Comprehensive understanding of tablet disintegration processes

Kód výsledku v IS VaVaI

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Výsledek na webu

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DOI - Digital Object Identifier

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Jazyk výsledku

angličtina

Název v původním jazyce

Comprehensive understanding of tablet disintegration processes

Popis výsledku v původním jazyce

It is commonly known that composition, excipients and manufacturing process significantly affect behaviour of the pharmaceutical tablets in aqueous media. Tablets consisting of ibuprofen and lactose (ibuprofen content: 0.2 ? 0.5 w/w) and tableted at different compaction pressures (low, medium, high) were prepared and subjected to tests exploring their dissolution behaviour, mechanical properties, wettability, liquid penetration and surface characteristics. Certified dissolution tests showed differences in dissolution rate between 0.2/0.3 and 0.4/0.5 tablets, while compaction pressure did not play important role. It was proved, that compaction pressure does not affect contact angle, which is only a function of the tablet composition. Further experiments showed that compaction pressure affects final soaking time, where this time increases not only with compaction pressure, but also with ibuprofen content. MRI results showed that higher concentration of ibuprofen leads to slower disintegration. Higher compaction pressure applied in the tabletting process slows down the disintegration and dissolution processes in the tablets regardless the concentration of ibuprofen. There is a surface erosion of the tablet observed, when exposed to dissolution medium. Characteristic ibuprofen clusters appear and their amount increases with increasing ibuprofen content. These clusters significantly differ from primary particles and are present in case of all compaction pressures and compositions. Dissolution tests in discriminative conditions (lactose dissolution prevented) showed significant decrease in ibuprofen dissolution rate, which might indicate the presence of the clusters formed by compressed ibuprofen crystals covered in lactose. The other interesting discovery concerns with the tablet disintegration and its driving force. During the dissolution tests it was observed that in case of 0.2 tablets disintegration occurs independently on the dissolution medium. These findings lead to the idea of the disintegration driven by affinity of the hydrophobic substance to the solvent, which facilitates water penetration and subsequent disintegration.

Název v anglickém jazyce

Comprehensive understanding of tablet disintegration processes

Popis výsledku anglicky

It is commonly known that composition, excipients and manufacturing process significantly affect behaviour of the pharmaceutical tablets in aqueous media. Tablets consisting of ibuprofen and lactose (ibuprofen content: 0.2 ? 0.5 w/w) and tableted at different compaction pressures (low, medium, high) were prepared and subjected to tests exploring their dissolution behaviour, mechanical properties, wettability, liquid penetration and surface characteristics. Certified dissolution tests showed differences in dissolution rate between 0.2/0.3 and 0.4/0.5 tablets, while compaction pressure did not play important role. It was proved, that compaction pressure does not affect contact angle, which is only a function of the tablet composition. Further experiments showed that compaction pressure affects final soaking time, where this time increases not only with compaction pressure, but also with ibuprofen content. MRI results showed that higher concentration of ibuprofen leads to slower disintegration. Higher compaction pressure applied in the tabletting process slows down the disintegration and dissolution processes in the tablets regardless the concentration of ibuprofen. There is a surface erosion of the tablet observed, when exposed to dissolution medium. Characteristic ibuprofen clusters appear and their amount increases with increasing ibuprofen content. These clusters significantly differ from primary particles and are present in case of all compaction pressures and compositions. Dissolution tests in discriminative conditions (lactose dissolution prevented) showed significant decrease in ibuprofen dissolution rate, which might indicate the presence of the clusters formed by compressed ibuprofen crystals covered in lactose. The other interesting discovery concerns with the tablet disintegration and its driving force. During the dissolution tests it was observed that in case of 0.2 tablets disintegration occurs independently on the dissolution medium. These findings lead to the idea of the disintegration driven by affinity of the hydrophobic substance to the solvent, which facilitates water penetration and subsequent disintegration.

Druh

D - Stať ve sborníku

CEP obor

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OECD FORD obor

20401 - Chemical engineering (plants, products)

Projekt

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Návaznosti

S - Specificky vyzkum na vysokych skolach

Rok uplatnění

2017

Kód důvěrnosti údajů

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Název statě ve sborníku

PROCEEDINGS 44th International Conference of the Slovak Society of Chemical Engineering

ISBN

978-80-89597-58-1

ISSN

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e-ISSN

neuvedeno

Počet stran výsledku

10

Strana od-do

649-658

Název nakladatele

Slovak Society of Chemical Engineering

Místo vydání

Bratislava

Místo konání akce

Demänovská dolina

Datum konání akce

22. 5. 2017

Typ akce podle státní příslušnosti

WRD - Celosvětová akce

Kód UT WoS článku

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