Study Of Transdermal Delivery Of Cyclodextrin Inclusion Of Andrographolide With β-cyclodextrin

Andrographolide was used to treat colds, fever, infections and other diseases,which was contained by "Chinese Pharmacopoeia".In this paper, the inclusion complex of Andrographolide withβ-CD was prepared by saturated aqueous solution method.The formation of the inclusion complex were testifyed by FT-IR and X-ray spectra,and the phase solubility graph showed thatβ-cyclodextrin had effectly improved the solubility of Andrographolide,and the dissolution rate has developed a lot.The effect on percutaneous absorption of Andrographolide was investigated in vitro.These investigation proved bases for forther dosage study of Andrographolide.1. Determination of physical and chemical constants of Andrographolide In this paper,we have determied the solubility, drug oil/water distribution coefficient and the pKa values of drugs. The experimental results show that: pH have a greater impact on solubility and oill-water distribution coefficient of Andrographolide,both the solubility and the oil-water distribution coefficient perform larger in the neutral solution.In acidic and alkaline conditions,the solubility and oil-water distribution coefficient of Andrographolide were small. The pKa value of Andrographolide was 6.92.2. Preparation of Andrographolide andβ-cyclodextrin inclusion compoundIn this paper,Andrographolide-β-cyclodextrin inclusion compound was prepared by saturated aqueous solution method, respectively, and through the orthogonal test to optimize the preparation process, and IR, X-ray method were used to characterize the formation ofβ-cyclodextrin inclusion complex, and investigated the effect ofβ-cyclodextrin on dissolution of Andrographolide.The results show that molar ratio of Andrographolide/β-CD was 1:1,inclusion of time was 5h,inclusion temperature at 50℃, stirring speed at 400r.min-1, the encapsulation rate of Andrographoilde was 72.425%, inclusion compound yield for 67.54%; IR, X-ray method proved the formation of inclusion complex of Andrographolide withβ-cyclodextrin, the results proved thatβ-CD increased the solubility of andrographolide in vitro dissolution. 3.Effect ofβ-cyclodextrin on percutaneous absorption of AndrographolideIn this paper, we investagated the effect ofβ-cyclodextrin on percutaneous absorption of Andrographolide,The results showed thatβ-cyclodextrin effectively promoted Andrographolide percutaneous absorption, and after the formation of inclusion complex the percutaneous absorption of Andrographolide was better than physical mixtures, which showed thatβ-cyclodextrin was good percutaneous absorption enhancers.The study was supported by science and tachnology office of Jilin Province,it settles a good foundation for the study of new dosage of Andrographolide.