CAJ | 학술논문

卡马西平%微胶囊%超临界制备%溶出性能%超临界流体注入%聚乳酸-羟基乙酸%聚乙二醇单甲醚-聚乳酸-羟基乙酸%差示扫描量热法%红外光谱分析卡馬西平%微膠囊%超臨界製備%溶齣性能%超臨界流體註入%聚乳痠-羥基乙痠%聚乙二醇單甲醚-聚乳痠-羥基乙痠%差示掃描量熱法%紅外光譜分析
잡마서평%미효낭%초림계제비%용출성능%초림계류체주입%취유산-간기을산%취을이순단갑미-취유산-간기을산%차시소묘량열법%홍외광보분석
carbamazepine%microcapsule%supercritical preparation%dissolution property%supercritical fluid impregnation%poly lactic-co-glycolic acid%methoxy polyethylene glycol-poly lactic-co-glycolic acid%differential scanning calorimetry%infrared spectroscopy

为提高卡马西平药物的溶出性能，基于超临界流体注入( SFI)技术，先后开展了聚乳酸-羟基乙酸( PLGA)、聚乙二醇单甲醚-聚乳酸-羟基乙酸( MPEG-PLGA)聚合物包裹卡马西平的微胶囊制备实验。结合差示扫描量热法和红外光谱分析，探讨了卡马西平在微胶囊中的形态及其与聚合物分子间的作用，同时实测了相应的药物体外溶出性能。结果表明：该文所制PLGA及MPEG-PLGA载药微胶囊中，卡马西平药物分子均呈无定形状态，均匀分散于包裹剂中；MPEG-PLGA载药微胶囊内药物与聚合物分子间有较强的相互作用，其塑性优于PLGA载药微胶囊；以MPEG-PLGA为聚合物基体的微胶囊的药物溶出速率明显高于单纯以PLGA为基体的微胶囊，且外加的MPEG分子量越小、相应PLGA中n( LA)：n( GA)越低越利于药物溶出速率的提高；为提高药物溶出速率，进行SFI时也可适当增加微胶囊的载药量，但不宜过高，当载药量从9.8%、28.3%升至35.8%时，卡马西平药物的溶出速率依次增大，但当载药量达45.2%时，对应微胶囊的溶出速率不升反降。
위제고잡마서평약물적용출성능，기우초림계류체주입( SFI)기술，선후개전료취유산-간기을산( PLGA)、취을이순단갑미-취유산-간기을산( MPEG-PLGA)취합물포과잡마서평적미효낭제비실험。결합차시소묘량열법화홍외광보분석，탐토료잡마서평재미효낭중적형태급기여취합물분자간적작용，동시실측료상응적약물체외용출성능。결과표명：해문소제PLGA급MPEG-PLGA재약미효낭중，잡마서평약물분자균정무정형상태，균균분산우포과제중；MPEG-PLGA재약미효낭내약물여취합물분자간유교강적상호작용，기소성우우PLGA재약미효낭；이MPEG-PLGA위취합물기체적미효낭적약물용출속솔명현고우단순이PLGA위기체적미효낭，차외가적MPEG분자량월소、상응PLGA중n( LA)：n( GA)월저월리우약물용출속솔적제고；위제고약물용출속솔，진행SFI시야가괄당증가미효낭적재약량，단불의과고，당재약량종9.8%、28.3%승지35.8%시，잡마서평약물적용출속솔의차증대，단당재약량체45.2%시，대응미효낭적용출속솔불승반강。
In order to improve the dissolution property of carbamazepine,corresponding experiments on producing microcapsule of carbamazepine wrapped by poly lactic-co-glycolic acid ( PLGA ) or methoxy polyethylene glycol-poly lactic-co-glycolic acid ( MPEG-PLGA ) are carried out using supercritical fluid impregnation ( SFI ) . The forms of carbamazepine in the polymer matrices and molecular interactions between carbamazepine and the polymers are characterized by differential scanning calorimetry and infrared spectroscopy. The dissolution of carbamazepine in vitro is determined. The results show that:for the microcapsule using PLGA or MPEG-PLGA to carry drug, the carbamazepine molecules present amorphous state and disperse evenly in the matrices;the molecular interaction between carbamazepine and MPEG-PLGA is strong, and the plasticity of MPEG-PLGA microcapsule is better than that of PLGA microcapsule;the drug dissolution rate of the MPEG-PLGA matrix is obviously higher than that of the PLGA matrix,and the drug dissolution rate increases with the decrease of molecular weight of the adscititious MPEG and n( LA):n( GA);the drug dissolution rate can be appropriately enhanced when the drug loading rises from 9 . 8%,28 . 3%to 35. 8%,when the drug loading reaches about 45. 2%,the drug dissolution rate begins to descend.