[Preparation of sinomenine hydrochloride delayed-onset sustained-release tablets].
OBJECTIVE
To prepare sinomenine hydrochloride delayed-onset sustained-release tablets.


METHODS
The tablets containing sinomenine hydrochloride were prepared by dry-compression coating technique with the ratio of HPMC in core tablet and the ratio of HPMC in coating film as the influence factors and the lag-time and release rate as the evaluation parameters. Experiments were done on the central composite design, the data were simulated by using multi-linear equation and second-order polynomial equation. The possibly optimal formulation was predicted by response surface method. The dissolution date (lag-time and release rate) of the tablets prepared under the optimum condition were compared with the predicted. The drug released mechanism of the tablet were studied by Model-fitted of drug released within 6-15 h with zero-order, Higuchi and Peppas equation, respectively.


RESULTS
The lag-time and release rate were simulated using second-order polynomial equation, regression coefficients of the two parameters were 0.9901 and 0.9876, respectively. Bias between the observed and predicted values of lag-time and release rate were -3.15% and -0.34%, respectively. The lag-time of the tablet prepared under the optimum condition in vitro was about 6 h, then drug released from the tablet within 6-15 h was found to conform to zero-order kinetics and was controlled by bulk erosion mechanism.


CONCLUSIONS
Sinomenine hydrochloride delayed-onset sustained-release tablets release drug slowly after lag time. The models developed in this study are proved to be highly predictable.
Zhang
Yu
Y
Institute of Materia Medica, Henan University, Kaifeng 475004, China. zy1219@henu.edu.cn
Geng
Yanna
Y
D002626:Chemistry, Pharmaceutical; D003692:Delayed-Action Preparations / Q000008:administration & dosage*; D016503:Drug Delivery Systems / Q000379:methods*; D005079:Excipients / Q000008:administration & dosage*; D009019:Morphinans / Q000008:administration & dosage*; D004364:Pharmaceutical Preparations / Q000008:administration & dosage; D013607:Tablets / Q000008:administration & dosage*; D013678:Technology, Pharmaceutical
D003692:Delayed-Action Preparations; D005079:Excipients; D009019:Morphinans; D004364:Pharmaceutical Preparations; D013607:Tablets; C009271:sinomenine