联苯双酯制剂的物理分散状态及体外释放度

用X-射线衍射法,考察不同载体制备的固体分散体系中联笨双酯的物理分散状态,聚乙二醇6000(PEG 6000)固体分散系为有限互溶固体溶液,聚乙烯吡咯烷酮(PVP)共沉淀物为无定形粉末,脲共熔物为简单低共熔混合物,热分析研究亦证实PEG 6000固体分散物较其相应比例的物理混合物及片剂有更高的分散度。比较两种联苯双酯片剂与滴丸的体外释放度,两种片剂的释放度参数td值分别为37和178min,滴丸未包衣者为11min,包衣者为26.in。由此可知物理分散状态是影响释放速度的主要因素。

THE DISSOLUTION RATE AND PHYSICAL DISPERSION STATE OF PREPARATIONS OF BIPHENYL DIMETHYL DICARBOXYLATE(DDB)

DDB is poorly soluble in water. The solid dispersions of DDB with easily soluble carriers such as polyethylene glycol 6000 (PEG 6000), polyvinyl pyrrolidone (PVP) and urea were prepared by melting and solvent methods.The two DDB--PEG 6000 systems are thermodynamically stable interstitial solid solutions. The DDB-PVP system is an amorphous precipitate and the DDB-urea system is a simple eutectic physical mixture judged by X-ray diffraction and thermal analysis methods. The dissolution rate of DDB-PEG 6000 pilule and two kinds of DDB tablets were determined. The dissolution rate of DDB-PEG 6000 pilule was found to be faster. The physical dispersion state is an important factor in relation to the dissolution rate of DDB preparations.