A novel formulation for solubility and content uniformity enhancement of poorly water-soluble drugs using highly-porous mannitol
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- 作者：Morteza Saffari ; morteza.saffari@sydney.edu.au" class="auth_mail" title="E-mail the corresponding author ; Amirali Ebrahimi ; Timothy Langrish
- 关键词：Adsorption ; Poorly water-soluble drug ; Templating process ; High-porosity mannitol ; Indomethacin ; Nifedipine
- 刊名：European Journal of Pharmaceutical Sciences
- 出版年：2016
- 出版时间：15 February 2016
- 年：2016
- 卷：83
- 期：Complete
- 页码：52-61
- 全文大小：1362 K
文摘
The present study investigates the enhancement of the dissolution rates for poorly-water soluble drugs by a new adsorption method. The results show that the current adsorption method enhanced the dissolution rate of both nifedipine and indomethacin to a significant extent by nano-confinement of drugs into the pore spaces of highly-porous excipients. Porous mannitol particles with a surface area and pore volume of 6.3 ± 0.1 m2 g− 1 and 0.036 ± 0.002 ml g− 1, respectively, were drug loaded in two different concentrations of indomethacin and nifedipine. The results of drug loading for nifedipine showed an increase from 3.2 ± 0.1% w/w for a 0.08 M drug solution to 9.1 ± 0.3% w/w drug loading for a 0.16 M drug solution, while indomethacin had slightly better performance for the adsorption process, with 4.1 ± 0.2% w/w and 12.6 ± 0.4% w/w for 0.08 M and 0.16 M concentrations of indomethacin, respectively, in the final formulation. This result also indicated highly-uniform blends with a percentage relative standard deviation of less than 4% for drug-loaded mannitol in both nifedipine and indomethacin. This method gave a significant enhancement of the dissolution rate for both drugs due to nano-confinement of drugs into porous excipients and high solubility of porous mannitol, with 80% drug release within the first 15 min for the drug-loaded samples.