کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
2083782 | 1545361 | 2012 | 7 صفحه PDF | دانلود رایگان |

Enteric polymers such as cellulose esters (cellulose acetate phthalate, hydroxypropylmethylcellulose acetate succinate) and methacrylic acid–acrylate copolymers (Eudragit® L100-55 and S100) are quite brittle in the dry state and thus not suitable as pellet coatings for compression into tablets. The objective of this study was to investigate the role of humidity treatment for moisture plasticization in order to successfully compress the enterically coated pellets. The mechanical properties of Eudragit® L100-55 improved dramatically, while the properties of the other enteric polymers showed only minor changes after storage at higher humidity. The significant increase in flexibility of the Eudragit® L film was caused by hydration/plasticization; its elongation value changed from approx. 3% in the dry state to approx. 140% at the higher storage humidity. Storage at 84% relative humidity resulted in comparable release profiles of compressed and uncompressed pellets. The glass transition temperature of Eudragit® L films decreased below the compression temperature (room temperature) at storage humidities between 75% and 84%. The glass transition relative humidity leading to a change from the glassy to the rubbery state was determined by dynamic vapor sorption (DVS) to be 76.8%. Moisture resulted in superior plasticization for Eudragit® L than the conventional plasticizer triethyl citrate. The improved compressibility of high humidity treated Eudragit® L-coated pellets was also shown with single pellet compression data as indicated by an increased crushing force and deformation. In conclusion, moisture plasticization was a highly effective tool to enable the successful compression of pellets coated with the brittle enteric polymer Eudragit® L.
Moisture plasticization in the form of high humidity storage of the coated pellets prior to compression resulted in the decreasing puncture strength and increasing elongation of Eudragit® films with increasing moisture content. The damage to the Eudragit® L-coated pellets decreased with increasing storage humidity and storage time, as indicated by a lower increase in release upon compression.Figure optionsDownload high-quality image (101 K)Download as PowerPoint slide
Journal: European Journal of Pharmaceutics and Biopharmaceutics - Volume 81, Issue 1, May 2012, Pages 223–229