Isradipine

The present research work describes the  improvement of  bioavailability of Isradipine through buccal delivery. Isradipine buccal tablets were prepared with β cyclodextrin which improved the photostability of the drug. Buccal formulations were evaluated for in vitro release, moisture absorption, mechanical properties, and bioadhesion, and optimized formulation was subjected for bioavailability studies in healthy human volunteers and compared with marketed tablet. The pharmacokinetic parameters Cmax, tmax and AUCo-t of test formulation were calculated and compared with the reference i.e., marketed product. It was observed from the study that the drug release from the test formulation could be sustained and it was concluded that the test formulation was able to sustain the drug release as compared to reference marketed product with 1.672 fold increase in extent of absorption i.e., AUC0-t.

The present work aimed at preparing fast dissolving buccal films of Isradipine solid dispersion, since Isradipine is a poorly soluble drug and the rate of absorption is often controlled by the rate of dissolution. The purpose of developing a dosage form for a very quick onset of action and for improved bioavailability along with the convenience of administration i.e. without the problem of swallowing and using water. The rate of dissolution can be increased by incorporating the drug in a fast dissolving buccal film as a solid dispersion that prepared using polyethylene glycol (PEG4000) or polyvinyl pyrrolidone (PVP k30). The fast dissolving films of Isradipine solid dispersion were prepared by solvent casting method using Lycoat RS720 polymer and glycerin as a plasticizer. The formulated films were evaluated for their physiochemical parameters like disintegration time, surface pH, thickness & weight of the films, percent moisture absorption, folding endurance, drug content and stability testing. Different factors affecting the dissolution rate of solid dispersion and fast dissolving film were studied. It was seen that as the ratio of drug to PEG4000 or PVP k30 in solid dispersion increased the release rate increased and the solvent evaporation method gave greater drug release than fusion method. In fast dissolving film it was seen that as the concentration of Lycoat RS720 increased the release rate decreased and as the concentration of glycerin increased the release rate increased. Formulation F6 showed 98.89% drug release from the film within 7 minutes which is an essential character for faster absorption.