目的研究柠檬酸三乙酯(triethyl c itrate,TEC)在奥美拉唑肠溶微丸中的应用。方法分别比较包衣中含TEC和不含TEC对Eudragit L30D-55膜(尤特奇肠溶包衣材料)性质的影响和对奥美拉唑肠溶微丸释药及其表面衣膜质量的影响。结果含10%TEC的Eu...目的研究柠檬酸三乙酯(triethyl c itrate,TEC)在奥美拉唑肠溶微丸中的应用。方法分别比较包衣中含TEC和不含TEC对Eudragit L30D-55膜(尤特奇肠溶包衣材料)性质的影响和对奥美拉唑肠溶微丸释药及其表面衣膜质量的影响。结果含10%TEC的Eudragit L30D-55膜较不含TEC的Eudragit L30D-55膜的玻璃化转变温度(Tg)值降低19.75℃;含10%TEC和含5%TEC的肠溶微丸释放度分别为98.7%和82.6%,远远高于不含TEC的微丸。结论TEC能显著改善树脂类包衣材料的Tg,提高膜的柔韧性和完整性,并且能够有效地控制药物释放,可广泛应用于制剂包衣中。展开更多
Changes in structure of oral solid dosage forms(OSDF) elementally determine the drug release and its therapeutic effects.In this research,synchrotron radiation X-ray micro-computed tomography was utilized to visualize...Changes in structure of oral solid dosage forms(OSDF) elementally determine the drug release and its therapeutic effects.In this research,synchrotron radiation X-ray micro-computed tomography was utilized to visualize the 3 D structure of enteric coated pellets recovered from the gastrointestinal tract of rats.The structures of pellets in solid state and in vitro compendium media were measured.Pellets in vivo underwent morphological and structural changes which differed significantly from those in vitro compendium media.Thus,optimizations of the dissolution media were performed to mimic the appropriate in vivo conditions by introducing pepsin and glass microspheres in media.The sphericity,pellet volume,pore volume and porosity of the in vivo esomeprazole magnesium pellets in stomach for2 h were recorded 0.47,1.55 × 10^(8)μm^(3),0.44 × 10^(8)μm^(3)and 27.6%,respectively.After adding pepsin and glass microspheres,the above parameters in vitro reached to 0.44,1.64 × 10^(8)μm^(3)0.38 × 10^(8)μm^(3)and 23.0%,respectively.Omeprazole magnesium pellets behaved similarly.The structural features of pellets between in vitro media and in vivo condition were bridged successfully in terms of 3 D structures to ensure better design,characterization and quality control of advanced OSDF.展开更多
基金financial support from National Key R&D Program of China(2020YFE0201700)Major New Drugs Innovation and Development(2017ZX09101001-005,China)+1 种基金the National Natural Science Foundation of China(81803441,81803446 and 81773645)Youth Innovation Promotion Association CAS(2018323,China)。
文摘Changes in structure of oral solid dosage forms(OSDF) elementally determine the drug release and its therapeutic effects.In this research,synchrotron radiation X-ray micro-computed tomography was utilized to visualize the 3 D structure of enteric coated pellets recovered from the gastrointestinal tract of rats.The structures of pellets in solid state and in vitro compendium media were measured.Pellets in vivo underwent morphological and structural changes which differed significantly from those in vitro compendium media.Thus,optimizations of the dissolution media were performed to mimic the appropriate in vivo conditions by introducing pepsin and glass microspheres in media.The sphericity,pellet volume,pore volume and porosity of the in vivo esomeprazole magnesium pellets in stomach for2 h were recorded 0.47,1.55 × 10^(8)μm^(3),0.44 × 10^(8)μm^(3)and 27.6%,respectively.After adding pepsin and glass microspheres,the above parameters in vitro reached to 0.44,1.64 × 10^(8)μm^(3)0.38 × 10^(8)μm^(3)and 23.0%,respectively.Omeprazole magnesium pellets behaved similarly.The structural features of pellets between in vitro media and in vivo condition were bridged successfully in terms of 3 D structures to ensure better design,characterization and quality control of advanced OSDF.
