Formulation and Evaluation of Carvedilol Transdermal Patches by Using Hydrophilic & Hydrophobic Polymers

Author(s)

Oza, N. A., Patadiya, D. D., Patel, P. U., Patel, D. M.

Author's Affiliation

Abstract

Carvedilol is an antihypertensive drug use for management of Hypertension. It has the half-life of 6 hr and oral bioavailability of 25% due to first pass metabolism. The total daily dose of Carvedilol is 25 mg, hence it required frequent dosing. Transdermal patches of Carvedilol were prepared for sustained release and improve bioavailability of drug and patient compliance. Different formulations were prepared by varying the amount of HPMC-K4M and Eudragit RS-100 by solvent casting method. The prepared formulations were evaluated for various parameters like thickness, tensile strength, folding endurance, % elongation, % moisture content, % moisture uptake, % drug content, In-vitro drug release, In-vitro permeation and skin irritation study. A 3² full factorial design was applied to check the effect of varying the amount of Eudragit-RS 100 (X₁) and amount of HPMC-K4M (X₂) on the responses i.e. tensile strength and percentage drug released in 20 hr (Q₂₀) as dependent variables. Regression analysis and analysis of variance were performed for dependent variables. In-vitro release data were fitted to various models to ascertain kinetic of drug release. The best selected formulation is subjected to in-Vitro skin permeation and skin irritation study. Batch F₇ was considered optimum batch which contained 400 mg of Eudragit RS-100 and 600 mg of HPMC-K4M, showed release 95.73% up to 24 hr and was more similar to Zero order release kinetics (r²=0.982). Batch F₇ showed flux of 125.8 μg/2cm²/h, hence the patch area of 1.33 cm² would be expected to deliver targeted flux of 83.72μg/cm²/h.

Keywords

Carvedilol, Transdermal patch, Eudragit RL 100, Eudragit RS 100

Cite This Article

Oza, N. A., Patadiya, D. D., Patel, P. U., & Patel, D. M. (2013). Formulation and Evaluation of Carvedilol Transdermal Patches by Using Hydrophilic & Hydrophobic Polymers. International Journal for Pharmaceutical Research Scholars (IJPRS), 2(1), 151-162.