Abstract

DESIGN, DEVELOPMENT AND OPTIMIZATION OF TELMESARTAN BY USING SOLID DISPERSION TECHNIQUES

Haribansh Narayan Singh*, Abhishek Kumar Saxena and Rohit Kumar

Abstract

Solubility studies showed a significant, linear increase in the aqueous solubility of the Telmisartan with increasing concentration of β-CD, maximum concentration of β-CD (15mM/L) so improvements in the saturation solubility of Telmisartan. An inclusion complex of Telmisartan with β-CD was prepared successfully by the physical mixing, kneading, solvent evaporation and fusion methods in the molar ratio of 1:1. This was confirmed by FTIR and XRD studies. The complex of Telmisartan with β-CD & PEG-6000 prepared successfully by the physical mixing, kneading, solvent evaporation and fusion methods in the molar ratio of 1:1. This was confirmed by FTIR and XRD studies. With the present investigations it can be concluded that solubility of poorly soluble drug Telmisartan can be enhanced effectively using solubility enhancement approaches such as solid dispersion. The results obtained proved that in vitro dissolution of both the drugs was improved after solubility enhancement as compared to pure drug and marketed tablet. Pharmacokinetic data proved the hypothesis of improvement in bioavailability proving that developed formulations have better oral absorption than the conventional dosage form and pure drug. Hence the developed formulations have scope of better patient compliance and therapeutic efficacy. These in all five methods employing kneading method using methanolwater as solvent employing exhibited the fastest and highest in vitro dissolution rate when compared to the tablet of pure telmisartan, and during stability study there was very slight decrease in its dissolution profile. These findings are extremely important from a commercial point of view as the prepared complexes removes drawback of a poor dissolution profile of Telmisartan and stability.

Keywords: Telmisartan, FTIR and XRD studies.