Preparation and Characterization of TPGS‐Colloidal Silica Microparticles for Enhancement of Solubility and Oral Bioavailability of Lercanidipine Hydrochloride

Bulletin of the Korean Chemical Society

Sol Ha¹  Soo Kim¹  hwan Baek²  In‐³  Min‐⁴  Eun‐⁴ 

[1] 735 Korea;736 Republic of Korea;College of Pharmacy Kyungsung University Busan 608‐College of Pharmacy Pusan National University Busan 609‐

关键词: Oral absorption;    Lercanidipine;    Dissolution;   

DOI  :  10.1002/bkcs.10746

学科分类：化学（综合）

来源: Korean Chemical Society

【 摘 要 】

In this study, colloidal silica microparticles containing solubilizing excipient were prepared using the spray‐drying process to enhance dissolution and oral absorption of lercanidipine hydrochloride. Several measurements including scanning electron microscopy, powder X‐ray diffraction, particle size determination, in vitro dissolution, and pharmacokinetic study were conducted in rats. Among the tested solubilizing excipients, d‐α‐tocopheryl polyethylene glycol 1000 succinate (TPGS) dramatically enhanced the solubility of lercanidipine hydrochloride through micelle solubilization. In addition, TPGS‐colloidal silica microparticles at the ratio of 11010 (drugTPGScolloidal silica) showed rapid dissolution rate in all dissolution media and displayed higher area under the curve and maximum plasma concentration values compared with raw lercanidipine hydrochloride. Therefore, amorphous TPGS‐colloidal silica microparticles fabricated using the spray‐drying process have great potential in the clinical application of lercanidipine hydrochloride.

【 授权许可】

Unknown