Compatibility study of rosmarinic acid with excipients used in pharmaceutical solid dosage forms using thermal and non-thermal techniques
Rosmarinic acid (RA) is a phenolic compound that presents well-documented anti-inflammatory, antioxidant and antitumor activities, and based on its pharmacological potential and poor bioavailability, several solid dosage forms have been developed to RA delivery. Therefore, in literature, there are n...
| Main Authors: | , , , , , , , , |
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| Format: | Article |
| Language: | English |
| Published: |
Elsevier
2019-12-01
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| Series: | Saudi Pharmaceutical Journal |
| Online Access: | http://www.sciencedirect.com/science/article/pii/S1319016419301240 |
| _version_ | 1819062648124211200 |
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| author | Kleyton Santos Veras Flávia Nathiely Silveira Fachel Vanessa Pittol Keth Ribeiro Garcia Valquíria Linck Bassani Venina dos Santos Amélia Teresinha Henriques Helder Ferreira Teixeira Letícia Scherer Koester |
| author_facet | Kleyton Santos Veras Flávia Nathiely Silveira Fachel Vanessa Pittol Keth Ribeiro Garcia Valquíria Linck Bassani Venina dos Santos Amélia Teresinha Henriques Helder Ferreira Teixeira Letícia Scherer Koester |
| author_sort | Kleyton Santos Veras |
| collection | DOAJ |
| description | Rosmarinic acid (RA) is a phenolic compound that presents well-documented anti-inflammatory, antioxidant and antitumor activities, and based on its pharmacological potential and poor bioavailability, several solid dosage forms have been developed to RA delivery. Therefore, in literature, there are no reports about RA compatibility with excipients. In this regard, the aim of the present study was to evaluate, for the first time, the compatibility of RA with excipients commonly used in solid dosage forms at a 1:1 (RA:excipient) ratio using differential scanning calorimetry (DSC), thermogravimetry (TG), Fourier-transform infrared (FTIR), solid-state nuclear magnetic resonance (ssNMR), and isothermal stress testing (IST) coupled with liquid chromatography (LC). The excipients selected were hydroxypropyl methylcellulose (HPMC), microcrystalline cellulose (MCC), lactose monohydrate (LAC), polyvinylpyrrolidone (PVP), talc (TALC), croscarmellose sodium (CCS), and magnesium stearate (MgSTE). According to DSC results, physical interactions were found between RA and HPMC, LAC, CCS, and MgSTE. The TG analyses confirmed the physical interactions and suggested chemical incompatibility. FTIR revealed physical interaction of RA with TALC and MgSTE and the ssNMR confirmed the physical interaction showed by FTIR and excluded the presence of chemical incompatibility. By IST, the greatest loss of RA content was found to CCS and MgSTE (>15%), demonstrating chemical incompatibilities with RA. High temperatures used in DSC and TG analyses could be responsible for incompatibilities in binary mixtures (BMs) with HPMC and LAC, while temperature above 25 °C and presence of water were factors that promote incompatibilities in BMs with CCS and MgSTE. Overall results demonstrate that RA was compatible with MCC and PVP. Keywords: Rosmarinic acid, Excipient, Compatibility, TG, ssNMR, IST |
| first_indexed | 2024-12-21T15:02:07Z |
| format | Article |
| id | doaj.art-1b75c53e56ae499bafba73b545d46d9c |
| institution | Directory Open Access Journal |
| issn | 1319-0164 |
| language | English |
| last_indexed | 2024-12-21T15:02:07Z |
| publishDate | 2019-12-01 |
| publisher | Elsevier |
| record_format | Article |
| series | Saudi Pharmaceutical Journal |
| spelling | doaj.art-1b75c53e56ae499bafba73b545d46d9c2022-12-21T18:59:34ZengElsevierSaudi Pharmaceutical Journal1319-01642019-12-0127811381145Compatibility study of rosmarinic acid with excipients used in pharmaceutical solid dosage forms using thermal and non-thermal techniquesKleyton Santos Veras0Flávia Nathiely Silveira Fachel1Vanessa Pittol2Keth Ribeiro Garcia3Valquíria Linck Bassani4Venina dos Santos5Amélia Teresinha Henriques6Helder Ferreira Teixeira7Letícia Scherer Koester8Programa de Pós-Graduação em Ciências Farmacêuticas, Faculdade de Farmácia, Universidade Federal do Rio Grande do Sul, Avenida Ipiranga, 2752, 90610-000 Porto Alegre, BrazilPrograma de Pós-Graduação em Ciências Farmacêuticas, Faculdade de Farmácia, Universidade Federal do Rio Grande do Sul, Avenida Ipiranga, 2752, 90610-000 Porto Alegre, BrazilPrograma de Pós-Graduação em Ciências Farmacêuticas, Faculdade de