Experimental Design Approach for the Formulation of Controlled Release Buccal Bilayer Tablets of Carvedilol
Introduction: The absolute bioavailability of carvedilol is ~25% - 35% even though it rapidly and extensively absorbed following oral administration due to a significant degree of presystemic metabolism. The purpose of this study was to develop controlled release mucoadhesive buccal bilayer tablet o...
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| Format: | Article |
| Language: | English |
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Wolters Kluwer – Medknow Publications
2018-07-01
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| Series: | Journal of Integrated Health Sciences |
| Subjects: | |
| Online Access: | https://journals.lww.com/10.4103/JIHS.JIHS_19_18 |
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| author | Vinodkumar D. Ramani Girish U. Sailor Maulik M. Patel Ghanshyam R. Parmar Avinash K. Seth |
| author_facet | Vinodkumar D. Ramani Girish U. Sailor Maulik M. Patel Ghanshyam R. Parmar Avinash K. Seth |
| author_sort | Vinodkumar D. Ramani |
| collection | DOAJ |
| description | Introduction:
The absolute bioavailability of carvedilol is ~25% - 35% even though it rapidly and extensively absorbed following oral administration due to a significant degree of presystemic metabolism. The purpose of this study was to develop controlled release mucoadhesive buccal bilayer tablet of carvedilol using HPMC K4M and carbomer 934 as the mucoadhesive polymer.
Method:
The formulation optimization was performed using 32 full factorial design to study the effect of independent variables viz. HPMC K4M (X1), carbomer 934 (X2) levels on % drug release in 8 h (Y1), mucoadhesive time (Y2) in buccal cavity and mucoadhesive strength (Y3). The tablets were evaluated for its appearance, thickness, diameter, weight uniformity, content uniformity, surface pH, swelling index and in vitro drug permeation.
Results:
The optimized formulation evaluated for responses which showed an in vitro drug release of 81.3% in 8 h, mucoadhesive strength 11.2 g with mucoadhesive time of 471.32 min and demonstrated case-II transport mechanism. The results of response variables were found to be very close with the predicted values. These results support the fact that 32 full factorial designs with desirability function could be effectively used in optimization of controlled release mucoadhesive buccal bilayer tablets.
Conclusion:
It can be concluded that buccal route can be one of the alternatives available to bypass the extensive hepatic first-pass metabolism and to improve the bioavailability of carvedilol. |
| format | Article |
| id | doaj-art-40de110bd13e4838949dc2896cd8948b |
| institution | OA Journals |
| issn | 2347-6486 2347-6494 |
| language | English |
| publishDate | 2018-07-01 |
| publisher | Wolters Kluwer – Medknow Publications |
| record_format | Article |
| series | Journal of Integrated Health Sciences |
| spelling | doaj-art-40de110bd13e4838949dc2896cd8948b2025-08-20T02:26:37ZengWolters Kluwer – Medknow PublicationsJournal of Integrated Health Sciences2347-64862347-64942018-07-0162535910.4103/JIHS.JIHS_19_18Experimental Design Approach for the Formulation of Controlled Release Buccal Bilayer Tablets of CarvedilolVinodkumar D. RamaniGirish U. SailorMaulik M. PatelGhanshyam R. ParmarAvinash K. SethIntroduction: The absolute bioavailability of carvedilol is ~25% - 35% even though it rapidly and extensively absorbed following oral administration due to a significant degree of presystemic metabolism. The purpose of this study was to develop controlled release mucoadhesive buccal bilayer tablet of carvedilol using HPMC K4M and carbomer 934 as the mucoadhesive polymer. Method: The formulation optimization was performed using 32 full factorial design to study the effect of independent variables viz. HPMC K4M (X1), carbomer 934 (X2) levels on % drug release in 8 h (Y1), mucoadhesive time (Y2) in buccal cavity and mucoadhesive strength (Y3). The tablets were evaluated for its appearance, thickness, diameter, weight uniformity, content uniformity, surface pH, swelling index and in vitro drug permeation. Results: The optimized formulation evaluated for responses which showed an in vitro drug release of 81.3% in 8 h, mucoadhesive strength 11.2 g with mucoadhesive time of 471.32 min and demonstrated case-II transport mechanism. The results of response variables were found to be very close with the predicted values. These results support the fact that 32 full factorial designs with desirability function could be effectively used in optimization of controlled release mucoadhesive buccal bilayer tablets. Conclusion: It can be concluded that buccal route can be one of the alternatives available to bypass the extensive hepatic first-pass metabolism and to improve the bioavailability of carvedilol.https://journals.lww.com/10.4103/JIHS.JIHS_19_18buccal bilayer tabletscarvediloldesirabilityfactorial designmucoadhesivebuccal bilayer tabletscarvediloldesirabilityfactorial designmucoadhesive |
| spellingShingle | Vinodkumar D. Ramani Girish U. Sailor Maulik M. Patel Ghanshyam R. Parmar Avinash K. Seth Experimental Design Approach for the Formulation of Controlled Release Buccal Bilayer Tablets of Carvedilol Journal of Integrated Health Sciences buccal bilayer tablets carvedilol desirability factorial design mucoadhesivebuccal bilayer tablets carvedilol desirability factorial design mucoadhesive |
| title | Experimental Design Approach for the Formulation of Controlled Release Buccal Bilayer Tablets of Carvedilol |
| title_full | Experimental Design Approach for the Formulation of Controlled Release Buccal Bilayer Tablets of Carvedilol |
| title_fullStr | Experimental Design Approach for the Formulation of Controlled Release Buccal Bilayer Tablets of Carvedilol |
| title_full_unstemmed | Experimental Design Approach for the Formulation of Controlled Release Buccal Bilayer Tablets of Carvedilol |
| title_short | Experimental Design Approach for the Formulation of Controlled Release Buccal Bilayer Tablets of Carvedilol |
| title_sort | experimental design approach for the formulation of controlled release buccal bilayer tablets of carvedilol |
| topic | buccal bilayer tablets carvedilol desirability factorial design mucoadhesivebuccal bilayer tablets carvedilol desirability factorial design mucoadhesive |
| url | https://journals.lww.com/10.4103/JIHS.JIHS_19_18 |
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