Radhika Padarthy*1, Dr. M. Venkata Ramana2
1Research Scholar, Department of Pharmaceutics, JNTU Hyderabad, Telangana
2Principal, Gurram Balanarasaiah Institute of Pharmacy, Edulabad, Ghatkesar, Ranga Reddy – 501 301.
A B S T R A C T
The main objective of the current research was to improve the dissolution rate and solubility of an antihypertensive drug Olmesartan Medoxomil(OM) using cyclodextrin inclusion complexation and followed by converting to orally administerable tablets using a super disintegrants. OM is a BCS Class II drug having low solubility and high permeability. Inclusion complexes of OM were prepared by solvent evaporation method at the ratio of 1:1, 1:3 and 1:5 using different cyclodextrins such as α-cyclodextrin (α-CD), β-cyclodextrin(β-CD), Hydroxy Propyl β-cyclodextrin (HP-β-CD), Methylated β-cyclodextrin (M-β-CD) and γ-Cyclodextrin (γ- CD). Prepared inclusion complexes were characterized for their solubility and in-vitro drug release. It was observed that formulations prepared with M-β-CD at 1:5 ratio (OCD12) has shown faster drug release and higher solubility than other formulations. Hence, this formulation was converted to oral tablet using different superdisintegrants like sodium starch glycollate, croscarmellose sodium and soluplus. Tablets were prepared by direct compression method. From in vitro dissolution study of tablets, it was observed that the tablet formulation prepared with soluplus has shown faster drug release than marketed formulation and pure drug formulation. Hence, it can be concluded that the cyclodextrin inclusion complexation and further conversion to tablet using superdisintegrants is a good technique to improve the dissolution rate and solubility of poorly soluble BCS Class II drug such as OM.
Keywords: Olmesartan medoximil, Cyclodextrins, complexation, Methylated β-cyclodextrin