The Use of Calcium Phosphate-Based Starter Pellets for the Preparation of Sprinkle IR MUPS Formulation of Rosuvastatin Calcium
Sprinkle formulations represent an interesting concept of medicinal products aimed at the steadily growing population of patients suffering from swallowing difficulties (dysphagia). In the present work, immediate-release sprinkle MUPS (multiple-unit pellet system) containing rosuvastatin calcium as a model drug substance was successfully developed. The formulation was prepared by drug layering technique using novel calcium phosphate-based starting pellets (PharSQ® Spheres CM) of three different particle sizes.
The study showed that the developed multiparticulates were characterized by uniform distribution of coating layers thickness, as well as fast dissolution rate (more than 85% of rosuvastatin calcium dissolved within 30 min, as required by the relevant USP/NF monograph). Rosuvastatin calcium, like other statins, has a bitter, unpleasant taste. Investigations conducted with an electronic tongue suggested that the developed formulation achieved the desired taste-masking efficiency. The effect was found to be particle size-dependent, improving as the size of the multiparticulates increased.
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Materials
Rosuvastatin calcium EP (RSC) from Cadchem Laboratories Limited (Chandigarh, India). Calcium phosphate-based starter pellets (DCPA pellets)—Small size: PharSQ® Spheres CM S, medium size: PharSQ® Spheres CM M, large size: PharSQ® Spheres CM L produced by Chemische Fabrik Budenheim (Budenheim, Germany). Hydroxypropylmethylcellulose (HPMC)—Tylopur® 606 manufactured by ShinEtsu SE Tylose GmbH & Co. KG (Wiesbaden, Germany). Isomalt (E953) from Modecor Italiana s.r.l. (Cuvio, Italy). Talc—Micro ACE P-3 produced by Nippon Talc Co., Ltd. (Osaka, Japan). Polyethylene glycol (PEG 400) from POCH S.A. (Gliwice, Poland). Apple juice Riviva manufactured by Sokpol Sp. z o.o. (Myszkow, Poland) and applesauce Owolovo from Real S.A. (Siedlce, Poland) both with a pH of approximately 3.5. Kefir Robico produced by OSM (Radomsko, Poland) with a pH of around 4.4. Rice gruel manufactured by Nestle Polska S.A. (Warsaw, Poland) with a pH of approximately 7.1.
Cal, K.; Mikolaszek, B.; Hess, T.; Papaioannou, M.; Lenik, J.; Ciosek-Skibińska, P.; Wall, H.; Paszkowska, J.; Romanova, S.; Garbacz, G.; Zakowiecki, D. The Use of Calcium Phosphate-Based Starter Pellets for the Preparation of Sprinkle IR MUPS Formulation of Rosuvastatin Calcium. Pharmaceuticals 2023, 16, 242. https://doi.org/10.3390/ph16020242