Taste masking of naproxen sodium granules by fluid-bed coating

Abstract

The taste of oral dosage forms is an important argument regarding patient's compliance and acceptability. For this reason, it is often necessary to mask an undesirable and unpleasant taste of an active pharmaceutical ingredient. The purpose of this study was to mask the taste of naproxen sodium by a new fluid-bed coating approach. Different compositions of coating suspensions were used to coat naproxen sodium granules. It was found that products with the addition of a plasticizer were not stable at 40 °C and tended to agglomerate. Subsequently, formulations without plasticizer were used and the ratio between water and Eudragit® E was varied. Increasing the fraction of water in the suspension from 3% to 14% reduced the effective release of naproxen sodium. An optimum ratio between naproxen sodium granules and Eudragit® E was found to be 1:1.576, where less naproxen sodium was released than the threshold bitter value and an appropriate taste masking for more than 5 min was guaranteed. Investigation of the particle size distribution revealed a d(10) of 138.35 ± 21.52 µm, a d(50 )= 256.40 ± 11.27 µm and a d(90 )= 500.85 ± 69.08 µm, which guarantees an acceptable mouthfeel for patients.

Formulation, Preparation, and Evaluation of Novel Orally Disintegrating Tablets Containing Taste-Masked Naproxen Sodium Granules and Naratriptan Hydrochloride

“…Previous results of other research groups reported reduced mechanical strength for freeze‐dried suspensions of phenobarbital and hydrochlorothiazide in comparison to placebo . Note that X‐ray powder diffraction measurements confirmed the crystalline state of NaS before and after coating with Eudragit® E . However, because of the polymeric coating, the overall granules were predominantly amorphous .…”

“…The taste‐masking properties of both batches of NaS granules were preserved after freeze‐drying and storage, indicating that the formulation and the process conditions provide sufficient incorporation without rupture of the coating. The measured values are well below the threshold bitterness value of NaS determined in a previous study . However, it is critical to examine the stability of the coating on a longer timescale, particularly at elevated temperatures.…”

“…The targeted load of naproxen sodium in the taste‐masked granules was about 28% of the total mass of coated granules. This is because of the required masses of Eudragit® E and talcum to ensure sufficient taste masking . However, the drug entrapment efficiency of all produced batches was between 96.34% and 120.12% of the desired amount of naproxen sodium.…”

“…Note that the term incorporation efficiency is used to describe the ability of the different ODT formulations to sufficiently embed taste‐masked naproxen sodium granules in the freeze‐dried matrix. The taste masking of naproxen sodium granules by fluid‐bed coating is described elsewhere . The mass of granules required to obtain the target dose of 200 mg naproxen per ODT was in the range of 690–797 mg because of variations in the drug entrapment efficiency.…”

“…The purpose of this study was to develop a novel formulation for ODTs for migraine therapy, prepared by freeze-drying and containing a combination of naratriptan hydrochloride and naproxen sodium, the latter taste-masked by fluid-bed coating with Eudragit R E. 36 The taste-masked particles were successfully incorporated in a freeze-dried matrix along with naratriptan hydrochloride. Note that only two previous studies examined the formulation of an ODT for migraine therapy, prepared by direct compression and containing taste-masked sumatriptan succinate.…”