Exploration of Neusilin<sup>®</sup> US2 as an Acceptable Filler in HPMC Matrix Systems—Comparison of Pharmacopoeial and Dynamic Biorelevant Dissolution Study
Modern pharmaceutical technology still seeks new excipients and investigates the further use in already known ones. An example is magnesium aluminometasilicate Neusilin<sup>®</sup> US2 (NEU), a commonly used inert filler with unique properties that are usable in various pharmaceutical fi...
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| Format: | Article |
| Language: | English |
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MDPI AG
2022-01-01
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| Series: | Pharmaceutics |
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| Online Access: | https://www.mdpi.com/1999-4923/14/1/127 |
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| author | Tomáš Bílik Jakub Vysloužil Martina Naiserová Jan Muselík Miroslava Pavelková Josef Mašek Drahomíra Čopová Martin Čulen Kateřina Kubová |
| author_facet | Tomáš Bílik Jakub Vysloužil Martina Naiserová Jan Muselík Miroslava Pavelková Josef Mašek Drahomíra Čopová Martin Čulen Kateřina Kubová |
| author_sort | Tomáš Bílik |
| collection | DOAJ |
| description | Modern pharmaceutical technology still seeks new excipients and investigates the further use in already known ones. An example is magnesium aluminometasilicate Neusilin<sup>®</sup> US2 (NEU), a commonly used inert filler with unique properties that are usable in various pharmaceutical fields of interest. We aimed to explore its application in hypromellose matrix systems (HPMC content 10–30%) compared to the traditionally used microcrystalline cellulose (MCC) PH 102. The properties of powder mixtures and directly compressed tablets containing individual fillers NEU or MCC, or their blend with ratios of 1.5:1, 1:1, and 0.5:1 were investigated. Besides the routine pharmaceutical testing, we have enriched the matrices’ evaluation with a biorelevant dynamic dissolution study and advanced statistical analysis. Under the USP apparatus 2 dissolution test, NEU, individually, did not provide advantages compared to MCC. The primary limitations were the <i>burst effect</i> increase followed by faster drug release at the 10–20% HPMC concentrations. However, the biorelevant dynamic dissolution study did not confirm these findings and showed similarities in dissolution profiles. It indicates the limitations of pharmacopoeial methods in matrix tablet development. Surprisingly, the NEU/MCC blend matrices at the same HPMC concentration showed technologically advantageous properties. Besides improved flowability, tablet hardness, and a positive impact on the in vitro drug dissolution profile toward zero-order kinetics, the USP 2 dissolution data of the samples N75M50 and N50M50 showed a similarity to those obtained from the dynamic biorelevant apparatus with multi-compartment structure. This finding demonstrates the more predictable in vivo behaviour of the developed matrix systems in human organisms. |
| first_indexed | 2024-03-10T00:43:15Z |
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| id | doaj.art-87f7400036d947c78f63d0cc2dd6c72a |
| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-03-10T00:43:15Z |
| publishDate | 2022-01-01 |
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| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj.art-87f7400036d947c78f63d0cc2dd6c72a2023-11-23T15:04:22ZengMDPI AGPharmaceutics1999-49232022-01-0114112710.3390/pharmaceutics14010127Exploration of Neusilin<sup>®</sup> US2 as an Acceptable Filler in HPMC Matrix Systems—Comparison of Pharmacopoeial and Dynamic Biorelevant Dissolution StudyTomáš Bílik0Jakub Vysloužil1Martina Naiserová2Jan Muselík3Miroslava Pavelková4Josef Mašek5Drahomíra Čopová6Martin Čulen7Kateřina Kubová8Department of Pharmaceutical Technology, Faculty of Pharmacy, Masaryk University, 61200 Brno, Czech RepublicDepartment of Pharmaceutical Technology, Faculty of Pharmacy, Masaryk University, 61200 Brno, Czech RepublicDepartment of Pharmaceutical Technology, Faculty of Pharmacy, Masaryk University, 61200 Brno, Czech RepublicDepartment of Pharmaceutical Technology, Faculty of Pharmacy, Masaryk University, 61200 Brno, Czech