Comparative Study of Different Combinational Mucoadhesive Formulations of Sumatriptan-Metoclopramide
Purpose: Sumatriptan succinate (Sum) is a Serotonin 5- HT1 receptor agonist, used in the treatment of migraine. It is absorbed rapidly but incompletely when taken orally and underwent first - pass metabolism, resulting in a low bioavailability of about 15%. The aim was to design mucoadhesive buccal...
| Main Authors: | , , , , , |
|---|---|
| Format: | Article |
| Language: | English |
| Published: |
Tabriz University of Medical Sciences
2016-03-01
|
| Series: | Advanced Pharmaceutical Bulletin |
| Subjects: | |
| Online Access: | http://journals.tbzmed.ac.ir/APB/Manuscript/APB-6-119.pdf |
| _version_ | 1819059176116060160 |
|---|---|
| author | Mitra Jelvehgari Hadi Valizadeh Sanam Ziapour Mahdieh Rahmani Seyed Hassan Montazam Saieede Soltani |
| author_facet | Mitra Jelvehgari Hadi Valizadeh Sanam Ziapour Mahdieh Rahmani Seyed Hassan Montazam Saieede Soltani |
| author_sort | Mitra Jelvehgari |
| collection | DOAJ |
| description | Purpose: Sumatriptan succinate (Sum) is a Serotonin 5- HT1
receptor agonist, used in the treatment of migraine. It is absorbed rapidly but
incompletely when taken orally and underwent first - pass metabolism, resulting
in a low bioavailability of about 15%. The aim was to design mucoadhesive
buccal discs and sublingual films of Sum and metoclopramide
(Met) combined to improve their bioavailability.
Methods: In the
current study, the microparticles and films were prepared by emulsion solvent
diffusion (ESD) and solvent casting methods, respectively. Buccal-mucoadhesive
microparticles and films with different
drug to polymer ratios were prepared and characterized by encapsulation
efficiency, particle size, DSC
(Differential Scanning Calorimetric), folding endurance, mucoadhesive property
and drug
release studies.
Results: The best
drug/s to polymer ratios in films and microparticles were 1:2.7:8 (SM2)
and 1:4:6 (SM4), respectively. The film of SM2 showed
11.01 mg weight, 123 µm thickness and 300 folding endurance. The production
yield was 107.33% for SM4 microparticles, 323.59 µm for mean
particle size and 94.53% for loading efficiency (for Sum) and 104.18% (for
Met). The DSC showed no stable characteristic of Sum and Met in the drug loaded
films/discs and revealed amorphous form and transition of hydrate to anhydrous
form for Met. The films exhibited very good mucoadhesive properties and shorter
retention time (15-30 s) in comparison with the discs (130 min). The results
showed that the discs prepared had slower release than the films (p<0.05).
Conclusion: Films and discs of Sum-Met combinations were
successfully prepared with improved release and mucoadhesive properties. |
| first_indexed | 2024-12-21T14:06:56Z |
| format | Article |
| id | doaj.art-87b265c9c5604c7483aa4b849ad295ad |
| institution | Directory Open Access Journal |
| issn | 2228-5881 2251-7308 |
| language | English |
| last_indexed | 2024-12-21T14:06:56Z |
| publishDate | 2016-03-01 |
| publisher | Tabriz University of Medical Sciences |
| record_format | Article |
| series | Advanced Pharmaceutical Bulletin |
| spelling | doaj.art-87b265c9c5604c7483aa4b849ad295ad2022-12-21T19:01:12ZengTabriz University of Medical SciencesAdvanced Pharmaceutical Bulletin2228-58812251-73082016-03-016111913010.15171/apb.2016.018APB_932_20150414083036Comparative Study of Different Combinational Mucoadhesive Formulations of Sumatriptan-MetoclopramideMitra Jelvehgari0Hadi Valizadeh1Sanam Ziapour2Mahdieh Rahmani3Seyed Hassan Montazam4Saieede Soltani5 Drug Applied Research Center, Tabriz University of Medical Sciences, Tabriz, Iran. Drug Applied Research Center, Tabriz University of Medical Sciences, Tabriz, Iran. Biotechnology Research center, Tabriz University of Medical Sciences, Tabriz, Iran. Student Research Committee, Tabriz