基于液固压缩技术的伊曲康唑速释制剂分析-analysis of itraconazole rapid release preparation based on liquid-solid compression technology.docxVIP

AbstractThus far, about 40% of promising pharmacological active substances have bioavailability problem due to their poor solubility, which restricts the development of new drugs to a certain extent. Many common technologies are available today for dissolution rate enhancement, but these involve high production cost, sophisticated machinery, complicated technologies, intellectual property issues, and advanced preparation methods. However, the emergence of liquisolid technology overcomes these barriers.It has been proved that the liquisolid technology can significantly increase the solubility of water-insoluble drugs, improving the bioavailability, especially for the low dose water-insoluble drugs.However, In order to have acceptable flowability and compactability for liquisolid powder formulation, high levels of carrier and coating materials should be added and that in turn will increase the weight of each tablet which is very difficult to swallow, formulation of the high dose insoluble-drugs as liquisolid tablets is one of the limitations of the liquisolid technique. Also,few research of the liquisolid technology has been reported, especially for the study of its solubilization mechanism, and the conclusion is not consistent. Therefore, further research and exploration of the solubilization mechanism in liquisolid technology is necessary.As a broad-spectrum antimicrobial agent, itraconazole has a superiority in low minimum bacteriostatic concentration, high security and good efficacy, but the water-insolubility reduce its clinical pharmacological effects. More over,during the preparation process of itraconazole pellet,huge amounts of dichloromethane is needed to dissolve the drugs and HPMC, this process need high -level equipment and cause pollution.There are also some reports about self-emulsifying formulation and solid dispersion technique,but both of them have a complex preparation process and low yield.In order to solve the problem above, this research use itra