CAJ | 학술논문

应用反相乳液分散－离子键合法，以戊二醛（ GD ）为交联剂制备负载拉米夫定的海藻酸钠／壳聚糖微球（ LAMV-SALG／CS）．利用拉米夫定的氨基与海藻酸钠的羧基形成弱酸弱碱盐键，使该药物被稳定包覆在微球内层，再以交联壳聚糖作为微球外层而形成具有核壳结构的复合微球．对微球的理化性质及释药性能进行表征及研究．结果表明，制备的LAMV-SALG／CS微球形貌规整，平均粒径约为2μm．测得微球载药质量分数为11.6％，药物包封率为70.3％；CS的活性氨基和戊二醛的羰基结合，形成交联网络，药物被包覆在微球中，且以单分子形式存在．体外模拟释放结果表明，微球释药性能良好，释药平缓，在酸性介质中累积释药率为27％时，其释药周期长达82 h；随制备微球时SALG浓度增大，药物释药速率减缓；在酸性介质中释药速率大于碱性介质；碱性介质合成的微球其释药速率快于弱酸性和弱碱性介质中合成的微球．
응용반상유액분산－리자건합법，이무이철（ GD ）위교련제제비부재랍미부정적해조산납／각취당미구（ LAMV-SALG／CS）．이용랍미부정적안기여해조산납적최기형성약산약감염건，사해약물피은정포복재미구내층，재이교련각취당작위미구외층이형성구유핵각결구적복합미구．대미구적이화성질급석약성능진행표정급연구．결과표명，제비적LAMV-SALG／CS미구형모규정，평균립경약위2μm．측득미구재약질량분수위11.6％，약물포봉솔위70.3％；CS적활성안기화무이철적탄기결합，형성교련망락，약물피포복재미구중，차이단분자형식존재．체외모의석방결과표명，미구석약성능량호，석약평완，재산성개질중루적석약솔위27％시，기석약주기장체82 h；수제비미구시SALG농도증대，약물석약속솔감완；재산성개질중석약속솔대우감성개질；감성개질합성적미구기석약속솔쾌우약산성화약감성개질중합성적미구．
With glutaraldehyde as cross-linking agent, LAMV-SALG/CS microspheres were prepared by means of the inverse emulsion dispersion and ionic bonding.The amino of lamivudine and carboxyl of sodium alginate can form weak salt bonds, so the drug can be stably wrapped in the inner layer of the microspheres, and then chitosan was crosslinked by glutaraldehyde to form the shell layer of the composite microspheres.The physicochemical prop-erties and the drug-release performances of the microspheres were investigated.The microspheres have a regular spherical shape and an average diameter of about 2μm.The drug mass content was 11.6%, and the drug encapsu-lation efficiency reached to 70.3%.The amino groups in chitosan combined with the carbonyl group in glutaralde-hyde to form the cross-linked network, and lamivudine have been enwrapped inside the microspheres.The drug-re-lease measurement results indicated that the microspheres have a satisfactory performance of releasing lamivudine at slow and steady rate.The drug release period corresponding to cumulative drug-release rate of 27%reached to 82 h in the acid medium.With the increase of the concentration of SALG, the releasing rate of lamivudine decreased. The releasing rate of lamivudine in acidic buffer was faster than in alkaline one.Drug-releasing rate of the micro-spheres prepared in the alkaline reaction medium was faster than that prepared in weak alkaline and acid ones.