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Glimepiride/hydroxypropyl-β-cyclodextrin inclusion compound: preparation, characterization, and evaluation.
Xin Quan1, Shurui Wang1, Jiamin Lu1
1Key Laboratory for Green Pharmaceutical Technologies and Related Equipment of Ministry of Education, College of Pharmaceutical Sciences, Zhejiang University of Technology, Hangzhou, China.
Drug Development and Industrial Pharmacy
|March 13, 2025
Summary
This study enhanced glimepiride (GM) solubility and bioavailability using a hydroxypropyl-β-cyclodextrin (HP-β-CD) inclusion compound prepared by ball milling. The novel formulation significantly improved drug release and pharmacokinetic profiles.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Physical Chemistry
Background:
- Glimepiride (GM) exhibits poor solubility and bioavailability, limiting its therapeutic efficacy.
- Developing advanced formulations is crucial for improving GM's oral administration and patient outcomes.
Purpose of the Study:
- To prepare and characterize a glimepiride/hydroxypropyl-β-cyclodextrin (GM/HP-β-CD) inclusion compound using optimized ball milling.
- To evaluate the in vitro and in vivo performance of the novel GM/HP-β-CD inclusion compound.
Main Methods:
- Response surface methodology was employed to optimize ball milling parameters for GM/HP-β-CD inclusion compound formation.
- Characterization involved powder x-ray diffraction, DSC, SEM, and FTIR; stability, in vitro dissolution, and in vivo pharmacokinetic studies were conducted.
Main Results:
- Optimized ball milling yielded a stable GM/HP-β-CD inclusion compound with 20x higher solubility and 12.7x faster dissolution than GM.
- In vivo studies demonstrated a 3.5x increase in maximum plasma concentration and significantly enhanced bioavailability, with a shortened Tmax.
Conclusions:
- The GM/HP-β-CD inclusion compound prepared by ball milling shows improved solubility, dissolution, stability, and bioavailability.
- This formulation holds potential for sustained-release glimepiride delivery, reducing dosing frequency and improving patient compliance.
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