【摘要】 以茶碱为模型药物,采用直接压片法制备亲水凝胶骨架片,从骨架片吸水性、膨胀性、溶蚀性及凝胶强度4个方面,全面比较了几种亲水凝胶骨架材料羟丙甲纤维素(hydroxypropylmethylcellulose,HPMC)、聚氧化乙烯(polyethylene oxide,PEO)、海藻酸钠[sodium alginate、低黏度NaAlg(L)、高黏度NaAlg(H)]和黄原胶(xanthan gum,XG)辅料性质和释药机制的差异。结果表明,吸水速率常数XG>>NaAlg(H)>PEO>NaAlg(L)>>HPMC;膨胀指数为XG>>PEO>>HPMC>>NaAlg;溶蚀速率NaAlg(L)>NaAlg(H)>>PEO80>PEO200>PEO300>XG≈PEO400≈K4M>K15M>PEO600≈K100M;凝胶层强度PEO>HPMC>XG>>NaAlg。对于PEO和HPMC骨架片,随着聚合物分子量增加,药物逐渐从以溶蚀机制为主的释放转移为以扩散机制为主的释放;对于NaAlg骨架片,药物主要以溶蚀机制释放;对于XG骨架片,药物主要以非Fick扩散机制释放。通过比较不同高分子材料之间的性能差异有助于合理设计和预测骨架系统中药物的释放速度,使其最终达到临床需要的体外释药行为。更多还原

【Abstract】 Pure and drug hydrophilic matrix tablets were prepared by direct compression method with theophylline as a model drug.The characteristics of four hydrophilic matrix polymers,hydroxypropylmethylcellulose(HPMC),polyethylene oxide(PEO),sodium alginate(NaAlg) and xanthan gum(XG),were compared by investigating the water absorption,swelling,erosion and gel layer strength.The sequence of water absorption rate was XG >> NaAlg(H) > PEO > NaAlg(L) >> HPMC;The sequence of swelling index was XG >> PEO >> HPMC >> NaAlg;The sequence of erosion rate was NaAlg(L) > NaAlg(H) >> PEO80 > PEO200 > PEO300 > XG ≈ PEO400 ≈ K4M > K15M > PEO600 ≈ K100M;The sequence of the gel layer strength was PEO > HPMC > XG >> NaAlg.For the PEO and HPMC matrix tablets,with the polymer molecular weight increased,the drug release mechanism was gradually transferred from mainly depending on the erosion to the diffusion;for SAL matrix tablets,the drug release mainly depends on erosion mechanism;and for XG matrix tablets,the drug release mainly depends on non-Fick diffusion mechanism.Comparison of the performance difference between the polymer materials will contribute to rational design and prediction of drug release behaviors from matrix tables and ultimately to achieve clinical needs.更多还原