天美传媒

Abstract

Risperidone is 3-[2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl]-2-methyl- 6,7,8,9-tetrahydropyrido[1,2-a] pyrimidin-4-one. The primary action of risperidone is to decrease dopaminergic and serotonergic pathway activity in the brain, therefore decreasing symptoms of schizophrenia and mood disorders (Figure 1).

Figure 1: Graphical Abstract..

The primary action of Risperidone is to decrease dopaminergic and serotonergic pathway activity in the brain, therefore decreasing symptoms of schizophrenia and mood disorders. Risperidone has a high binding affinity for serotonergic 5-HT2A receptors when compared to dopaminergic D2 receptors in the brain. The absolute oral bioavailability of risperidone is 70%. The apparent half-life of risperidone is 3 hours (CV=30%) in extensive metabolizers and 20 hours (CV=40%) in poor metabolizers.

The objective of this study is to formulate and evaluate a transdermal patch of Risperidone using a suitable film former. Transdermal patches of Risperidone were prepared by solvent casting method using HPMC K200M and Eudragit RS100. Glycerine and also PEG 400 was used as plasticizer & permeation enhancer. All the formulations were examined for evaluation parameter like physicochemical properties.

The prepared formulation which were evaluated for different physicochemical characteristics like weight of patch, thickness, folding endurance, tensile strength have exhibited satisfactory results.

Based on the evaluation data, the most effective plasticizer was found to be glycerine (F1) as compared to PEG 400 (F2). It was observed that based on the diffusion study that transdermal patch of Risperidone with Glycerine (F1) shows higher release characteristics than the PEG 400 (F2) transdermal patch. Drug content uniformity of F1 (Glycerine) transdermal patch was also higher than the F2 (PEG 400) transdermal patch. It was also observed that the folding endurance was >300 for all the prepared transdermal patches. Based on the studies, it was concluded that the transdermal patch of Risperidone using glycerine (F1) was the best compared to the formulations using PEG 400 (F2).