Hybrid polymeric matrices for oral modified release of Desvenlafaxine succinate tablets
Purpose: Desvenlafaxine succinate (DSV) is a water soluble anti-depressant drug, which is rapidly absorbed after oral administration exaggerating its side effects. The current work aimed to prepare controllable release DSV matrix to reduce DSV side effects related to its initial burst. Methods: Fift...
| Main Authors: | , , , |
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| Format: | Article |
| Language: | English |
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Elsevier
2017-07-01
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| Series: | Saudi Pharmaceutical Journal |
| Subjects: | |
| Online Access: | http://www.sciencedirect.com/science/article/pii/S1319016416301104 |
| _version_ | 1818019869748101120 |
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| author | Wael Samy Ayman Elnoby Hanan M. El-Gowelli Nazik Elgindy |
| author_facet | Wael Samy Ayman Elnoby Hanan M. El-Gowelli Nazik Elgindy |
| author_sort | Wael Samy |
| collection | DOAJ |
| description | Purpose: Desvenlafaxine succinate (DSV) is a water soluble anti-depressant drug, which is rapidly absorbed after oral administration exaggerating its side effects. The current work aimed to prepare controllable release DSV matrix to reduce DSV side effects related to its initial burst. Methods: Fifteen DSV matrix formulations were prepared using different polymers, polymer/drug ratios and matrix excipients and characterized using Differential Scanning Calorimetry (DSC), infrared (IR) spectroscopy, water uptake and in vitro DSV release. The release kinetics were calculated to determine the drug release mechanism. Ex-vivo DSV absorption via rat intestinal mucosal cells and the calculation of the apparent permeability coefficient (Papp) were performed using everted sac technique. Results: Maltodextrin was the best matrix excipient (F7 and F10) showing acceptable decrease in the initial burst compared to the innovator. The addition of negatively charged polymers sodium carboxy methyl cellulose (SCMC) or sodium alginate resulted in an interaction that was proved by DSC and IR findings. This interaction slowed DSV release. F10 showed an excellent absorption of more than 80% of DSV after 4 h and the highest similarity factor with the innovator (84.7). Conclusion: A controllable release pattern of DSV was achieved using Methocel, Maltodextrin and SCMC. The obtained results could be used as a platform to control the release of cationic water soluble drugs that suffer from side effects associated with their initial burst after oral administration. |
| first_indexed | 2024-04-14T07:57:28Z |
| format | Article |
| id | doaj.art-650dcf93570b4323ad33c635552b3b1d |
| institution | Directory Open Access Journal |
| issn | 1319-0164 |
| language | English |
| last_indexed | 2024-04-14T07:57:28Z |
| publishDate | 2017-07-01 |
| publisher | Elsevier |
| record_format | Article |
| series | Saudi Pharmaceutical Journal |
| spelling | doaj.art-650dcf93570b4323ad33c635552b3b1d2022-12-22T02:04:59ZengElsevierSaudi Pharmaceutical Journal1319-01642017-07-0125567668710.1016/j.jsps.2016.10.005Hybrid polymeric matrices for oral modified release of Desvenlafaxine succinate tabletsWael Samy0Ayman Elnoby1Hanan M. El-Gowelli2Nazik Elgindy3Department of Industrial Pharmacy, Faculty of Pharmacy, Alexandria University, Alexandria, EgyptDepartment of Industrial Pharmacy, Faculty of Pharmacy, Alexandria University, Alexandria, EgyptDepartment of Pharmacology and Toxicology, Faculty of Pharmacy, Alexandria University, Alexandria, EgyptDepartment of Industrial Pharmacy, Faculty of Pharmacy, Alexandria University, Alexandria, EgyptPurpose: Desvenlafaxine succinate (DSV) is a water soluble anti-depressant drug, which is rapidly absorbed after oral administration exaggerating its side effects. The current work aimed to prepare controllable release DSV matrix to reduce DSV side effects related to its initial burst. Methods: Fifteen DSV matrix formulations were prepared using different polymers, polymer/drug ratios and matrix excipients and characterized using Differential Scanning Calorimetry (DSC), infrared (IR) spectroscopy, water uptake and in vitro DSV release. The release kinetics were calculated to determine the drug release mechanism. Ex-vivo DSV absorption via rat intestinal mucosal cells and the calculation of the apparent permeability coefficient (Papp) were performed using everted sac technique. Results: Maltodextrin was the best matrix excipient (F7 and F10) showing acceptable decrease in the initial burst compared to the innovator. The addition of negatively charged polymers sodium carboxy methyl cellulose (SCMC) or sodium alginate resulted in an interaction that was proved by DSC and IR findings. This interaction slowed DSV release. F10 showed an excellent absorption of more than 80% of DSV after 4 h and the highest similarity factor with the innovator (84.7). Conclusion: A controllable release pattern of DSV was achieved using Methocel, Maltodextrin and SCMC. The obtained results could be used as a platform to control the release of cationic water soluble drugs that suffer from side effects associated with their initial burst after oral administration.http://www.sciencedirect.com/science/article/pii/S1319016416301104Desvenlafaxine succinateControlled release matrixApparent permeability coefficientEverted sac |
| spellingShingle | Wael Samy Ayman Elnoby Hanan M. El-Gowelli Nazik Elgindy Hybrid polymeric matrices for oral modified release of Desvenlafaxine succinate tablets Saudi Pharmaceutical Journal Desvenlafaxine succinate Controlled release matrix Apparent permeability coefficient Everted sac |
| title | Hybrid polymeric matrices for oral modified release of Desvenlafaxine succinate tablets |
| title_full | Hybrid polymeric matrices for oral modified release of Desvenlafaxine succinate tablets |
| title_fullStr | Hybrid polymeric matrices for oral modified release of Desvenlafaxine succinate tablets |
| title_full_unstemmed | Hybrid polymeric matrices for oral modified release of Desvenlafaxine succinate tablets |
| title_short | Hybrid polymeric matrices for oral modified release of Desvenlafaxine succinate tablets |
| title_sort | hybrid polymeric matrices for oral modified release of desvenlafaxine succinate tablets |
| topic | Desvenlafaxine succinate Controlled release matrix Apparent permeability coefficient Everted sac |
| url | http://www.sciencedirect.com/science/article/pii/S1319016416301104 |
| work_keys_str_mv | AT waelsamy hybridpolymericmatricesfororalmodifiedreleaseofdesvenlafaxinesuccinatetablets AT aymanelnoby hybridpolymericmatricesfororalmodifiedreleaseofdesvenlafaxinesuccinatetablets AT hananmelgowelli hybridpolymericmatricesfororalmodifiedreleaseofdesvenlafaxinesuccinatetablets AT nazikelgindy hybridpolymericmatricesfororalmodifiedreleaseofdesvenlafaxinesuccinatetablets |