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Rational use of antioxidants in solid oral pharmaceutical preparations
| Content Provider | Scilit |
|---|---|
| Author | Celestino, Maísa Teodoro Magalhães, Uiaran De Oliveira Fraga, Aline Guerra Manssour Carmo, Flávia Almada Do Lione, Viviane Castro, Helena Carla Sousa, Valéria Pereira De Rodrigues, Carlos Rangel Cabral, Lucio Mendes |
| Copyright Year | 2012 |
| Description | Antioxidants are currently used as efficient excipients that delay or inhibit the oxidation process of molecules. Excipients are often associated with adverse reactions. Stability studies can guide the search for solutions that minimize or delay the processes of degradation. The ability to predict oxidation reactions in different drugs is important. Methods: This study was conducted to assess the rational use of butylated hydroxyanisole (BHA), butylated hydroxytoluene (BHT), sodium metabisulfite (SMB), propyl gallate (PG) and cysteine (CYS) in tablet formulations of simvastatin and ketoconazole. These antioxidants were evaluated according to stability parameters and the relationship between efficiency of the antioxidant and chemical structure of the drugs. Results were compared with DPPH tests and computational simulations. BHT was most efficient regarding simvastatin stability, and the most effective BHT concentrations for maintaining stability were 0.5 and 0.1%. In relation to ketoconazole, SMB was most efficient for maintaining content and dissolution profile. The evaluation by DPPH showed that the largest percentage of absorbance reduction was observed for PG, while SMB proved most efficient and had lower consumption of DPPH. The same pattern was observed, albeit with lower efficiency, for the other lipophilic antioxidants such as BHT and BHA. The results of the molecular modeling study demonstrated that electronic properties obtained were correlated with antioxidant activity in solution, being useful for the rational development of liquid pharmaceutical formulations but not for solid oral formulations. This study demonstrated the importance of considering stability parameters and molecular modeling to elucidate the chemical phenomena involved in antioxidant activity, being useful for the rational use of antioxidants in the development of pharmaceutical formulations. |
| Related Links | http://www.scielo.br/pdf/bjps/v48n3/a07v48n3.pdf http://www.scielo.br/scielo.php?script=sci_pdf&pid=S1984-82502012000300007&lng=en&nrm=iso&tlng=en |
| Ending Page | 415 |
| Page Count | 11 |
| Starting Page | 405 |
| e-ISSN | 21759790 |
| DOI | 10.1590/s1984-82502012000300007 |
| Journal | Brazilian Journal of Pharmaceutical Sciences |
| Issue Number | 3 |
| Volume Number | 48 |
| Language | English |
| Publisher | FapUNIFESP (SciELO) |
| Publisher Date | 2012-09-01 |
| Access Restriction | Open |
| Subject Keyword | Brazilian Journal of Pharmaceutical Sciences Pharmacology and Pharmacy Butylated Hydroxyanisole Butylated Hydroxytoluene Sodium Metabisulfite Hidroxianisol Butilado Hidroxitolueno Butilado Metabissulfito Sódico Galato De Propila |
| Content Type | Text |
| Resource Type | Article |
