Exploration of Neusilin® US2 as an Acceptable Filler in HPMC
Matrix Systems—Comparison of Pharmacopoeial and Dynamic
Biorelevant Dissolution Study

J 2022

Exploration of Neusilin® US2 as an Acceptable Filler in HPMC Matrix Systems—Comparison of Pharmacopoeial and Dynamic Biorelevant Dissolution Study

BÍLIK, Tomáš, Jakub VYSLOUŽIL, Martina NAISEROVÁ, Jan MUSELÍK, Miroslava PAVELKOVÁ et. al.

Basic information

Original name

Exploration of Neusilin® US2 as an Acceptable Filler in HPMC Matrix Systems—Comparison of Pharmacopoeial and Dynamic Biorelevant Dissolution Study

Authors

BÍLIK, Tomáš (203 Czech Republic, belonging to the institution), Jakub VYSLOUŽIL (203 Czech Republic, belonging to the institution), Martina NAISEROVÁ (203 Czech Republic, belonging to the institution), Jan MUSELÍK (203 Czech Republic, belonging to the institution), Miroslava PAVELKOVÁ (203 Czech Republic, belonging to the institution), Josef MAŠEK (203 Czech Republic), D. ČOPOVÁ (703 Slovakia) and Kateřina KUBOVÁ (203 Czech Republic, guarantor, belonging to the institution)

Edition

Pharmaceutics, BASEL, MDPI, 2022, 1999-4923

Other information

Language

English

Type of outcome

Článek v odborném periodiku

Field of Study

30104 Pharmacology and pharmacy

Country of publisher

Switzerland

Confidentiality degree

není předmětem státního či obchodního tajemství

References:

URL

Impact factor

Impact factor: 5.400

RIV identification code

RIV/00216224:14160/22:00125248

Organization unit

Faculty of Pharmacy

DOI

http://dx.doi.org/10.3390/pharmaceutics14010127

UT WoS

000759108700001

Keywords in English

Dynamic dissolution study; HPMC; Matrix tablets; Microcrystalline cellulose; Neusilin® US2; USP apparatus 2 dissolution test

Abstract

V originále

Modern pharmaceutical technology still seeks new excipients and investigates the further use in already known ones. An example is magnesium aluminometasilicate Neusilin® 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 burst effect 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.

Links

MUNI/A/1574/2020, interní kód MU

Name: Pokročilé technologie pro přípravu a hodnocení částicových systémů

Investor: Masaryk University

Citovat

BÍLIK, Tomáš, Jakub VYSLOUŽIL, Martina NAISEROVÁ, Jan MUSELÍK, Miroslava PAVELKOVÁ, Josef MAŠEK, D. ČOPOVÁ and Kateřina KUBOVÁ. Exploration of Neusilin® US2 as an Acceptable Filler in HPMC Matrix Systems—Comparison of Pharmacopoeial and Dynamic Biorelevant Dissolution Study. Pharmaceutics. BASEL: MDPI, 2022, vol. 14, No 1, p. 1-18. ISSN 1999-4923. Available from: https://dx.doi.org/10.3390/pharmaceutics14010127.

@article{1826403,
   author = {Bílik, Tomáš and Vysloužil, Jakub and Naiserová, Martina and Muselík, Jan and Pavelková, Miroslava and Mašek, Josef and Čopová, D. and Kubová, Kateřina},
   article_location = {BASEL},
   article_number = {1},
   doi = {http://dx.doi.org/10.3390/pharmaceutics14010127},
   keywords = {Dynamic dissolution study; HPMC; Matrix tablets; Microcrystalline cellulose; Neusilin® US2; USP apparatus 2 dissolution test},
   language = {eng},
   issn = {1999-4923},
   journal = {Pharmaceutics},
   title = {Exploration of Neusilin® US2 as an Acceptable Filler in HPMC Matrix Systems—Comparison of Pharmacopoeial and Dynamic Biorelevant Dissolution Study},
   url = {https://www.mdpi.com/1999-4923/14/1/127},
   volume = {14},
   year = {2022}
}

TY  - JOUR
ID  - 1826403
AU  - Bílik, Tomáš - Vysloužil, Jakub - Naiserová, Martina - Muselík, Jan - Pavelková, Miroslava - Mašek, Josef - Čopová, D. - Kubová, Kateřina
PY  - 2022
TI  - Exploration of Neusilin® US2 as an Acceptable Filler in HPMC Matrix Systems—Comparison of Pharmacopoeial and Dynamic Biorelevant Dissolution Study
JF  - Pharmaceutics
VL  - 14
IS  - 1
SP  - 1-18
EP  - 1-18
PB  - MDPI
SN  - 19994923
KW  - Dynamic dissolution study
KW  - HPMC
KW  - Matrix tablets
KW  - Microcrystalline cellulose
KW  - Neusilin® US2
KW  - USP apparatus 2 dissolution test
UR  - https://www.mdpi.com/1999-4923/14/1/127
N2  - Modern pharmaceutical technology still seeks new excipients and investigates the further use in already known ones. An example is magnesium aluminometasilicate Neusilin® 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 burst effect 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.
ER  -

BÍLIK, Tomáš, Jakub VYSLOUŽIL, Martina NAISEROVÁ, Jan MUSELÍK, Miroslava PAVELKOVÁ, Josef MAŠEK, D. ČOPOVÁ and Kateřina KUBOVÁ. Exploration of Neusilin® US2 as an Acceptable Filler in HPMC Matrix Systems—Comparison of Pharmacopoeial and Dynamic Biorelevant Dissolution Study. \textit{Pharmaceutics}. BASEL: MDPI, 2022, vol.~14, No~1, p.~1-18. ISSN~1999-4923. Available from: https://dx.doi.org/10.3390/pharmaceutics14010127.

Detailed Information on Publication Record