Abstract

*Bhatia Anirudh (Research Scholar) and Khalid Mohammed

ABSTRACT

Labetalol HCl is an antihypertensive medication used to treat hypertension. Its oral bioavailability is only 25% due to first-pass metabolism, and it has a half-life of 6 hours. Given the 100mg maximum daily dose, frequent dosing was required. To enhance bioavailability and improve patient compliance, Labetalol HCl transdermal patches were developed. Different formulations were created by adjusting the proportions of HPMC, Methyl Cellulose, and PVP using the solvent casting method. These formulations were evaluated for various factors, including weight variation, patch thickness, folding durability, drug content, moisture absorption and loss rates, and in-vitro drug release. A chemical compatibility study of Labetalol HCl with the polymers was conducted using FTIR Spectrometry, confirming that there was no interaction between the drug and polymers. Standard graphs were created for Labetalol HCl, demonstrating linearity (R2=0.998) and adherence to Beer's and Lambert's law. Through a 32 complete factorial design, the impact of changing the proportions of HPMC (X1) and PVC (X2) on the tensile strength and the percentage of medication released in 20 hours (Q20) were determined. Regression analysis and analysis of variance were performed on the dependent variables. It was concluded that Labetalol HCl could indeed be formulated into transdermal patches for controlled release. The formulation HPMC, Methyl Cellulose, & PVP (2:1) F4 was identified as the most suitable for controlled release, releasing 96.20% of the medication in 24 hours. The goal of this research was to administer the medication through intact skin at a controlled rate to increase bioavailability and extend the duration of hypertension treatment using transdermal patches. The skin offers numerous advantages over other routes of drug administration, such as avoiding issues related to gastric irritation, gastric emptying rate, hepatic first-pass metabolism, and minimizing the risk of systemic side effects.