Hibiscus Rosa-Sinesis Leaves Polysaccharide as Solubility Enhancing Agent for Poorly Soluble Drug

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The main purpose of this research was to use hydrophilic Hibiscus Rosa-sinesis (HRS) dry leaves mucilage as functionality solubility enhancing agent for the design and development of solid dispersion of the drug Telmisartan (TS) to formulate tablets and to study its in vitro quality control tests. The mucilage was extracted, isolated, purified and prepared solid dispersions with different ratio of drug: mucilage (1:0.5, 1:1.0, 1:1.5, 1:2.0 and 1:2.5) using solvent evaporation method and another. Two formulations were prepared using drug: mucilage ratio of 1:1.0 as co-grinding method (GM) and physical mixture (PM). The solubility study showed a significant enhancement in the aqueous solubility of the drug where the solubility rate was increased with the increment in ratio of the mucilage. The formulation giving the best solubility enhancement of Telmisartan in aqueous media was in the order of SD > GM > PM > API. Then, the dispersions were compressed into tablets where it passed the precompression and post-compression evaluation parameters. Swelling index increased as the amount of mucilage added to each formulation (SD1 to SD3). Nevertheless as the amount of mucilage is increased for formulation SD4 and SD5 (1:2.0 and 1:2.5 ratio of drug: mucilage) the swelling index were decreased. The in-vitro dissolution study revealed that there is marked decrease in the dissolution rate of Telmisartan for all the solid dispersion containing tablets when compared to Telmisartan API tablets. This proves with the increase in mucilage ratio, the drug release from the solid dispersion tablet got retarded because of the formation of highly viscous barrier layer at the interface of the tablet and dissolution medium. In conclusion, the solubility of the drug has been greatly enhanced by the solid dispersion technique incorporating HRS mucilage using solvent evaporation method. Therefore, it is suggested that the drug Telmisartan can be converted to solid dispersion using Hibiscus Rosa-sinesis dry leaves mucilage as solubility enhancing agent and the solid dispersion granules can be filled in capsules as a dosage form.