The Study On Increasing In Solubility Of Andrographolide And The Preparation Of Andrographolide Dispersible Tablets

The solid dispersion and the cyclodextrin inclusion and the ultra-fine powder technique were used to increase Andrographolide's solubility and the Andrographolide dispersible tablets were prepared in this paper. The experimental results follow as:The Andrographolide solid dispersion was produced by solvent evaporation method. The effect of the amount of the carrier (PVPk30) and the surfactant (Tween 80) and the evaporation tempture on the solubility of the Andrographolide solid dispersion was investigated by orthogonal design. The optimization process was Andro:PVP: surfactant=1: 9: 1.5. The amorphous Andrographolide was found in the Andrographolide solid dispersion by SEM and X-Ray diffraction spectra. The ratio of surfactant and PVPk30 was the key factor and the best range of surfactant is 5%～13%.Theβ-CD-Andro inclusion was prepared by pH regulation. The results of SEM and the dissolution test showed that the smallestβ-CD-Andro inclusion crystal and the highest solubility ofβ-CD-Andro were obtained when the molecular ratio ofβ-CD to Andro is 3:1. The PVPk30 was effective in improving the dissolution ofβ-CD-Andro and the PEG is no work on that ofβ-CD-Andro.The ultra-fine particles of Andrographolide was prepared by Jet grinding mill, the average size of particle was 13.5um. The accumulated dissolution rate of ultra-fine powder within 5min reached 96% that is three time as large as that of Andrographolide. Comparing the dissolution rate of solid dispersion, cyclodextrin inclusion and ultrafine, we can find the ultra-fine powder technique was simple and low cost. Then the Andrographolide ultrafine powder as raw materials was used to prepare the dispersible tablets.The process of the prescription of Andrographolide dispersible tablet is determined by orthogonal design. The optimal prescription is Andrographolide 33.3%, surfactant 1.5%, within disintegrant 10%, foreign disintegrant 1.5%, sweetener 50.7%, magnesium stearate 2%, talc 1%. The range of tablet hardness is 4～8kg. Foreign Disintegrant have the greatest impact on disintegration time. With the the amount of surfactant increasing, the release of Andrographolide from Andrographolide dispersible tablet was improved.