Sarpogrelate API is a pharmaceutical active ingredient primarily supplied in the form of Sarpogrelate Hydrochloride. Sarpogrelate is a serotonin receptor antagonist with particular activity at the 5-HT2A receptor and is associated with inhibition of serotonin-mediated platelet aggregation and vascular smooth-muscle responses. The hydrochloride salt is the established pharmaceutical form and is identified by CAS Number 135159-51-2. The Japanese Pharmacopoeia recognizes Sarpogrelate Hydrochloride as an official pharmaceutical substance with an assay requirement of 98.5–101.0% on an anhydrous basis.
Sarpogrelate Hydrochloride is a synthetic small-molecule drug substance belonging to the serotonin receptor antagonist class. It is also known by development code MCI-9042 and the trade name Anplag. The API has the molecular formula C24H31NO6·HCl and a molecular weight of 465.97 g/mol. It occurs as a white crystalline powder and is slightly soluble in water and ethanol (99.5), while it dissolves in dilute hydrochloric acid. The Japanese Pharmacopoeia also notes that Sarpogrelate Hydrochloride exhibits crystal polymorphism, making solid-state characterization an important aspect of pharmaceutical quality control.
Sarpogrelate works by antagonizing serotonin-mediated 5-HT2 receptor activity. Serotonin can contribute to platelet aggregation and vascular constriction, while Sarpogrelate can reduce these responses through receptor blockade. The pharmaceutical ingredient has therefore been developed for cardiovascular and peripheral vascular applications, particularly conditions associated with arterial circulation and platelet-related vascular responses.
Its pharmacological profile has also resulted in research interest in vascular complications associated with diabetes, peripheral arterial disease and other disorders involving impaired microcirculation. Product indications should always be determined according to the applicable national regulatory approval and approved product labeling.
Sarpogrelate Hydrochloride is the hydrochloride salt of Sarpogrelate, a hemisuccinate derivative. The free active moiety has CAS Number 125926-17-2, while the pharmaceutical hydrochloride salt is CAS 135159-51-2. FDA GSRS identifies Sarpogrelate Hydrochloride under UNII FQN8N8QP1B, and PubChem identifies the substance as a 1:1 hydrochloride salt.
The API is characterized by UV and infrared identification procedures, chromatographic assay and related-substance testing. The Japanese Pharmacopoeia specifies HPLC-based assay and controls water content and residue on ignition. Related substances are also controlled chromatographically, reflecting the importance of degradation-product monitoring for this pharmaceutical ingredient.
Quality evaluation of Sarpogrelate Hydrochloride includes identity testing, assay, related substances, water determination and residue on ignition. The current JP specification requires 98.5–101.0% assay calculated on an anhydrous basis. Water is limited to not more than 0.5%, while residue on ignition is limited to not more than 0.1%.
The JP analytical procedure uses liquid chromatography for assay and related-substance evaluation. The monograph also specifies system-suitability requirements for chromatographic performance. These controls are useful for ensuring consistency of API quality during pharmaceutical manufacturing.
Sarpogrelate Hydrochloride API intended for pharmaceutical manufacturing should be supported by appropriate analytical documentation, including Certificate of Analysis, identification results, assay data, related-substance profile, water determination and residue-on-ignition results. Manufacturing controls should also address polymorphic form, residual solvents and process-related impurities where applicable.
Sarpogrelate Hydrochloride should be protected from environmental factors that could affect its chemical and physical quality. The Japanese Pharmacopoeia specifies storage in tight containers. Appropriate packaging should be selected according to the validated stability profile, moisture sensitivity and intended transportation conditions.
Typical pharmaceutical API documentation can include a Certificate of Analysis, specification sheet, analytical method information, stability data, residual-solvent information, impurity profile, safety documentation and applicable regulatory or GMP documentation.
Sarpogrelate Hydrochloride has a defined pharmacopoeial identity and analytical framework, including a verified JP assay range of 98.5–101.0% on an anhydrous basis. Its established chromatographic testing, controlled water content and residue-on-ignition requirements make it suitable for quality-focused pharmaceutical API sourcing and manufacturing applications.
| Parameter | Specification |
|---|---|
| Appearance | white to off-white crystalline powder |
| Identification | IR & HPLC compliant |
| Assay (HPLC) | 98.0% – 102.0% |
| Residue on Ignition | NMT 0.1% |
| Individual Impurity | NMT 0.10% |
| Total Impurities | NMT 0.50% |
| Water Content | NMT 0.5% |