Andrographolide (AG) is a diterpene lactone present in Andrographis paniculata Nees. AG has an antimalarial activity, but the problem is its low aqueous solubility and low bioavailability after oral administration. Solid dispersions can be used to enhance the solubility of the poorly soluble drug. The solid dispersion of andrographolide (SAG) using carboxymethyl chitosan (CMChi) carriers with ratio 1:5 was prepared by solubilization and spray drying method. The objective of this research was to study the effect of solid dispersion of andrographolide forming to its bioavailability parameter(C_max, t_max, AUC). From the previous study, the DTA thermogram and X-Ray diffractogram of SAG showed a decreased in the melting point temperature and crystallinity of andrographolide. The solubility and the dissolution rate of SAG increased up to 2.2 times and 2.9 times, respectively. In vivo antimalarial activity on Plasmodium berghei infected mice also increased up to 2.14 time. This study revealed that the bioavailability of SAG increased significantly compared to andrographolide.

Keywords:  andrographolide, carboxymethyl chitosan, solid dispersions, bioavailability