To circumvent the bad taste of drugs, many technologies are available, such as pro-drugs synthesis, formulating with flavors and sweeteners or coating drug particles with a lipid film. The versatility of the latter technology is particularly attractive and at Gattefossé we have worked on developing a simple, efficient and robust taste masking method.
We use a standard high shear mixer, very common equipment in the pharmaceutical industry, with a limited number of process parameters to control. A simple binary formulation consisting of 80% API and 20% Precirol® ATO 5 is used.
During mixing, frictions are generated which induce enough heat to melt the lipid excipient. Therefore, no external heating is required. The molten lipid coats the drug particles and, upon cooling, solidifies, covering the drug particles and masking the taste.
SEM pictures show the uniformity of the film coating around drug particles. The thin and homogenous film covers the particles, providing a neutral barrier to taste. Drug release is well below the detection threshold, meaning bad taste of drug is not perceived. This was further confirmed by human taste panel assessment.
The high shear coating process proves to be highly robust with straightforward scaling-up and excellent reproducibility. Moreover, it is also suitable for a wide range of drugs, with different crystalline shape, melting point and particle size.