Development and Comparison of Various Coated Hard Capsules Suitable for Enteric Administration to Small Patient Cohorts
Pharmaceutical technology offers several options for protecting substances from acidic environments, such as encapsulation in enteric capsules or dosage form with enteric coating. However, commercial enteric capsules do not always meet limits for pharmacopeial delayed release, and the coating proces...
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| Format: | Article |
| Language: | English |
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MDPI AG
2022-07-01
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| Series: | Pharmaceutics |
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| Online Access: | https://www.mdpi.com/1999-4923/14/8/1577 |
| _version_ | 1797408368305897472 |
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| author | Nicole Fülöpová Sylvie Pavloková Ivan DeBono David Vetchý Aleš Franc |
| author_facet | Nicole Fülöpová Sylvie Pavloková Ivan DeBono David Vetchý Aleš Franc |
| author_sort | Nicole Fülöpová |
| collection | DOAJ |
| description | Pharmaceutical technology offers several options for protecting substances from acidic environments, such as encapsulation in enteric capsules or dosage form with enteric coating. However, commercial enteric capsules do not always meet limits for pharmacopeial delayed release, and the coating process is generally challenging. Preparing small enteric batches suitable for clinical use is, therefore, an unsolved problem. This experiment offers a simple coating process of DRcaps<sup>TM</sup> capsules based on hypromellose (HPMC) and gellan gum to achieve small intestine administration. In addition, DRcaps<sup>TM</sup> capsules were compared to hard gelatin capsules to evaluate the suitability of the coating method. Both capsules were immersed in dispersions of Eudragit<sup>®</sup> S 100, Acryl-EZE<sup>®,</sup> and Cellacefate at concentrations of 10.0, 15.0, and 20.0% and dried. Coated capsules were evaluated by electron microscopy, disintegration, and dissolution test with a two-step pH change (from 1.2 to 6.8, then to 7.5) to simulate passage through the digestive tract. DRcaps<sup>TM</sup> capsules coated with Eudragit<sup>®</sup> S and Cellacefate achieved acid resistance. While samples coated with Eudragit<sup>®</sup> S released their contents within 360 min at pH 6.8 (small intestine), regardless of polymer concentration, capsules with 15.0 and 20.0% coatings of Cellacefate released content at pH 7.5 (colon) within 435 and 495 min, respectively. |
| first_indexed | 2024-03-09T03:58:27Z |
| format | Article |
| id | doaj.art-5b10a03843f9471c99482891d3a82292 |
| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-03-09T03:58:27Z |
| publishDate | 2022-07-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj.art-5b10a03843f9471c99482891d3a822922023-12-03T14:17:03ZengMDPI AGPharmaceutics1999-49232022-07-01148157710.3390/pharmaceutics14081577Development and Comparison of Various Coated Hard Capsules Suitable for Enteric Administration to Small Patient CohortsNicole Fülöpová0Sylvie Pavloková1Ivan DeBono2David Vetchý3Aleš Franc4Department of Pharmaceutical Technology, Faculty of Pharmacy, Masaryk University, 612 42 Brno, Czech RepublicDepartment of Pharmaceutical Technology, Faculty of Pharmacy, Masaryk University, 612 42 Brno, Czech RepublicDepartment of Pharmacy, Mater Dei Hospital, 2090 Msida, MaltaDepartment of Pharmaceutical Technology, Faculty of Pharmacy, Masaryk University, 612 42 Brno, Czech RepublicDepartment of Pharmaceutical Technology, Faculty of Pharmacy, Masaryk University, 612 42 Brno, Czech RepublicPharmaceutical technology offers several options for protecting substances from acidic environments, such as encapsulation in enteric capsules or dosage form with enteric coating. However, commercial enteric capsules do not always meet limits for pharmacopeial delayed release, and the coating process is generally challenging. Preparing small enteric batches suitable for clinical use is, therefore, an unsolved problem. This experiment offers a simple coating process of DRcaps<sup>TM</sup> capsules based on hypromellose (HPMC) and gellan gum to achieve small intestine administration. In addition, DRcaps<sup>TM</sup> capsules were compared to hard gelatin capsules to evaluate the suitability of the coating method. Both capsules were immersed in dispersions of Eudragit<sup>®</sup> S 100, Acryl-EZE<sup>®,</sup> and Cellacefate at concentrations of 10.0, 15.0, and 20.0% and dried. Coated capsules were evaluated by electron microscopy, disintegration, and dissolution test with a two-step pH change (from 1.2 to 6.8, then to 7.5) to simulate passage through the digestive tract. DRcaps<sup>TM</sup> capsules coated with Eudragit<sup>®</sup> S and Cellacefate achieved acid resistance. While samples coated with Eudragit<sup>®</sup> S released their contents within 360 min at pH 6.8 (small intestine), regardless of polymer concentration, capsules with 15.0 and 20.0% coatings of Cellacefate released content at pH 7.5 (colon) within 435 and 495 min, respectively.https://www.mdpi.com/1999-4923/14/8/1577DRcaps<sup>TM</sup> capsuleshard gelatin capsulesEudragit<sup>®</sup> Senteric coatingimmersion methodprincipal component analysis |
| spellingShingle | Nicole Fülöpová Sylvie Pavloková Ivan DeBono David Vetchý Aleš Franc Development and Comparison of Various Coated Hard Capsules Suitable for Enteric Administration to Small Patient Cohorts Pharmaceutics DRcaps<sup>TM</sup> capsules hard gelatin capsules Eudragit<sup>®</sup> S enteric coating immersion method principal component analysis |
| title | Development and Comparison of Various Coated Hard Capsules Suitable for Enteric Administration to Small Patient Cohorts |
| title_full | Development and Comparison of Various Coated Hard Capsules Suitable for Enteric Administration to Small Patient Cohorts |
| title_fullStr | Development and Comparison of Various Coated Hard Capsules Suitable for Enteric Administration to Small Patient Cohorts |
| title_full_unstemmed | Development and Comparison of Various Coated Hard Capsules Suitable for Enteric Administration to Small Patient Cohorts |
| title_short | Development and Comparison of Various Coated Hard Capsules Suitable for Enteric Administration to Small Patient Cohorts |
| title_sort | development and comparison of various coated hard capsules suitable for enteric administration to small patient cohorts |
| topic | DRcaps<sup>TM</sup> capsules hard gelatin capsules Eudragit<sup>®</sup> S enteric coating immersion method principal component analysis |
| url | https://www.mdpi.com/1999-4923/14/8/1577 |
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