实时紫外成像研究氯霉素眼用原位凝胶的固有溶出特征  

Real-time UV imaging of chloramphenicol intrinsic dissolution characteristics from ophthalmic in situ gel

作　　者：陈建秀[1,2] 郭桢[2] 李海燕[2] 伍丽[1,2] 何仲贵[3] 胡容峰[1] 张继稳[1,2] 

机构地区：[1]安徽中医学院,安徽合肥230038 [2]中国科学院上海药物研究所,上海201203 [3]沈阳药科大学,辽宁沈阳110016

出　　处：《药学学报》2013年第7期1156-1163,共8页Acta Pharmaceutica Sinica

基　　金：国家自然科学基金资助项目(81273453);国家科技重大专项资助项目(2012ZX09301001-001)

摘　　要：本文以氯霉素为模型药物,采集氯霉素从原位凝胶中溶出过程的紫外实时成像谱图,从而测得氯霉素原位凝胶的固有溶出速率,考察处方因素和pH、泪液等生理因素对氯霉素原位凝胶固有溶出特征的影响。结果表明,随着泊洛沙姆浓度的增大,氯霉素温敏原位凝胶的固有溶出速率明显减小;加入增稠剂会降低氯霉素的固有溶出速率,其中以卡波姆影响最大;不同泪液稀释比例对胶凝温度影响较大,对氯霉素的固有溶出速率影响较小;不同pH条件下氯霉素固有溶出速率无明显变化。氯霉素pH敏原位凝胶在弱酸性及中性条件下溶出速率比弱碱性条件下慢。氯霉素原位凝胶的固有溶出特征与处方因素、生理因素存在一定的相关性。实时紫外成像测定所需样品量少、检测迅速,可用于眼用原位凝胶的药物释放特征评价。In this paper, chloramphenicol was selected as a model drug to prepare in situ gels. The intrinsic dissolution rate of chloramphenicol from in situ gel was evaluated using the surface dissolution imaging system. The results indicated that intrinsic dissolution rate of chloramphenicol thermosensitive in situ gel decreased significantly when the poloxamer concentration increased. The addition of the thickener reduced the intrinsic dissolution rate of chloramphenicol thermosensitive gel, wherein carbomer had the most impact. Different dilution ratios of simulated tear fluid greatly affected gel temperature, and had little influence on the intrinsic dissolution rate of chloramphenicol from the thermosensitive in situ gel. The pH of simulated tear fluid had little influence on the intrinsic dissolution rate of chloramphenicol thermosensitive in situ gel. For the pH sensitive in situ gel, the dissolution rates of chloramphenicol in weak acidic and neutral simulated tear fluids were slower than that in weak alkaline simulated tear fluid. In conclusion, the intrinsic dissolution of chloramphenicol from in situ gel was dependent on formulation and physiological factors. With advantages of small volume sample required and rapid detection, the UV imaging method can be an efficient tool for the evaluation of drug release characteristics of ophthalmic in situ gel.

关 键 词：原位凝胶 固有溶出速率 紫外实时成像 氯霉素 温敏原位凝胶 pH敏原位凝胶 

分 类 号：R943[医药卫生—药剂学] R917[医药卫生—药学]