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Previous issue date: 2016-11-28 / A utiliza??o de ciclodextrinas para aumentar a solubilidade de f?rmacos em solu??o aquosa tem sido bastante estudada. No presente estudo, o mecanismo de intera??o do praziquantel (PZQ) com a beta-ciclodextrina e com a hidroxipropil-beta-ciclodextrina na presen?a dos co-solventes trietanolamina (TEA) e a N-metilpirrolidona (NMP) foi realizado com o objetivo do aumento da solubilidade do praziquantel. Atrav?s dos diagramas de solubilidade e dos diagramas de Job?s Plot foi poss?vel observar a forma??o de complexos sol?veis com estequiometria 1:1. A presen?a dos co-solventes TEA e NMP diminuiu a estabilidade e solubilidade dos complexos formados, no entanto atrav?s dos estudos de modelagem molecular foi mostrado que este efeito pode facilitar a sa?da do f?rmaco da cavidade e, consequentemente, beneficiar a absor??o do f?rmaco. Os resultados mostraram-se elucidativos e bastantes promissores na obten??o futura de complexos que possam ser utilizados para melhor biodisponibilidade do praziquantel. / The use of cyclodextrin (CD) to enhace the praziquantel (PZQ) water solubility has been widely studied in the literature. In this present paper, the interaction has not yet studied between the PZQ and both the beta-cyclodextrin (?-CD) and hydroxyl-propyl-cyclodextrin (HP-?-CD) or its association with the solvents triethanolamine (TEA) and N-methyl-pyrrolidone (NMP) was carefully conducted with the purpose to enhance the water solubility of the PZQ. The solubility diagrams and job?s plot diagrams showed that water soluble complexes were formed with 1:1 stoichiometry. The association of the complexes with the TEA and NMP diminished considerably the complex stability and its solubility. However, throught the molecular modeling study it was showed that this effect may be beneficial for the output of the drug from the CD cavity, and consequently to benefit the drug absorption. The results showed up adequately enlightening to propose that these systems can be investigated to enhance the PZQ bioavailability.
| Identifer | oai:union.ndltd.org:IBICT/oai:repositorio.ufrn.br:123456789/23415 |
| Date | 28 November 2016 |
| Creators | Souza, Jairo Sotero Nogueira de |
| Contributors | 00840406452, http://lattes.cnpq.br/2593509584288129, Menezes, Fabricio Gava, 03114939988, http://lattes.cnpq.br/2848745987784319, Silva J?nior, Jos? Ot?vio Carr?ra, 22775277268, http://lattes.cnpq.br/4437885351749994, Barbosa, Euz?bio Guimar?es, Silva J?nior, Arn?bio Antonio da |
| Publisher | PROGRAMA DE P?S-GRADUA??O EM CI?NCIAS FARMAC?UTICAS, UFRN, Brasil |
| Source Sets | IBICT Brazilian ETDs |
| Language | Portuguese |
| Detected Language | English |
| Type | info:eu-repo/semantics/publishedVersion, info:eu-repo/semantics/masterThesis |
| Source | reponame:Repositório Institucional da UFRN, instname:Universidade Federal do Rio Grande do Norte, instacron:UFRN |
| Rights | info:eu-repo/semantics/openAccess |
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