Author(s): Jitendra Banweer*1, Subhash Pandey2, A. K. Pathak1
Journal: Drug Invention Today
ISSN 0975-7619
Volume: 2;
Issue: 2;
Start page: 134;
Date: 2010;
Original page
Keywords: Transdermal system | Lisinopril dihydrate | anti-hypertensive | penetration enhancers | matrix dispersion | Iso propyl alcohol | Oleic acid.
ABSTRACT
The Lisinopril dihydrate (angiotensin converting enzyme inhibitor) is lysine derivative of enalaprilat and does not require hydrolysis to exert pharmacological activity. It is given orally; suffer severely from hepatic first pass metabolism resulting in bioavailability of 6-60%. To overcome the poor bioavailability of the drug, transdermal patches have been prepared. The present study also aims at optimization of the formulation by incorporating the penetration enhancers in different concentration and ratios. The patches were prepared employing Hydroxy propyl methyl cellulose (HPMC) & Polyvinyl alcohol (PVA) in 1:1 ratio as polymeric matrix using glycerol as plasticizer in 6% concentration. Binary solvent system (Water: Methanol) in the ratio of 70: 30 was taken for the study. The Transdermal devices were fabricated on glass substrate using solvent casting technique. Iso propyl alcohol (IPA) & Oleic acid (OA) were added as the penetration enhancers individually and in blend in different concentrations and ratios. Various physico-chemical evaluatory parameters were carried over prepared patches to ascertain their integrity and physical stability at normal and accelerated temperature conditions.Optimization of the penetration enhancer’s concentration and ratio was done by performing in-vitro diffusion rate studies using Keshary-Chein diffusion cell on Goatskin. The best results in terms of C.P.R. obtained individually through OA & IPA patches were 54% & 70.65% respectively at the highest concentration (15 %) of enhancer employed individually. But when the blend of enhancers is used in lowest concentration of 5 %, they produce the C.P.R. of 84.33 %, which clearly dictates the synergistic effect of the enhancers if used in combination. The rate of drug permeation further increases on increasing the concentration of blend from 5 to 15 %. The drug release from the patches follows Higuchi’s kinetics and gives a linear relation between q (amount released) vs t1/2 (time).
Journal: Drug Invention Today
ISSN 0975-7619
Volume: 2;
Issue: 2;
Start page: 134;
Date: 2010;
Original page
Keywords: Transdermal system | Lisinopril dihydrate | anti-hypertensive | penetration enhancers | matrix dispersion | Iso propyl alcohol | Oleic acid.
ABSTRACT
The Lisinopril dihydrate (angiotensin converting enzyme inhibitor) is lysine derivative of enalaprilat and does not require hydrolysis to exert pharmacological activity. It is given orally; suffer severely from hepatic first pass metabolism resulting in bioavailability of 6-60%. To overcome the poor bioavailability of the drug, transdermal patches have been prepared. The present study also aims at optimization of the formulation by incorporating the penetration enhancers in different concentration and ratios. The patches were prepared employing Hydroxy propyl methyl cellulose (HPMC) & Polyvinyl alcohol (PVA) in 1:1 ratio as polymeric matrix using glycerol as plasticizer in 6% concentration. Binary solvent system (Water: Methanol) in the ratio of 70: 30 was taken for the study. The Transdermal devices were fabricated on glass substrate using solvent casting technique. Iso propyl alcohol (IPA) & Oleic acid (OA) were added as the penetration enhancers individually and in blend in different concentrations and ratios. Various physico-chemical evaluatory parameters were carried over prepared patches to ascertain their integrity and physical stability at normal and accelerated temperature conditions.Optimization of the penetration enhancer’s concentration and ratio was done by performing in-vitro diffusion rate studies using Keshary-Chein diffusion cell on Goatskin. The best results in terms of C.P.R. obtained individually through OA & IPA patches were 54% & 70.65% respectively at the highest concentration (15 %) of enhancer employed individually. But when the blend of enhancers is used in lowest concentration of 5 %, they produce the C.P.R. of 84.33 %, which clearly dictates the synergistic effect of the enhancers if used in combination. The rate of drug permeation further increases on increasing the concentration of blend from 5 to 15 %. The drug release from the patches follows Higuchi’s kinetics and gives a linear relation between q (amount released) vs t1/2 (time).
