摘要
目的利用固体分散技术改善环孢素A(CsA)的溶解性能,提高其体外溶出速率。方法以Poloxamer188为载体,溶剂熔融法制备不同比例组成的环孢素A固体分散体,考察体外溶出速率及不同转速和不同溶出介质对溶出的影响,并配合X-射线粉末衍射分析药物在载体中的存在状态。对溶出度结果用Weibull分布模型进行拟合,计算体外溶出主要参数td和t50,并进行方差分析。结果CsA在药物-载体比例为1:4或1:6的固体分散体中呈非晶态。固体分散体的溶出速率与相应物理混合物及原料药间存在极显著差异(P<0.01),溶出介质对药物溶出无显著性影响(P>0.05)。结论制成固体分散体能显著提高CsA的溶出速率。
OBJECTIVE: To improve the dissolution rate of cyclosporine A. METHODS: Solid dispersion system of CsA in Poloxamer188 was prepared at various weight ratios by solvent-melting method. The effects of carriers ratios, different dissolution media and rotational speeds on dissolution rate were studied. The parameters of t50 and td were calculated using Weibull model. Statistical significance were analyzed using ANOVA. X-ray power diffractometry was used to determine the state of CsA in the preparation. RESULTS: When the drug-carrier ratio was 1:4 or 1:6, CsA existed as non-crystal. The dissolution rates of CsA in solid dispersion were obviously raised in vitro. Drug release was not influenced by the dissolution media. CONCLUSION: CsA-Poloxamer188 solid dispersion can increase the dissolution rate of CsA significantly.
出处
《中国药学杂志》
EI
CAS
CSCD
北大核心
2005年第10期760-762,共3页
Chinese Pharmaceutical Journal
关键词
环孢素A
固体分散体
溶出度
高效液相色谱法
Dispersions
Dissolution
High performance liquid chromatography
Mathematical models
Rotation
Solvents
Weibull distribution
X ray powder diffraction
