摘要
目的:应用连续动态的药物溶出仿生系统(drug dissolution si mulating system,DDSS)研究黄芩苷原料药及其普通片、缓释片、固体脂质纳米粒冻干粉等三种固体制剂的体外释放特性,为药物剂型设计研究提供新技术和新方法。方法:分别采用连续动态的DDSS和桨法体外释放度实验,对黄芩苷三种不同固体制剂进行体外释放度研究。以高效液相色谱法测定含量,用SPSS软件对数据进行模型拟合,从拟合方程中提取T50、Td、m等溶出参数,并对两种溶出系统的释药规律进行相关性评价。结果:黄芩苷普通片及其缓释片在两种溶出系统中释放特性分别都符合Weibull、Higuchi方程。分别对黄芩苷普通片及其缓释片在两种溶出系统中释放结果进行相关性评价,相关水平r值各为0.975、0.9995,均大于临界值(r4,0.01=0.917),即相关性良好。黄芩苷原料药和固体脂质纳米粒冻干粉在连续动态DDSS的释放特性均符合Weibull方程。结论:该DDSS模拟了一个连续动态的、更接近人体消化道环境的释药过程,其体外溶出度研究结果与《中华人民共和国药典》(2005年版二部)溶出度测定法(桨法)的良好相关性表明该DDSS作为评价药物固体制剂释药特性研究的合理性,为药物剂型设计研究提供了新的技术平台。
AIM： To study the release features of the baicalin crude drugs and three baicalin solid preparations such as ordinary tablets, sustained-release tablets and solid lipid nanopartitles by using a continuously dynamic drug dissolution simulating system （DDSS）, and to provide a new technology and a new method for the study of devising drug preparations. METHODS： The DDSS method and the oar method were used to study their release features of three different baicalin solid preparations, respectively. Furthermore, the high performance liquid chromatography method was used to determine the contents of baicalin. The data were fitted by SPSS software, and the dissolution parameters such as T50, Td, m were extracted from the fitting equations, and the correlation between the two systems were estimated. RESULTS： The release equations of the ordinary tablets and the sustained-release tablets of baicalin, in the two different systems, were Weibull and Higuchi equations, respectively. When the correlation of the release results of the baicalin tablets and the sustained-release tablets in the two different dissolution systems were evaluated, respectively, their corresponding correlational values were 0. 975 and 0. 9995, which were greater than the critical values （r4.0.01 = 0. 917）. It means they have a good correlation. The release features of the crude drugs and the solid lipid nanoparticles of baicalin on DDSS fit to Weibull CONCLUSION： The DDSS simulates equations a drug release course which is continuously dynamic and close to the gastrointestinal tract environment. The release feature results of DDSS and the oar methods embodied to Chinese Pharmacopoeia （edited in 2005） correlated well, which illustrated the reasonableness of the simulating systems to assess the release features of solid preparations. It provides a new technology platform to the study of devising drug preparations.
出处
《中国临床药理学与治疗学》
CAS
CSCD
2010年第1期11-20,共10页
Chinese Journal of Clinical Pharmacology and Therapeutics
基金
国家重大新药创制专项(2009ZX09304-002)
国家自然科学基金项目(30772778)
国际科技合作计划项目(2007DFC31670)
天津市自然科学基金项目(07JCYBJC18800)
国家高等学校博士学科点专项科研基金项目(200800630005)
国家中医药管理局中医药行业科研专项(200807051)
