ABSTRACT
AIM To prepare colon-targeted pellets of Prunellae Spica effective components and to evaluate the in vitro drug-release behaviors.METHODS Fluidized bed coating method was adopted in the preparation of pellets.With in vitro accumulative release rate as an evaluation index,hydroxypropyl methyl cellulose (HMPC),polyacrylic resin (Eudragit S100) and triethyl citrate (TEC) amounts as influencing factors,orthogonal test was applied to optimizing the formulation.The in vitro drug-release behaviors were evaluated with rosmarinic acid content as an index.RESULTS The optimal formulation was determined to be 5％ for HPMC amount,70％ for Eudragit S100 amount,and 20％ for TEC amount.The obtained pellets attained an accumulative release rate of more than 90％ in pH 7.6 PBS (transportation for 2 h),while no drug dissolution was found in pH 1.0 HCl (transportation for 2 h) or pH 6.8 PBS (transportation for 3 h).CONCLUSION Colon-targeted pellets of Prunellae Spica effective components can achieve in vitro colon-targeted effect.
ABSTRACT
Objective: To prepare the pH dependent-microbially triggered colon targeted pellets of Rheum and optimize the preparation formulation of the targeted pellets. Methods: The pill-core was prepared by dropping preparation method, the pill-core fomulation was optimized by the orthogonal test, with drug loading, entrapment rate, and releasing rate as indexes. With release performance as index, the lagging cover weight increment was screened, the Rheum pellet that released at colon was obtained. Results: The 2% alginate-pectin solution, 0.7% chitosan solution, 1% CaCl2 solution, chitosan-CaCl2 solution with pH of 6.0, and the 4∶1 quantity of reagent (Rheum-accessory) were chosen as the top gallant fomulation to prepare the pill core, then enteric coating weight increased to 30% and the enteric coated-pellet was obtained. In gastric juice after 2 h and in small intestinal juice after 3 h, the coated pellet is cumulatively released to 2.01% and 8.72%, respectively, and released to 92.58% in the colon fluid after 4 h. Conclusion: The preparation fomulation of colon targeted pellet of Rheum is definited, and the colon targeted release is preliminary implemented.
ABSTRACT
Objective: To prepare pH-dependent Paridis Rhizoma saponin (PRS) and Astragali Radix polysaccharide (ARP) colon targeting pellets for the treatment of colon cancer and finish its in vitro release performance evaluation. Methods: The colon targeted pellets were prepared with extrusion-spheronization and air-flow coating method and the the process parameters were optimized by orthogonal design. The coating fluid prescription was investigated by single factor test. In vitro release performance evaluation of the pellets was evaluated with polyphyllin I and II as the indexes. Results: The optimum technologic parameters of extrusion spheronization equipment were as follows: the rate of extrusion was 60 r/min, the rate of spheronization was 1 200 r/min, and the time of spheronization was 5 min. The optimum coating liquid formulation of pH-dependent colon targetting pellets was 15% weight gains of Eudrugit S100, 1.5% anti-plastering aid amount of Glycerin monostearate, and 5% plasticizer amount of TEC. In vitro release test showed that cumulative release rate of berberine hydrochloride was close to 0% in artificial gastric juice after 2 h and less than 10% in artificial intestinal fluid after 4 h, but the cumulative release rate in artificial colon juice after 2 h was more than 90%. Conclusion: The preparation method can be applied to the preparation of colon targeted pellets and the pellets can achieve the targeted release in the colon.