Sustained-release formulation of sarpogrelate hydrochloride

Area of Science:

• Pharmaceutical Sciences
• Drug Delivery Systems
• Pharmacokinetics

Background:

• Sarpogrelate hydrochloride (SGL) is an anti-platelet agent used to prevent thrombosis and vascular smooth muscle cell proliferation.
• Current formulations require frequent administration, impacting patient compliance.
• Developing a sustained-release formulation is crucial for improving therapeutic outcomes.

Purpose of the Study:

• To investigate the bioavailability and release characteristics of a novel sustained-release solid dispersion (SR-SD) formulation of Sarpogrelate HCl (SGL).
• To evaluate the potential of the SR-SD formulation for once-daily administration.
• To optimize drug release profiles for extended therapeutic effect.

Main Methods:

• SR-SD formulations of SGL were prepared using a hot-melt coating technique with waxy materials (Compritol 888 ATO, stearyl alcohol) and hydroxypropyl methylcellulose (HPMC K 15).
• Dissolution profiles and pharmacokinetic parameters (AUC, Tmax) were assessed and compared to SGL powder.
• The impact of varying drug-to-polymer ratios and HPMC concentrations on drug release was analyzed.

Main Results:

• Compritol 888 ATO demonstrated initial control over SGL release.
• Incorporation of HPMC further prolonged drug release up to 24 hours, with increased HPMC concentrations reducing the release rate due to gel layer formation.
• Pharmacokinetic studies revealed increased AUC and Tmax for the SR-SD formulation compared to SGL powder, indicating enhanced bioavailability and sustained drug exposure.

Conclusions:

• The developed SR-SD formulation effectively achieves sustained release of Sarpogrelate HCl for 24 hours.
• The formulation shows potential for improving the therapeutic efficacy and convenience of SGL treatment.
• This study supports the development of a once-daily SGL formulation, enhancing patient compliance and therapeutic outcomes.