Study On Preparation And The Quality Evaluation Of Diclazuril Solid Dispersion

Solid dispersion is one of the strategies forced drug being at high disperdion state. Generally, drug particle diameter in solid dispersions was 0.001～0.1μm, mainly dispersed condition was molecularity, metastable amorphism and colloidal state.Diclazuril is a chemical substance synthesized from the benzeneacetonitrile class of compounds, developed successfully as anticoccidial agent for poultry, rabbits and sheep and is commercially available as a feed additive at a dose of 1 ppm in the feed in these hosts. Despite prophylactic administration of anticoccidials in the feed, there are many reports of coccidiosis occurring as a result of insufficient effective medication with conventional diclazuril formulation because its solubility problem. Thus effective therapeutic agents from water soluble formulation of diclazuril are required as supplements to current treatments or as alternatives to them.The objective of this thesis was to study the preparation, quality evaluation of solid dispersions with diclazuril as a model drug in details. There were four chapters in this thesis.Chapter one: A review was concerned with the application characteristics, the recent progress in solid dispersions, the varieties of carrier materials, and the preparing methods, the factors of effecting preparation, release mechanism and quality evaluation. The research objective and significance on diclazuril were introduced in brief.Chapter two: Developed a quantitative analysis method (HPLC) through preformulation. The analytical method was simple, with high sensitivity, specificity and recovery for the next studies of formulation and preparing technology.Chapter three: The impact factors of diclazuril solid dispersions on preparing technology were studied, such as the types and dosages of carrier materials and temperature etc. We ultimately selected the suitable diclazuril solid dispersions prescription and technology, and prepared ideal diclazuril solid dispersions.Chapter four: The quality evaluation of diclazuril solid dispersions was studied by apparatus in details, including X-ray diffraction and the release behavior in vitro, stability.