Optimization of glycyrrhizic acid bile salt/phospholipid mixed micelles fast dissolving sublingual films by response surface method
10.7501/j.issn.0253-2670.2014.24.008
- Author:
Hong-Yan MIN
1
Author Information
1. Jiangxi University of Traditional Chinese Medicine
- Publication Type:Journal Article
- Keywords:
Bile salt/phosphatidylcholine mixed-micelles;
Box-Behnken response surface method;
Fast dissolving sublingual films;
Glycyrrhizic acid;
Sodium alginate;
Thin film dispersion method
- From:
Chinese Traditional and Herbal Drugs
2014;45(24):3543-3548
- CountryChina
- Language:Chinese
-
Abstract:
Objective: To prepare and optimize glycyrrhizic acid bile salt/phosphatidylcholine mixed-micelles fast dissolving sublingual films (GL-BS/PC-MM-FDSFs) and preliminarily evaluate its mucous membrane permeation in vitro. Methods: The formulations of GL-BS/PC-MM-FDSFs were optimized by employing Box-Behnken design-response surface methodology with the amounts of sodium alginate, propylene glycol, and GL-BS/PC-MM as investigation factors, and the disintegration time, cumulative release of drug from the GL-BS/PC-MM-FDSFs within 5 min, and particle size of reconstituted MM from GL-BS/PC-MM-FDSFs as indexes. Mucous membrane permeation test was evaluated in vitro with porcine sublingual mucosa as a model by using Franz diffusion cell. Results: The GL-BS/PC-MM-FDSFs prepared by optimized formulation (23 g/L sodium alginate, 148.5 g/L propylene glycol, and 7.58 mL GL-BS/PC-MM) could fast disintegrate in (22.1 ± 0.7) s, release in vitro at 5 min to (85.30 ± 2.91)%, and the particle size of reconstituted MM from GL-BS/PC-MM-FDSFs was obtained as (146.46 ± 6.42) nm. There was a little deviation between the theoretically predicted value and measured value. It showed that this model had a good prediction. There was no significant difference between the accumulative permeation profiles of GL-BS/PC-MM-FDSFs and GL-BS/PC-MM at each time point. Conclusion: The process that GL-BS/PC-MM is solidified to GL-BS/PC-MM-FDSFs is simple and feasible, and GL-BS/PC- MM-FDSFs could significantly improve the mucous membrane absorption of GL.