RepublicDepartment of Pharmaceutical Technology, Faculty of Pharmacy, Masaryk University, 61200 Brno, Czech RepublicDepartment of Pharmacology and Toxicology, Veterinary Research Institute, 62100 Brno, Czech RepublicDepartment of Pharmaceutical Technology, Faculty of Pharmacy, Masaryk University, 61200 Brno, Czech RepublicDepartment of Chemistry, Faculty of Pharmacy, Masaryk University, 61200 Brno, Czech RepublicDepartment of Pharmaceutical Technology, Faculty of Pharmacy, Masaryk University, 61200 Brno, Czech RepublicModern pharmaceutical technology still seeks new excipients and investigates the further use in already known ones. An example is magnesium aluminometasilicate Neusilin<sup>®</sup> US2 (NEU), a commonly used inert filler with unique properties that are usable in various pharmaceutical fields of interest. We aimed to explore its application in hypromellose matrix systems (HPMC content 10–30%) compared to the traditionally used microcrystalline cellulose (MCC) PH 102. The properties of powder mixtures and directly compressed tablets containing individual fillers NEU or MCC, or their blend with ratios of 1.5:1, 1:1, and 0.5:1 were investigated. Besides the routine pharmaceutical testing, we have enriched the matrices’ evaluation with a biorelevant dynamic dissolution study and advanced statistical analysis. Under the USP apparatus 2 dissolution test, NEU, individually, did not provide advantages compared to MCC. The primary limitations were the <i>burst effect</i> increase followed by faster drug release at the 10–20% HPMC concentrations. However, the biorelevant dynamic dissolution study did not confirm these findings and showed similarities in dissolution profiles. It indicates the limitations of pharmacopoeial methods in matrix tablet development. Surprisingly, the NEU/MCC blend matrices at the same HPMC concentration showed technologically advantageous properties. Besides improved flowability, tablet hardness, and a positive impact on the in vitro drug dissolution profile toward zero-order kinetics, the USP 2 dissolution data of the samples N75M50 and N50M50 showed a similarity to those obtained from the dynamic biorelevant apparatus with multi-compartment structure. This finding demonstrates the more predictable in vivo behaviour of the developed matrix systems in human organisms.https://www.mdpi.com/1999-4923/14/1/127matrix tabletsHPMCNeusilin<sup>®</sup> US2microcrystalline celluloseUSP apparatus 2 dissolution testdynamic dissolution study |
| spellingShingle | Tomáš Bílik Jakub Vysloužil Martina Naiserová Jan Muselík Miroslava Pavelková Josef Mašek Drahomíra Čopová Martin Čulen Kateřina Kubová Exploration of Neusilin<sup>®</sup> US2 as an Acceptable Filler in HPMC Matrix Systems—Comparison of Pharmacopoeial and Dynamic Biorelevant Dissolution Study Pharmaceutics matrix tablets HPMC Neusilin<sup>®</sup> US2 microcrystalline cellulose USP apparatus 2 dissolution test dynamic dissolution study |
| title | Exploration of Neusilin<sup>®</sup> US2 as an Acceptable Filler in HPMC Matrix Systems—Comparison of Pharmacopoeial and Dynamic Biorelevant Dissolution Study |
| title_full | Exploration of Neusilin<sup>®</sup> US2 as an Acceptable Filler in HPMC Matrix Systems—Comparison of Pharmacopoeial and Dynamic Biorelevant Dissolution Study |
| title_fullStr | Exploration of Neusilin<sup>®</sup> US2 as an Acceptable Filler in HPMC Matrix Systems—Comparison of Pharmacopoeial and Dynamic Biorelevant Dissolution Study |
| title_full_unstemmed | Exploration of Neusilin<sup>®</sup> US2 as an Acceptable Filler in HPMC Matrix Systems—Comparison of Pharmacopoeial and Dynamic Biorelevant Dissolution Study |
| title_short | Exploration of Neusilin<sup>®</sup> US2 as an Acceptable Filler in HPMC Matrix Systems—Comparison of Pharmacopoeial and Dynamic Biorelevant Dissolution Study |
| title_sort | exploration of neusilin sup r sup us2 as an acceptable filler in hpmc matrix systems comparison of pharmacopoeial and dynamic biorelevant dissolution study |
| topic | matrix tablets HPMC Neusilin<sup>®</sup> US2 microcrystalline cellulose USP apparatus 2 dissolution test dynamic dissolution study |
| url | https://www.mdpi.com/1999-4923/14/1/127 |
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