol |
| API Type | Synthetic small molecule |
| Therapeutic Class | Potassium-competitive acid blocker / acid pump antagonist |
| Appearance | White to off-white solid/powder |
| Polymorphism | Five crystalline forms reported |
| Chirality | Racemic/undefined stereocenter |
| Melting Point | Form-dependent; approximately 210–226°C for reported polymorphs |
| Water Solubility | <0.1 mg/mL reported for hydrochloride in water |
FDA's substance record confirms the hydrochloride identity, while current analytical references report the white-to-off-white appearance and low aqueous solubility.
Revaprazan hydrochloride is a reversible acid-pump antagonist developed for suppression of gastric acid secretion. It has been investigated and used in relation to gastric-acid-associated disorders, including peptic-ulcer and gastritis-related conditions.
Potential pharmaceutical and development applications include:
Revaprazan hydrochloride requires particular attention to identity, assay, related substances, residual solvents, water content and crystalline form. The documented polymorphism of the hydrochloride makes solid-state characterization by techniques such as PXRD/XRPD particularly relevant.
Published patent data demonstrate high purity values above 99.9% for prepared crystalline forms during stability studies, but these values should not be represented as a universal pharmacopoeial release specification.
Analytical characterization can include:
A quality-focused Revaprazan API manufacturing process should control both chemical purity and the solid-state properties of the hydrochloride. The existence of five reported crystalline forms means that polymorphic-form control can be important for maintaining consistent API characteristics.
Manufacturing and analytical controls should therefore address:
Revaprazan hydrochloride should be packaged in a suitable, tightly closed pharmaceutical container and protected from moisture and contamination. Commercial analytical references recommend sealed storage away from moisture; one current reference specifies 4°C for storage of its analytical material.
Actual commercial API storage conditions should follow the validated stability data and approved product specification.
Typical Revaprazan API documentation can include:
Revaprazan hydrochloride has a technically important solid-state profile because multiple crystalline forms have been documented. Appropriate API quality control should therefore combine chemical analytical testing with solid-state characterization.
A quality-oriented Revaprazan API manufacturing program should emphasize:
| Parameter | Specification |
|---|---|
| Appearance | white to off-white crystalline powder |
| Identification | IR & HPLC compliant |
| Assay (HPLC) | NLT 98.0% by HPLC |
| Loss on Drying | NMT 0.5% |
| Residue on Ignition | NMT 0.1% |
| Individual Impurity | NMT 0.5% |
| Total Impurities | NMT 1.0% |
| Water Content | NMT 1.0% |