AN INVESTIGATION INTO TASTE MASKING OF A MICRONIZEDPARACETAMOL USING AQUACOAT® ECD APPLIED VIA DIFFERENTGRANULATION PROCESSES
INTRODUCTION AND PURPOSE
Taste masking is a very important step in the development of paediatric medications such as oral suspensions and tablets for products with APIs that are bitter or unpalatable. In this study, taste masking of a bitter, micronized API model (Paracetamol) was attempted using two different granulation methods. The influence of the type of granulation process and formulation on the properties of subsequent granules and taste masking effect was evaluated.
MATERIALS AND METHODS
- The aqueous ethylcellulose dispersion Aquacoat® ECD was used as the taste masking agent. Aquacoat® ECD was plasticized with Triethylcitrate (24%, based on ethylcellulose content).
- A micronized form of Paracetamol (d50 of 10 µm) was used as a model simulating a bitter, micronized API.
- The plasticized Aquacoat ECD was applied to the API via top spray granulation (TSG) in a fluid bed or via high shear granulation (HSG).
- API was granulated alone or with a pre-mix of MCC (Avicel® PH101) and lactose, since these are common excipients required to improve the granulation process and final granule properties.
- The particle size of the API and of the final granules was determined using sieve analysis and laser diffraction.
- Taste of the granules was assessed via a taste panel consisting of 4 adult males.
- The resultant granules were compacted into tablets using croscarmellose sodium (Ac-Di-Sol®) as a super disintegrant, mannitol as a filler/binder, and sodium stearyl fumarate (Alubra®) as a lubricant. Drug dissolution was measured in 0.1M HCl for 1h.
AN INVESTIGATION INTO TASTE MASKING OF A MICRONIZED PARACETAMOL USING AQUACOAT® ECD APPLIED VIA DIFFERENT GRANULATION PROCESSES
44. AN INVESTIGATION INTO TASTE MASKING
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