| Author | Guimarães, Thiago F. | |
| Author | Vital, Italo Carlos F. | |
| Author | Sousa, Eduardo G. | |
| Author | Boniatti, Janine | |
| Author | Bandini, Thiago B. | |
| Author | Carr, Olívia | |
| Author | Oliveira Jr., Osvaldo N. | |
| Author | Shimizu, Flávio M. | |
| Author | Fonseca, Laís B. | |
| Author | Viçosa, Alessandra L. | |
| Access date | 2022-02-24T18:13:19Z | |
| Available date | 2022-02-24T18:13:19Z | |
| Document date | 2022 | |
| Citation | GUIMARÃES, Thiago F. et al. Investigation of chloroquine resinate feasibility and in vitro taste masking evaluation for pediatric formulations. AAPS PharmSciTech, New York, v. 23, p. 69-1-69-12, 2022. | pt_BR |
| URI | https://www.arca.fiocruz.br/handle/icict/51475 | |
| Sponsorship | This work was supported by Inova Fiocruz/VPCCB, CNPq and FAPESP (2018/22214-6). | pt_BR |
| Language | eng | pt_BR |
| Rights | restricted access | pt_BR |
| Title | Investigation of chloroquine resinate feasibility and in vitro taste masking evaluation for pediatric formulations | pt_BR |
| Type | Article | |
| DOI | 10.1208/s12249-022-02219-7 | |
| Abstract | In this study, chloroquine resinates were prepared at a 1:1 (w:w) drug-to-resin ratio using the batch method with polacrilex (PC), sodium polystyrene sulfonate (SPS), and polacrilin potassium (PP) ion exchange resins (IER). The influence of drug/resin ratio and pH of the medium on drug loading efficiency was explored. UV-VIS spectrophotometric analysis showed that SPS resin had high loading efficiency for chloroquine diphosphate (CLP), above 89%, regardless of the pH. PP resin was more effective at pH 5.0 (90.68%) than at pH 1.0 (2.09%), and PC resin had only 27.63% of CLP loading efficiency. CLP complexation with IER yielded amorphous mixtures according to results from differential scanning calorimetry (DSC) and X-ray powder diffraction (XRPD), thus indicating drug-resin interaction. The taste masking efficiency was evaluated with in vitro methods using an adapted dissolution test and an electronic tongue system. During dissolution tests, SPS released only 1.0% of CLP after 300 s, while PP released over 10% after 90 s in simulated saliva solution. The electronic tongue distinguished the samples containing CLP, resins, and resinates by using multidimensional projection techniques that indicated an effective drug taste masking. In an accelerated stability study, the drug
contents did not decrease in chloroquine resinates, and there was no physical degradation of the resinates
after 60 days. Using chloroquine resinates therefore represents a novel way to evaluate taste masking
in vitro which is relevant for the early formulation development process. | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Instituto de Tecnologia em Fármacos. Rio de Janeiro, RJ, Brasil | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Instituto de Tecnologia em Fármacos. Rio de Janeiro, RJ, Brasil | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Instituto de Tecnologia em Fármacos. Rio de Janeiro, RJ, Brasil | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Instituto de Tecnologia em Fármacos. Rio de Janeiro, RJ, Brasil | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Instituto Carlos Chagas. Curitiba, PR, Brasil | pt_BR |
| Affilliation | Universidade de São Paulo. São Paulo, SP, Brasil | pt_BR |
| Affilliation | Universidade de São Paulo. São Paulo, SP, Brasil | pt_BR |
| Affilliation | Universidade de Campinas. Campinas, SP, Brasil. | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Vice-Presidência de Produção e Inovação em Saúde. Rio de Janeiro, RJ, Brasil | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Instituto de Tecnologia em Fármacos. Rio de Janeiro, RJ, Brasil | pt_BR |
| Subject | Chloroquine | pt_BR |
| Subject | Ion exchange resins | pt_BR |
| Subject | Resinates | pt_BR |
| Subject | Taste masking | pt_BR |
| Subject | Pediatrics | pt_BR |