University of Medical Sciences, Tabriz, Iran. Department of Microbiology, Bonab Branch, Islamic Azad University, Bonab, Iran. Drug Applied Research Center, Tabriz University of Medical Sciences, Tabriz, Iran. Purpose: Sumatriptan succinate (Sum) is a Serotonin 5- HT1 receptor agonist, used in the treatment of migraine. It is absorbed rapidly but incompletely when taken orally and underwent first - pass metabolism, resulting in a low bioavailability of about 15%. The aim was to design mucoadhesive buccal discs and sublingual films of Sum and metoclopramide (Met) combined to improve their bioavailability. Methods: In the current study, the microparticles and films were prepared by emulsion solvent diffusion (ESD) and solvent casting methods, respectively. Buccal-mucoadhesive microparticles and films with different drug to polymer ratios were prepared and characterized by encapsulation efficiency, particle size, DSC (Differential Scanning Calorimetric), folding endurance, mucoadhesive property and drug release studies. Results: The best drug/s to polymer ratios in films and microparticles were 1:2.7:8 (SM2) and 1:4:6 (SM4), respectively. The film of SM2 showed 11.01 mg weight, 123 µm thickness and 300 folding endurance. The production yield was 107.33% for SM4 microparticles, 323.59 µm for mean particle size and 94.53% for loading efficiency (for Sum) and 104.18% (for Met). The DSC showed no stable characteristic of Sum and Met in the drug loaded films/discs and revealed amorphous form and transition of hydrate to anhydrous form for Met. The films exhibited very good mucoadhesive properties and shorter retention time (15-30 s) in comparison with the discs (130 min). The results showed that the discs prepared had slower release than the films (p<0.05). Conclusion: Films and discs of Sum-Met combinations were successfully prepared with improved release and mucoadhesive properties.http://journals.tbzmed.ac.ir/APB/Manuscript/APB-6-119.pdfMucoadhesive;BuccalTransmucosalSumatriptanMetoclopramide |
| spellingShingle | Mitra Jelvehgari Hadi Valizadeh Sanam Ziapour Mahdieh Rahmani Seyed Hassan Montazam Saieede Soltani Comparative Study of Different Combinational Mucoadhesive Formulations of Sumatriptan-Metoclopramide Advanced Pharmaceutical Bulletin Mucoadhesive; Buccal Transmucosal Sumatriptan Metoclopramide |
| title | Comparative Study of Different
Combinational Mucoadhesive Formulations of Sumatriptan-Metoclopramide |
| title_full | Comparative Study of Different
Combinational Mucoadhesive Formulations of Sumatriptan-Metoclopramide |
| title_fullStr | Comparative Study of Different
Combinational Mucoadhesive Formulations of Sumatriptan-Metoclopramide |
| title_full_unstemmed | Comparative Study of Different
Combinational Mucoadhesive Formulations of Sumatriptan-Metoclopramide |
| title_short | Comparative Study of Different
Combinational Mucoadhesive Formulations of Sumatriptan-Metoclopramide |
| title_sort | comparative study of different combinational mucoadhesive formulations of sumatriptan metoclopramide |
| topic | Mucoadhesive; Buccal Transmucosal Sumatriptan Metoclopramide |
| url | http://journals.tbzmed.ac.ir/APB/Manuscript/APB-6-119.pdf |
| work_keys_str_mv | AT mitrajelvehgari comparativestudyofdifferentcombinationalmucoadhesiveformulationsofsumatriptanmetoclopramide AT hadivalizadeh comparativestudyofdifferentcombinationalmucoadhesiveformulationsofsumatriptanmetoclopramide AT sanamziapour comparativestudyofdifferentcombinationalmucoadhesiveformulationsofsumatriptanmetoclopramide AT mahdiehrahmani comparativestudyofdifferentcombinationalmucoadhesiveformulationsofsumatriptanmetoclopramide AT seyedhassanmontazam comparativestudyofdifferentcombinationalmucoadhesiveformulationsofsumatriptanmetoclopramide AT saieedesoltani comparativestudyofdifferentcombinationalmucoadhesiveformulationsofsumatriptanmetoclopramide |