A Novel Surfactant-Free Lipid-Based Formulation for Improving Oral Bioavailability of Loratadine Using Colloidal Silicon Dioxide as Emulsifier and Solid Carrier

作者：Huang, Ri; Tan, Yonggang; Shen, Lao; Wang, Tao; Quan, Dongqin^*

来源：Current Pharmaceutical Biotechnology, 2018, 19(3): 217-223.

DOI：10.2174/1389201019666180509094812

• Lipid-based formulation
• Loratadine
• colloidal silicon dioxide
• CSD
• bioavailability
• morphology

Background: The purpose of this study was to develop an innovative surfactant-free lipid-based formulation (LF) for improving oral bioavailability of loratadine based on using solid particles colloidal silicon dioxide (CSD) as emulsifier and solid carrier.
Methods: Loratadine was dissolved in oil solution with the aid of co-solvent and LF formulations were prepared by a simple adsorption and milling technique. The LF Powder was evaluated in terms of angle of repose and X-ray powder diffraction. After dispersing and emulsifying in water, the particle size and morphology were also characterized. In vitro dissolution and pharmacokinetic behavior in vivo were also studied.
Results: Orthogonal design indicated that the amount of CSD in formulations had a major and significant influence on emulsification. The optimal formulation showed LF with good flowability and without crystallization or deposition of loratadine in it.
Conclusion: After dispersing in water, an emulsion with the mean droplet size of 1.21 mu m was obtained. Although the dissolution of drug from LF was slower in vitro in acidic aqueous solution, pharmacokinetic studies in vivo showed that the bioavailability of loratadine increased 2.49-fold by CF compared to a commercial tablet.

• 出版日期2018
• 单位中国人民解放军军事医学科学院; 天津中医药大学