Pediatric Orally Disintegrating Tablets (ODTs) with Enhanced Palatability Based on Propranolol HCl Coground with Hydroxypropyl-β-Cyclodextrin
Background: Propranolol, largely prescribed as an antihypertensive and antiarrhythmic drug in pediatrics, is characterized by a bitter taste and an astringent aftertaste. Currently, the therapy requires crushing of tablets for adults and their dispersion in water many times a day, leading to loss of...
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| author | Marzia Cirri Paola A. Mura Francesca Maestrelli Simona Benedetti Susanna Buratti |
| author_facet | Marzia Cirri Paola A. Mura Francesca Maestrelli Simona Benedetti Susanna Buratti |
| author_sort | Marzia Cirri |
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| description | Background: Propranolol, largely prescribed as an antihypertensive and antiarrhythmic drug in pediatrics, is characterized by a bitter taste and an astringent aftertaste. Currently, the therapy requires crushing of tablets for adults and their dispersion in water many times a day, leading to loss of dosing accuracy, low palatability, and poor compliance for both patients and caregivers. Objectives: This work aimed to exploit cyclodextrin complexation by cogrinding to develop orally disintegrating tablets (ODTs) endowed with reliable dosing accuracy, good palatability and safety, ease of swallowability, and ultimately better compliance for both pediatric patients and caregivers. Results: Different formulation variables and process parameters were evaluated in preparing ODTs. The technological and morphological characterization and disintegration tests were performed according to official and alternative tests to select the ODT formulation based on the drug Hydroxypropyl-β-cyclodextrin (HPβCD) coground complex form containing Pearlitol<sup>®</sup> Flash as the diluent and 8% Explotab<sup>®</sup> as the superdisintegrant, which demonstrated the highest % drug dissolution in simulated saliva and acceptable in vitro palatability assessed by the electronic tongue, confirming the good taste-masking power of HPβCD towards propranolol. Conclusions: Such a new dosage form of propranolol could represent a valid alternative to the common extemporaneous preparations, overcoming the lack of solid formulations of propranolol intended for pediatric use. |
| format | Article |
| id | doaj-art-b99206718ab14b3e929cd9e6d0e9b3bf |
| institution | Kabale University |
| issn | 1999-4923 |
| language | English |
| publishDate | 2024-10-01 |
| publisher | MDPI AG |
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| series | Pharmaceutics |
| spelling | doaj-art-b99206718ab14b3e929cd9e6d0e9b3bf2024-11-26T18:17:39ZengMDPI AGPharmaceutics1999-49232024-10-011611135110.3390/pharmaceutics16111351Pediatric Orally Disintegrating Tablets (ODTs) with Enhanced Palatability Based on Propranolol HCl Coground with Hydroxypropyl-β-CyclodextrinMarzia Cirri0Paola A. Mura1Francesca Maestrelli2Simona Benedetti3Susanna Buratti4Department of Chemistry Ugo Schiff (DICUS), University of Florence, 50019 Sesto Fiorentino, ItalyDepartment of Chemistry Ugo Schiff (DICUS), University of Florence, 50019 Sesto Fiorentino, ItalyDepartment of Chemistry Ugo Schiff (DICUS), University of Florence, 50019 Sesto Fiorentino, ItalyDepartment of Food, Environmental and Nutritional Sciences (DeFENS), University of Milan, 20133 Milan, ItalyDepartment of Food, Environmental and Nutritional Sciences (DeFENS), University of Milan, 20133 Milan, ItalyBackground: Propranolol, largely prescribed as an antihypertensive and antiarrhythmic drug in pediatrics, is characterized by a bitter taste and an astringent aftertaste. Currently, the therapy requires crushing of tablets for adults and their dispersion in water many times a day, leading to loss of dosing accuracy, low palatability, and poor compliance for both patients and caregivers. Objectives: This work aimed to exploit cyclodextrin complexation by cogrinding to develop orally disintegrating tablets (ODTs) endowed with reliable dosing accuracy, good palatability and safety, ease of swallowability, and ultimately better compliance for both pediatric patients and caregivers. Results: Different formulation variables and process parameters were evaluated in preparing ODTs. The technological and morphological characterization and disintegration tests were performed according to official and alternative tests to select the ODT formulation based on the drug Hydroxypropyl-β-cyclodextrin (HPβCD) coground complex form containing Pearlitol<sup>®</sup> Flash as the diluent and 8% Explotab<sup>®</sup> as the superdisintegrant, which demonstrated the highest % drug dissolution in simulated saliva and acceptable in vitro palatability assessed by the electronic tongue, confirming the good taste-masking power of HPβCD towards propranolol. Conclusions: Such a new dosage form of propranolol could represent a valid alternative to the common extemporaneous preparations, overcoming the lack of solid formulations of propranolol intended for pediatric use.https://www.mdpi.com/1999-4923/16/11/1351pediatric formulationpropranolol HClcyclodextrin complexationorally disintegrating tabletstaste maskingelectronic tongue |
| spellingShingle | Marzia Cirri Paola A. Mura Francesca Maestrelli Simona Benedetti Susanna Buratti Pediatric Orally Disintegrating Tablets (ODTs) with Enhanced Palatability Based on Propranolol HCl Coground with Hydroxypropyl-β-Cyclodextrin Pharmaceutics pediatric formulation propranolol HCl cyclodextrin complexation orally disintegrating tablets taste masking electronic tongue |
| title | Pediatric Orally Disintegrating Tablets (ODTs) with Enhanced Palatability Based on Propranolol HCl Coground with Hydroxypropyl-β-Cyclodextrin |
| title_full | Pediatric Orally Disintegrating Tablets (ODTs) with Enhanced Palatability Based on Propranolol HCl Coground with Hydroxypropyl-β-Cyclodextrin |
| title_fullStr | Pediatric Orally Disintegrating Tablets (ODTs) with Enhanced Palatability Based on Propranolol HCl Coground with Hydroxypropyl-β-Cyclodextrin |
| title_full_unstemmed | Pediatric Orally Disintegrating Tablets (ODTs) with Enhanced Palatability Based on Propranolol HCl Coground with Hydroxypropyl-β-Cyclodextrin |
| title_short | Pediatric Orally Disintegrating Tablets (ODTs) with Enhanced Palatability Based on Propranolol HCl Coground with Hydroxypropyl-β-Cyclodextrin |
| title_sort | pediatric orally disintegrating tablets odts with enhanced palatability based on propranolol hcl coground with hydroxypropyl β cyclodextrin |
| topic | pediatric formulation propranolol HCl cyclodextrin complexation orally disintegrating tablets taste masking electronic tongue |
| url | https://www.mdpi.com/1999-4923/16/11/1351 |
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