Preparation and in vitro quality evaluation of self-microemulsion co-loaded with tenuifolin and β-asarone.
10.19540/j.cnki.cjcmm.20200922.301
- Author:
Ting ZHANG
1
;
Jing WANG
2
;
Bao-de SHEN
2
;
Jun-Jun ZHU
2
;
Li-Qiang WANG
3
;
Hai-Long YUAN
4
Author Information
1. School of Medicine, Huaqiao University Quanzhou 362021, China Department of Pharmacy,Air Force Medical Center Beijing 100142, China.
2. Department of Pharmacy,Air Force Medical Center Beijing 100142, China.
3. School of Medicine, Huaqiao University Quanzhou 362021, China.
4. Department of Pharmac,Air Force Medical Center Beijing 100142, China.
- Publication Type:Journal Article
- Keywords:
Box-Behnken response surface methodology;
in vitro quality evaluation;
pseudo-ternary phase diagram;
self-microemulsion;
tenuifolin;
β-asarone
- MeSH:
Anisoles;
Biological Availability;
Diterpenes, Kaurane;
Drug Delivery Systems;
Emulsions;
Particle Size;
Solubility;
Surface-Active Agents
- From:
China Journal of Chinese Materia Medica
2020;45(24):5988-5995
- CountryChina
- Language:Chinese
-
Abstract:
To prepare and optimize the self-microemulsion co-loaded with tenuifolin and β-asarone(TF/ASA-SMEDDS) and evaluate its quality. The prescription compositions of TF/ASA-SMEDDS were screened by solubility test, single factor test and pseudo-tern-ary phase diagram, and the prescriptions were further optimized by Box-Behnken response surface method, with the drug loading and particle size as the evaluation indexes. Then the optimized TF/ASA-SMEDDS was evaluated for emulsified appearance, particle size, morphology and drug release in vitro. The optimized prescription for TF/ASA-SMEDDS was as follows: caprylic citrate triglyceride polyoxyethylene castor oil-glycerol(10.8∶39.2∶50), drug loading of(5.563±0.065) mg·g~(-1) for tenuifolin and(5.526±0.022) mg·g~(-1) for β-asarone; uniform and transparent pan-blue nanoemulsion can be formed after emulsification, with particle size of(28.84±0.44) nm. TEM showed that TF/ASA-SMEDDS can form spherical droplets with a uniform particle size after emulsification; In vitro release test results showed that the drug release rate and cumulative release of tenuifolin and β-asarone were significantly improved. The preparation process of TF/ASA-SMEDDS was simple and can effectively improve in vitro release of tenuifolin and β-asarone.