Farmácia, Universidade Federal do Rio Grande do Sul, Avenida Ipiranga, 2752, 90610-000 Porto Alegre, BrazilPrograma de Pós-Graduação em Ciências Farmacêuticas, Faculdade de Farmácia, Universidade Federal do Rio Grande do Sul, Avenida Ipiranga, 2752, 90610-000 Porto Alegre, BrazilPrograma de Pós-Graduação em Ciências Farmacêuticas, Faculdade de Farmácia, Universidade Federal do Rio Grande do Sul, Avenida Ipiranga, 2752, 90610-000 Porto Alegre, BrazilPrograma de Pós-Graduação em Engenharia de Processos e Tecnologias, Universidade de Caxias do Sul, Rua Francisco Getúlio Vargas, 1130, 95070-560 Caxias do Sul, RS, BrazilPrograma de Pós-Graduação em Ciências Farmacêuticas, Faculdade de Farmácia, Universidade Federal do Rio Grande do Sul, Avenida Ipiranga, 2752, 90610-000 Porto Alegre, BrazilPrograma de Pós-Graduação em Ciências Farmacêuticas, Faculdade de Farmácia, Universidade Federal do Rio Grande do Sul, Avenida Ipiranga, 2752, 90610-000 Porto Alegre, BrazilPrograma de Pós-Graduação em Ciências Farmacêuticas, Faculdade de Farmácia, Universidade Federal do Rio Grande do Sul, Avenida Ipiranga, 2752, 90610-000 Porto Alegre, Brazil; Corresponding author.Rosmarinic acid (RA) is a phenolic compound that presents well-documented anti-inflammatory, antioxidant and antitumor activities, and based on its pharmacological potential and poor bioavailability, several solid dosage forms have been developed to RA delivery. Therefore, in literature, there are no reports about RA compatibility with excipients. In this regard, the aim of the present study was to evaluate, for the first time, the compatibility of RA with excipients commonly used in solid dosage forms at a 1:1 (RA:excipient) ratio using differential scanning calorimetry (DSC), thermogravimetry (TG), Fourier-transform infrared (FTIR), solid-state nuclear magnetic resonance (ssNMR), and isothermal stress testing (IST) coupled with liquid chromatography (LC). The excipients selected were hydroxypropyl methylcellulose (HPMC), microcrystalline cellulose (MCC), lactose monohydrate (LAC), polyvinylpyrrolidone (PVP), talc (TALC), croscarmellose sodium (CCS), and magnesium stearate (MgSTE). According to DSC results, physical interactions were found between RA and HPMC, LAC, CCS, and MgSTE. The TG analyses confirmed the physical interactions and suggested chemical incompatibility. FTIR revealed physical interaction of RA with TALC and MgSTE and the ssNMR confirmed the physical interaction showed by FTIR and excluded the presence of chemical incompatibility. By IST, the greatest loss of RA content was found to CCS and MgSTE (>15%), demonstrating chemical incompatibilities with RA. High temperatures used in DSC and TG analyses could be responsible for incompatibilities in binary mixtures (BMs) with HPMC and LAC, while temperature above 25 °C and presence of water were factors that promote incompatibilities in BMs with CCS and MgSTE. Overall results demonstrate that RA was compatible with MCC and PVP. Keywords: Rosmarinic acid, Excipient, Compatibility, TG, ssNMR, ISThttp://www.sciencedirect.com/science/article/pii/S1319016419301240 |
| spellingShingle | Kleyton Santos Veras Flávia Nathiely Silveira Fachel Vanessa Pittol Keth Ribeiro Garcia Valquíria Linck Bassani Venina dos Santos Amélia Teresinha Henriques Helder Ferreira Teixeira Letícia Scherer Koester Compatibility study of rosmarinic acid with excipients used in pharmaceutical solid dosage forms using thermal and non-thermal techniques Saudi Pharmaceutical Journal |
| title | Compatibility study of rosmarinic acid with excipients used in pharmaceutical solid dosage forms using thermal and non-thermal techniques |
| title_full | Compatibility study of rosmarinic acid with excipients used in pharmaceutical solid dosage forms using thermal and non-thermal techniques |
| title_fullStr | Compatibility study of rosmarinic acid with excipients used in pharmaceutical solid dosage forms using thermal and non-thermal techniques |
| title_full_unstemmed | Compatibility study of rosmarinic acid with excipients used in pharmaceutical solid dosage forms using thermal and non-thermal techniques |
| title_short | Compatibility study of rosmarinic acid with excipients used in pharmaceutical solid dosage forms using thermal and non-thermal techniques |
| title_sort | compatibility study of rosmarinic acid with excipients used in pharmaceutical solid dosage forms using thermal and non thermal techniques |
| url | http://www.sciencedirect.com/science/article/pii/S1319016419301240 |
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