·338·药学学报ActaPharmaceuticaSinica2011,46(3):338−343几种亲水凝胶骨架材料相关性质的比较聂淑芳1,2*,刘辉3,刘艳丽2,潘卫三2(1.武汉生物工程学院制药工程系,湖北武汉430415;2.沈阳药科大学药学院,辽宁沈阳110016;3.广州军区武汉陆军总院药剂科,湖北武汉430070)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(polyethyleneoxide,PEO)、海藻酸钠[sodiumalginate、低黏度NaAlg(L)、高黏度NaAlg(H)]和黄原胶(xanthangum,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。关键词:聚氧化乙烯;海藻酸钠;黄原胶;羟丙甲纤维素;骨架片中图分类号:R943文献标识码:A文章编号:0513-4870(2011)03-0338-06ComparisonofthecharacteristicsofseveralpolymermaterialsusedinhydrophilicmatrixtabletsNIEShu-fang1,2*,LIUHui3,LIUYan-li2,PANWei-san2(1.DepartmentofPharmaceuticalEngineering,WuhanBioengineeringInstitute,Wuhan430415China;2.DepartmentofPharmaceutics,ShenyangPharmaceuticalUniversity,Shenyang110016,China;3.DepartmentofPharmacy,ArmyGeneralHospitalofGuangzhouMilitaryRegion,Wuhan430070,China)Abstract:Pureanddrughydrophilicmatrixtabletswerepreparedbydirectcompressionmethodwiththeophyllineasamodeldrug.Thecharacteristicsoffourhydrophilicmatrixpolymers,hydroxypropylmethylcellulose(HPMC),polyethyleneoxide(PEO),sodiumalginate(NaAlg)andxanthangum(XG),werecomparedbyinvestigatingthewaterabsorption,swelling,erosionandgellayerstrength.ThesequenceofwaterabsorptionratewasXG>>NaAlg(H)>PEO>NaAlg(L)>>HPMC;ThesequenceofswellingindexwasXG>>PEO>>HPMC>>NaAlg;ThesequenceoferosionratewasNaAlg(L)>NaAlg(H)>>PEO80>PEO200>PEO300>XG≈PEO400≈K4M>K15M>PEO600≈K100M;ThesequenceofthegellayerstrengthwasPEO>HPMC>XG>>NaAlg.ForthePEOandHPMCmatrixtablets,withthepolymermolecularweightincreased,thedrugreleasemechanismwasgraduallytransferredfrommainlydependingontheerosiontothediffusion;forSALmatrixtablets,thedrugreleasemainlydependsonerosionmechanism;andforXGmatrixtablets,thedrugreleasemainlydependsonnon-Fickdiffusionmechanism.Comparisonoftheperformancedifferencebetweenthepolymermaterialswillcontributetorationaldesignandpredictionofdrugreleasebehaviorsfrommatrix收稿日期:2010-10-18.*通讯作者Tel:86-27-89648037,Fax:86-27-89649819,E-mail:niesf77@163.com聂淑芳等:几种亲水凝胶骨架材料相关性质的比较·339·tablesandultimatelytoachieveclinicalneeds.Keywords:polyethyleneoxide;sodiumalginate;xanthangum;hydroxypropylmethylcellulose;matrixtablet随着高分子材料学的发展,可供药用的新聚合物不断增加,其中亲水性聚合物应用最广,该类聚合物在水或消化液中能够膨胀,其特定的结构能保留水分并形成膨胀性水凝胶屏障而控制药物的释放。聚氧化乙烯(polyethyleneoxide,PEO)为白色易流动的高聚物,其结构为(CH2CH2O)n,是环氧乙烷经多相催化开环聚合而成的一种水溶性高分子均聚物,已被美国药典收载,目前广泛应用于双层渗透泵、凝胶骨架片以及生物粘附制剂等各类药物传递系统的开发与研究中[1,2]。国内有10～600万的聚氧化乙烯树脂...
