Moisture plasticization for enteric Eudragit庐 L30D-55-coated pellets prior to compression into tablets

详细信息	查看全文 | 推荐本文 |

• 作者：Soravoot Rujivipat^a ; ^b ; Roland Bodmeier^a ; ^{bodmeier@zedat.fu-berlin.de}
• 关键词：Coating ; Compression of coated pellets ; Enteric polymers ; Eudragit&reg ; L ; Mechanical properties ; Modified drug release
• 刊名：European Journal of Pharmaceutics and Biopharmaceutics
• 出版年：2012
• 期刊代码：16_09396411
• 类别：pha
• 出版时间：May, 2012
• 卷：81
• 期：1
• 页码：223-229
• 文件大小：451 K

摘要

Enteric polymers such as cellulose esters (cellulose acetate phthalate, hydroxypropylmethylcellulose acetate succinate) and methacrylic acid-acrylate copolymers (Eudragit庐 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庐 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庐 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庐 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庐 L than the conventional plasticizer triethyl citrate. The improved compressibility of high humidity treated Eudragit庐 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庐 L.