Palatable Orally Disintegrating Tablets of Losartan Potassium Developed by Spray-drying Technique and Direct Compression Intended for Pediatric Use

Abstract

Several diseases that affect the pediatric population, e.g., heart diseases, cannot be efficiently treated because of the absence of a suitable dosage form. In this sense, orally disintegrating tablets (ODT) are solid dosage forms that are gaining acceptance. Losartan potassium (LP) is the drug of choice for managing pediatric arterial hypertension, although its bitter taste represents a major challenge to treatment compliance. To mitigate this drawback, this study aimed to develop palatable ODT, by the incorporation of spray-dried powders (SDP), composed of LP, Eudragit® polymers and adjuvants (i.e., colloidal silicon dioxide, mannitol, and PEG4000).

The SDP were analyzed in terms of production yield and encapsulation efficiency. Selected SDP were incorporated into ODT by direct compression, and characterized in terms of mechanical and pharmaceutical properties, as well as palatability. Tablets with satisfactory disintegration time, hardness, and friability were obtained, though different performance during in vitro dissolution study.

In the palatability study, the volunteer panel confirmed that the ODT-7SDP formulation, prepared by spray drying with Eudragit® E PO and colloidal silicon dioxide, showed a marked reduction in LP bitterness. In conclusion, the applied technologies successfully reduced the bitter taste of LP, enabling its oral administration in the form of ODT, particularly for pediatric patients.

Materials

Losartan potassium (LP, 99.8% purity over anhydrous basis, Batch Number: C5455-20–085), colloidal silicon dioxide (SiO2), magnesium stearate (MgS), and menthol were acquired from Droguería Magel (Argentina); pineap-ple flavor (PF) from EUMA (Argentina), and mannitol (M) and polyethylene glycol 4000 (PEG 4000) from Parafarm (Argentina). Other excipients were kindly donated by the corresponding suppliers in Argentina: polymethacrylic acid ethyl acrylate (Eudragit® L 100, Evonik) and amino meth-acrylate copolymer (Eudragit® E PO, Evonik) by Etilfarma; crospovidone (Kollidon® CL, BASF-Pharma) by Rumapel; coprocessed mannitol and croscarmellose sodium (Parteck® ODT) and dimethylbutyl aspartylphenylalanine methyl ester (Neotame®) by Merck. Ethanol, hydrochloric acid (HCl), potassium chloride, monobasic potassium phosphate (Ane-dra, Argentina), sodium hydroxide (Cicarelli, Argentina), potassium bromide (Merck, Germany), and water (distilled in our laboratories) were employed for quality properties evaluation.

Juan, C., Gonzalez Vidal, N. & Gallo, L. Palatable Orally Disintegrating Tablets of Losartan Potassium Developed by Spray-drying Technique and Direct Compression Intended for Pediatric Use. AAPS PharmSciTech 26, 212 (2025). https://doi.org/10.1208/s12249-025-03208-2