Formulation and Evaluation of Carvedilol Transdermal Patches for the Treatment of Hypertension

Abstract

Carvedilol is a drug used to treat high blood pressure. It has a 6 hour half-life & a 25% oral bioavailability due to 1st pass metabolism. Frequent dosage was required because the daily maximum dose of cartedilol is 50mg. To improve patient compliance & drug's absorption, carvedilol transdermal patches were developed. Using the solvent casting technique, various formulations were produced by varying the ratios of HPMC, Methyl Cellulose, and PVP. The tested formulations were evaluated for weight variation, patch thickness, folding toughness, drug content, rates of moisture absorption & loss, in-vitro drug release, among other things. It was feasible to evaluate how altering the concentrations of HPMC (X1) & PVC (X2) would impact the results using a 32 full factorial design, i.e. Tensile strength & proportion of medicine released in 20 hours (Q20) are dependent variables. Regression analysis & analysis of variance were performed on dependent variables. To increase the features of its release, it is conceivable that carvedilol might be turned into transdermal patches. The combination HPMC, Methyl Cellulose, & PVP (3:1) F7 was shown to be best for controlled release because it released 84.36% of medication in 24 hours. To boost absorption and prolong the duration of transdermal patch therapy for hypertension, medicine had to be administered over undamaged skin at a controlled rate. The advantages the skin has over many other routes of drug administration include capacity to avoid issues with gastric discomfort, gastric emptying rate, prevent hepatic first-pass metabolism hence enhancing the bioavailability of drug, and reducing the danger of systemic side effects.

Keywords: Transdermal Patch, Moisture Absorption, Hypertension, Enhancing the Bioavailability