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Prasugrel (PSG) is used in minimizing the risk of atherothrombotic events in people with cardiovascular problems. Developing extended-release products for PSG is highly advantageous owing to its pharmacodynamic and pharmacokinetic properties. But, due to its insolubility in aqueous media with pH above 6.0, it becomes poorly bioavailable from the small intestine upon oral administration. Hence, an extended-release formulation which resides in gastric region until released completely is highly recommended. Polymeric hollow-microspheres with inherent floating property without lag time are highly preferable for the PSG kind of drugs. Emulsion solvent evaporation-diffusion technique was explored in this work to develop microspheres inner pores/hollowness. Box-Behnken design (BBD) was employed to study the influence of various formulation and process factors on the critical quality attributes or responses of the PSG hollow-microspheres. Various formulations according to the BBD were developed and studied for quality control tests like floating time, surface morphology, entrapment efficiency, particles size, drug release rate. Surface morphology by scanning electron microscopy indicated big dents and protrusions on the surface indicating inner hollowness. Design of experiments analysis was performed to develop regression equations for every response with the factors. Design validation by ANOVA indicated that all the factors were significant in having influence on every response at p < 0.05. The optimized microspheres were found to have 91.8% entrapment efficiency; 94.5% floating even after 24 h; and extended drug release for more than 18 hours. Ethyl cellulose hollow-microspheres for PSG were successfully optimized and developed by adopting quality by design approach.

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