1.药剂中使用辅料的目的
①有利于制剂形态的形成
②使制备过程顺利进行
③提高药物的稳定性
防止水解、氧化的措施:pH调节剂、抗氧剂、金属络合剂、将药物制成前体药物、将药物制成包合物/微囊/脂质体
④调节有效成分的作用或改善生理要求
缓释,控释,口感,外观,
2.辅料在药剂中的地位(只记最重要的内容)
①新辅料意味着新制剂、新剂型
>>脂质体——载体材料卵磷脂
>>微球、纳米粒——载体材料PLGA
>>缓控释制剂——骨架材料HPMC
>>透皮制剂——卡波姆
②辅料不同,剂型不同,疗效不同
>>速效制剂(注射剂、气雾剂)——起效快
>>缓、控释制剂——在体内维持时间较普通制剂长
辅料控制释放:定速(控释制剂零级恒速释药)、定时(脉冲制剂)、定位(靶向制剂、结肠定位制剂)
>>注射剂/气雾剂/舌下含片/透皮贴剂——避免肝脏首过效应、胃肠道pH及酶等对药物降解及药物对胃肠道的刺激,提高生物利用度
③辅料改变药物的理化性质
难溶性药物灰黄霉素+水溶性高分子材料PEG6000制成固体分散体,药物以微晶态、固态或不定型状态存在,溶解度提高,吸收快,生物利用度高。
④辅料增加制剂的可接受性
味道、外观
3.辅料举例
(1)液体药剂:表面活性剂、助悬剂、乳化剂——吐温、司盘、聚乳酸(PLA)、聚乳酸-聚乙醇酸共聚物(PLGA)
(2)固体药物:崩解剂、透皮吸收促进剂——羧甲基淀粉钠(CMS-Na)、交联聚维酮(PVPP)、交联羧甲基纤维素钠(CC-Na)、低取代羟丙基纤维素(L-HPC)、月桂氮酮(Azone)
3.辅料举例
(1)液体药剂:表面活性剂、助悬剂、乳化剂——吐温、司盘、聚乳酸(PLA)、聚乳酸-聚乙醇酸共聚物(PLGA)
(2)固体药物:崩解剂、透皮吸收促进剂——羧甲基淀粉钠(CMS-Na)、交联聚维酮(PVPP)、交联羧甲基纤维素钠(CC-Na)、低取代羟丙基纤维素(L-HPC)、月桂氮酮(Azone)
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【免费直播】6.20日2020年药学职称百天冲刺复习大作战!
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