Vol. 8, Issue 3 (2019)

Author(s):
Prasanthi D, Guvva Jagadish and K Lakshmi Aishwarya

Abstract:
The main objective of the study was to compare the effect of natural carriers and synthetic carriers in dissolution of fenofibrate (BCS class II), poorly soluble drug. Fenofibrate is an anti hyperlipidemic drug which reduces both cholesterol and triglycerides in the blood. Nowadays the formulation of poorly soluble compounds for oral delivery is the most frequent and greatest challenge to formulation scientists in pharmaceutical industry. There are many drugs for which dissolution poses a challenge for formulating oral dosage forms leading to bioavailability problems. To improve solubility of the drug, solid dispersions were prepared by different methods like physical mixture and kneading method with natural and synthetic carriers like agar, karaya gum, treated agar, modified karaya gum, PEG 4000 and PEG 6000 in the ratios of 1:2 to 1:10. Resultant formulations were evaluated for solubility, assay, flow properties, FTIR, X-ray diffraction, DSC and in vitro dissolution. Solubility of the solid dispersions was enhanced when compared to pure drug solubility (0.018 mg/ml). Natural gums, agar and karaya gum were modified and the swelling nature and viscosity of treated agar and modified karaya gum were less. Formulations with modified gums as carriers showed fast release (treated agar 87.56±1.40% release by K10 and modified karaya gum 93.73±1.35% release by K20) when compared to agar (79.46±1.37% release by K5) and karaya gum (82.16±1.37 % release by K15). When compared to natural carriers, synthetic carriers PEG 4000 (101.83±1.14% release in 60 mins by K25) and PEG 6000 (101.19±1.12% release in 30 minutes by K30) showed greater release. When compared to solid dispersions by physical mixture, kneading method formulations showed fast release. FTIR studies confirmed that there is no interaction between the drug and excipients. The solid state characterization of solid dispersion formulation by XRD and DSC studies confirmed that the drug present in the formulation was in an amorphous state. The optimized formulation was subjected to stability studies and was found to be stable. Hence, it can be concluded that solid dispersions of fenofibrate prepared by kneading method with synthetic carrier PEG 6000 are better in enhancing the dissolution rate.