Preformulation and Long-Term Stability Studies of an Optimized Palatable Praziquantel Ethanol-Free Solution for Pediatric Delivery
To date, the treatment for cysticercosis and neurocysticercosis consists of a single oral intake of praziquantel (5–10 mg/kg), which since it is only available as tablets, hinders its administration to pediatric patients. Praziquantel is a poorly water-soluble drug which represents a challenge for i...
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| Format: | Article |
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MDPI AG
2023-07-01
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| Series: | Pharmaceutics |
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| Online Access: | https://www.mdpi.com/1999-4923/15/8/2050 |
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| author | Giselle Bedogni Paula Garcia Katia Seremeta Nora Okulik Claudio Salomon |
| author_facet | Giselle Bedogni Paula Garcia Katia Seremeta Nora Okulik Claudio Salomon |
| author_sort | Giselle Bedogni |
| collection | DOAJ |
| description | To date, the treatment for cysticercosis and neurocysticercosis consists of a single oral intake of praziquantel (5–10 mg/kg), which since it is only available as tablets, hinders its administration to pediatric patients. Praziquantel is a poorly water-soluble drug which represents a challenge for its formulation in solution, particularly for the pediatric population. Thus, this study aimed to develop a palatable solution for praziquantel using pharmaceutical-accepted co-solvent systems. A design of experiments approach was applied to identify the optimal conditions for achieving a suitable amount of praziquantel in solution using co-solvent mixtures. Thus, praziquantel solubility increased from 0.38 up to 43.50 mg/mL in the optimized system. A taste masking assay in healthy human volunteers confirmed a successful reduction of drug bitterness after the addition of selected flavors and a sweetener. Stability studies were also conducted at different temperatures (4, 25, and 40 °C) for 12 months Even though the presence of the three known impurities of praziquantel was observed, their amounts never exceeded the acceptance criteria of the USP. Thus, this novel approach should be considered a valuable alternative for further preclinical studies considering the high prevalence of this infection worldwide. |
| first_indexed | 2024-03-10T23:39:43Z |
| format | Article |
| id | doaj.art-90c96b01c14e46b19293cbe565be8178 |
| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-03-10T23:39:43Z |
| publishDate | 2023-07-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj.art-90c96b01c14e46b19293cbe565be81782023-11-19T02:35:58ZengMDPI AGPharmaceutics1999-49232023-07-01158205010.3390/pharmaceutics15082050Preformulation and Long-Term Stability Studies of an Optimized Palatable Praziquantel Ethanol-Free Solution for Pediatric DeliveryGiselle Bedogni0Paula Garcia1Katia Seremeta2Nora Okulik3Claudio Salomon4Instituto de Química Rosario, Consejo Nacional de Investigaciones Científicas y Técnicas (IQUIR-CONICET), Suipacha 531, Rosario 2000, ArgentinaPlanta Piloto de Producción de Medicamentos, Facultad de Ciencias Bioquímicas y Farmacéuticas, Universidad Nacional de Rosario, Suipacha 570, Rosario 2000, ArgentinaInstituto de Investigaciones en Procesos Tecnológicos Avanzados, Consejo Nacional de Investigaciones Científicas y Técnicas, Universidad Nacional del Chaco Austral (INIPTA-CONICET-UNCAUS), Cte. Fernández 755, Presidencia Roque Sáenz Peña 3700, ArgentinaInstituto de Investigaciones en Procesos Tecnológicos Avanzados, Consejo Nacional de Investigaciones Científicas y Técnicas, Universidad Nacional del Chaco Austral (INIPTA-CONICET-UNCAUS), Cte. Fernández 755, Presidencia Roque Sáenz Peña 3700, ArgentinaInstituto de Química Rosario, Consejo Nacional de Investigaciones Científicas y Técnicas (IQUIR-CONICET), Suipacha 531, Rosario 2000, ArgentinaTo date, the treatment for cysticercosis and neurocysticercosis consists of a single oral intake of praziquantel (5–10 mg/kg), which since it is only available as tablets, hinders its administration to pediatric patients. Praziquantel is a poorly water-soluble drug which represents a challenge for its formulation in solution, particularly for the pediatric population. Thus, this study aimed to develop a palatable solution for praziquantel using pharmaceutical-accepted co-solvent systems. A design of experiments approach was applied to identify the optimal conditions for achieving a suitable amount of praziquantel in solution using co-solvent mixtures. Thus, praziquantel solubility increased from 0.38 up to 43.50 mg/mL in the optimized system. A taste masking assay in healthy human volunteers confirmed a successful reduction of drug bitterness after the addition of selected flavors and a sweetener. Stability studies were also conducted at different temperatures (4, 25, and 40 °C) for 12 months Even though the presence of the three known impurities of praziquantel was observed, their amounts never exceeded the acceptance criteria of the USP. Thus, this novel approach should be considered a valuable alternative for further preclinical studies considering the high prevalence of this infection worldwide.https://www.mdpi.com/1999-4923/15/8/2050parasitic diseasepraziquantelco-solvencysolubilitypalatabilitypediatric patients |
| spellingShingle | Giselle Bedogni Paula Garcia Katia Seremeta Nora Okulik Claudio Salomon Preformulation and Long-Term Stability Studies of an Optimized Palatable Praziquantel Ethanol-Free Solution for Pediatric Delivery Pharmaceutics parasitic disease praziquantel co-solvency solubility palatability pediatric patients |
| title | Preformulation and Long-Term Stability Studies of an Optimized Palatable Praziquantel Ethanol-Free Solution for Pediatric Delivery |
| title_full | Preformulation and Long-Term Stability Studies of an Optimized Palatable Praziquantel Ethanol-Free Solution for Pediatric Delivery |
| title_fullStr | Preformulation and Long-Term Stability Studies of an Optimized Palatable Praziquantel Ethanol-Free Solution for Pediatric Delivery |
| title_full_unstemmed | Preformulation and Long-Term Stability Studies of an Optimized Palatable Praziquantel Ethanol-Free Solution for Pediatric Delivery |
| title_short | Preformulation and Long-Term Stability Studies of an Optimized Palatable Praziquantel Ethanol-Free Solution for Pediatric Delivery |
| title_sort | preformulation and long term stability studies of an optimized palatable praziquantel ethanol free solution for pediatric delivery |
| topic | parasitic disease praziquantel co-solvency solubility palatability pediatric patients |
| url | https://www.mdpi.com/1999-4923/15/8/2050 |
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