Optimization and stability study of the formulation of Rebamipide sustained-release tablets
- VernacularTitle:瑞巴派特缓释片的处方优选及稳定性考察
- Author:
Yueying HUANG
1
;
Jun BIAN
2
;
Leilei BAO
1
Author Information
1. Dept. of Pharmacy，the Third Affiliated Hospital of Naval Medical University，Shanghai 200438，China
2. Dept. of Pharmacy，the First Affiliated Hospital of Naval Medical University，Shanghai 200433，China
- Publication Type:Journal Article
- Keywords:
rebamipide;
sustained-release tablets;
formulation optimization;
central composite design -response surface method
- From:
China Pharmacy
2022;33(20):2514-2518
- CountryChina
- Language:Chinese
-
Abstract:
OBJECTIVE To optimize the formulation of Rebamipide sustained -release tablets and investigate its stability . METHODS On the basis of single factor investigation ，the central composite design -response surface method was adopted to optimize and validate the formulation using the dosage of hypromellose K 100M（HPMC K 100M）and poloxamer 188 as factors ， comprehensive scores （Y）of the in vitro cumulative release （Y0.5，Y2，Y6，Y10，Y12）of sustained -release tablets at 0.5，2，6，10 and 12 h ，correlation coefficient of in vitro cumulative release curve （R）and viscosity （N）as evaluation indexes . The stability of the optimized prescription was validated . RESULTS The optimized formulation was as follows ：rebamipide 150.0 mg，L-arginine 75.0 mg，poloxamer 188 65.6 mg（13.12%），HPMC K 100M 114.5 mg（22.90%），microcrystalline cellulose proper amount ，micro- powder silica gel 5 mg（1%），and the total prescription amount was 500 mg. According to 3 validation experiments ，the contents of rebamipide in sustained -release tablets were 100.61%，98.69% and 99.01%，respectively. The obtained sustained -release tablets released for 12 h continuously ，with in vitro cumulative release ≥90%，with good repeatability . The deviation between the real values and the predicted values of the 3 indicators Y，N and R were all less than 10%. In the stability tests ，light would silightly reduce the content after 10 days of storage at 25 ℃andrelativehumidity （90±5）%，the tablets expanded and split from the 5th day，and the release rate slowed down ；in high temperature ，accelerated and long -term stability tests ，the properties of the tablets have no significant changes ，and the content and in vitro cumulative release have no significant differences compared with the 0th day or 0th month . CONCLUSIONS Successfully optimized the formlation of Rebamipide sustained -release tablets . The sustained - release tablets obtained have sustained -release effect and should be stored in a dark place under dry conditions .
