药物固体分散体和其磷脂载体的热力学分析-thermodynamic analysis of drug solid dispersion and its phospholipid carrier.docx

Study on the thermodynamic properties of drug solid dispersions and its phospholipid carriersAbstractThe hydrophobic property of flavonoids limits their solubility in solution, dissolution rate and bioavailability. To improve their medicine efficience, some pharmaceutical techniques have been developed, for example the solid dispersion method and phospholipid complexes formation method. During the pharmaceutical preparation process, the physical properties of the drug-carrier complexes will determine the medicine efficience directly. The thermodynamic properties of drug-carrier complexes measured by thermal analysis technique will provide valuable information for the pharmaceutical research and preparation techniques.In this work, the thermodynamic properties of solid dispersions of flavonoids, (quercetin and silybin), and its phospholipid carriers have been studied extensively. The effect of temperature, composition, and preparation conditions on the physical properties and on the mixing state of drug and carriers, have been considered. This study will provide valuable information for the pharmaceutical techniques. This work includes following details.In chapter 2, we report the study on the binary mixtures of (quercetin + PEG 6000). The phase transition state and the heat capacity (cp) of binary system have been measured by a differential scanning calorimeter (DSC). The effect of composition on the mixing state has been analyzed. To separate the effect of PEG melting on cp, the DSC curves were divided into two sections. In the first section, for temperatures range from 298 to 353 K, the variation of the melting properties with composition was concerned. With the increase in w1, (the mass fraction of quercetin), the temperature (Tfus/K) and enthalpy (?fush/J·g-1) offusion are decreased. This indicates that, the binary system is of the character of solidmixture/or solid dispersion in this temperature range. In the second section for temperatures ranges from 353 to