Novel Pediatric Dosage Forms: Formulation Devlopment and Optimization

Abstract

Oral formulations have carved a niche amongst the different drug delivery systems. Ease of administration and patient compliance are gaining significant importance in the design of dosage forms. Paracetamol is an orally administered antipyretic and anti-inflammatory drug, used in the management of fever and pain. Difficulty in swallowing (dysphagia) is common among paediatric patients. Although unpleasant taste is masked for paediatric administration, accurate dose administration cannot be ensured through syrup. In light of all above facts and challenges, it was decided to formulate and optimize Granules, Fast dissolving tablets, Oral Jelly and Spray dried powder for paediatric patients which could provide patient compliance, accurate dose with desirable taste masking. Different taste masking approaches were tried for each formulation. In granules, taste masking was achieved using polymer hyperomellose, in fast dissolving tablets, taste masking was achieved by using β-cyclodextrin, in jelly, taste masking was achieved by using citric acid and in spray dried powder, taste masking was achieved by complete coating of paracetamol with milk powder. The excipients like mannitol, sucrose, sucralose and cocoa powder were evaluated in granules, fast dissolving tablets and spray dried powder, while gelling agent, major component of jelly was optimized in oral jelly along with sucrose and starch. The optimized batches G21, F42, J27 and S12 showed drug release more than 85% within 15 min at all pH, along with all the desired organoleptic properties. The optimized batches showed substantial stability when subjected to short term stability study (0-8°C and room temperature). Amongst all the formulations, granules were found to be best in terms of assay, % yield, drug release profile, stability, operational skills, excipients and process costs. The developed unit dosage forms, granules, fast dissolving tablets, oral jelly and spray dried powder are found to be a very promising approach to administer drugs in paediatric population.