Preparation of silybin controlled-release formulations and study on their release mechanism / 中草药

ABSTRACT

Objective: To prepare silybin (SLB) controlled-release formulations with the utilization of solid dispersion and effervescent technology and to study their release mechanism. Methods: To determine the optimal formulation and preparation of SLB controlled release formulations was by using single factor test depending on drug release in vitro. The similarity factor method was used to explore the release mechanism of the controlled release formulations prepared. Results: The SLB controlled release formulations cores were prepared using SLB-polyethylene glycol 6000 solid dispersion (1 2) as main drug, tartaric acid and sodium bicarbonate as effervescence, sodium carboxymethyl cellulose as blockers. The tablets were prepared using cellulose acetate as coating materials, polyethylene glycol 400 as porogen. SLB controlled release formulations released at a rate of zero-order. In the research on the release mechanism, the coating solution with/without porogen, tablet cores with/without blockers and effervescence had a significant impact on the drug release. On the contrary, the speed of the dissolution tester and the pH value of the release medium had no significant effect on the drug release. Conclusion: The preparation process of SLB controlled release formulations is simple. SLB controlled release formulations release with zero-order release in 12 h (r > 0.996 5).