盐酸尼卡地平单层渗透泵片的制备及其体外释放行为的考察  

Preparation of Nicardipine Hydrochloride Monolithic Osmotic Pump Tablets and Its in Vitro Release Behavior

作　　者：马锐[1] 王洪亮[1] 刘玉玲[1] 夏学军[1] 董武军[1] 

机构地区：[1]北京协和医学院&中国医学科学院药物研究所,北京市100050

出　　处：《中国药房》2011年第21期1967-1969,共3页China Pharmacy

摘　　要：目的:制备盐酸尼卡地平(Nic)单层渗透泵片,提高难溶性药物溶解度,实现平稳释药。方法:以吸水速率、渗透压及Nic溶解度为指标,从柠檬酸、氯化钠、乳糖和甘露醇中筛选适当的渗透压促进剂,制备Nic单层渗透泵片,并考察其体外释放行为,拟合释药模型。结果:4种渗透压促进剂中,以柠檬酸所制片剂吸水速率较高(71.83mg·h-1),渗透压值最高,可使Nic溶解度(7.90mg·mL-1)提高约10倍(80.33mg·mL-1);以柠檬酸为渗透压促进剂制备的渗透泵片,其24h药物累积释放度在95%以上,且符合零级释药模型。结论:柠檬酸能显著提高Nic溶解度;以柠檬酸为渗透压促进剂制备的Nic单层渗透泵片可平稳释药,且24h内基本释放完全。OBJECTIVE：To prepare the monolithic osmotic pump tablets of nicardipine hydrochloride（Nic） which can enhance the dissolution and make a good performance on its’ releasing profile. METHODS：Using absorbing rate,osmotic pressure and the solubility of Nic as index,the optimal osmotic pressure accelerator was selected among critic acid,sodium chloride,lactose and mannitol to prepare Nic monolithic osmotic pump tablets. The drug release behavior of Nic monolithic osmotic pump tablets was investigated and drug release mode was fitted. RESULTS：Among 4 kinds of osmotic pressure accelerator,citric acid had high absorbing rate（71.83 mg·h-1） and osmotic pressure,the dissolubility of Nic in citric acid（80.33 mg·mL-1） was ten times than it in water（7.90 mg·mL-1） . Accumulative release rate of Nic monolithic osmotic pump tablets which was prepared using citric acid as osmotic pressure accelerator was more than 95% within 24 h and accorded with zero order kinetics equation. CONCLUSION：Citric acid can improve the solubility of Nic significantly. Nic monolithic osmotic pump tablets which were prepared using citric acid as osmotic pressure accelerator can release in full during 24h.

关 键 词：盐酸尼卡地平 单层渗透泵片 柠檬酸 溶解度 渗透压促进剂 体外释放 

分 类 号：R943[医药卫生—药剂学] R972[医药卫生—药学]