Improving tableting performance of lactose monohydrate by fluid-bed melt granulation co-processing
2021
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Co-processing is commonly used approach to improve functional characteristics of pharmaceutical excipients to become suitable for tablet production by direct compression. This study aimed to improve tableting characteristics of lactose monohydrate (LMH) by co-processing by fluid-bed melt granulation with addition of hydrophilic (PEG 4000 and poloxamer 188) and lipophilic (glyceryl palmitostearate) meltable binders. In addition to binding purpose, hydrophilic and lipophilic excipients were added to achieve self-lubricating properties of mixture. Co-processed mixtures exhibit superior flow properties compared to pure LMH and comparable or better flowability relative to commercial excipient Ludipress®. Compaction of mixtures co-processed with 20% PEG 4000 and 20% poloxamer 188 resulted in tablets with acceptable tensile strength (>2 MPa) and good lubricating properties (ejection and detachment stress values below 5 MPa) in a wide range of compression pressures. While the best lubricating ...properties were observed when glyceryl palmitostearate was used as meltable binder, obtained tablets failed to fulfil required mechanical characteristics. Although addition of meltable binder improves interparticle bonding, disintegration time was not prolonged compared to commercial excipient Ludipress®. Co-processed mixtures containing 20% of either PEG 4000 or poloxamer 188 showed superior tabletability and lubricant properties relative to LMH and Ludipress® and can be good candidates for tablet production by direct compression.
Ključne reči:
Direct compression / Co-processing / Fluid-bed melt granulation / Lactose monohydrate / Self-lubricating excipients / Tableting behaviourIzvor:
Pharmaceutics, 2021, 13, 12Izdavač:
- MDPI
Finansiranje / projekti:
- Ministarstvo nauke, tehnološkog razvoja i inovacija Republike Srbije, institucionalno finansiranje - 200161 (Univerzitet u Beogradu, Farmaceutski fakultet) (RS-MESTD-inst-2020-200161)
DOI: 10.3390/pharmaceutics13122165
ISSN: 1999-4923
WoS: 000736789500001
Scopus: 2-s2.0-85121468115
Institucija/grupa
PharmacyTY - JOUR AU - Medarević, Đorđe AU - Đuriš, Jelena AU - Krkobabić, Mirjana AU - Ibrić, Svetlana PY - 2021 UR - https://farfar.pharmacy.bg.ac.rs/handle/123456789/4013 AB - Co-processing is commonly used approach to improve functional characteristics of pharmaceutical excipients to become suitable for tablet production by direct compression. This study aimed to improve tableting characteristics of lactose monohydrate (LMH) by co-processing by fluid-bed melt granulation with addition of hydrophilic (PEG 4000 and poloxamer 188) and lipophilic (glyceryl palmitostearate) meltable binders. In addition to binding purpose, hydrophilic and lipophilic excipients were added to achieve self-lubricating properties of mixture. Co-processed mixtures exhibit superior flow properties compared to pure LMH and comparable or better flowability relative to commercial excipient Ludipress®. Compaction of mixtures co-processed with 20% PEG 4000 and 20% poloxamer 188 resulted in tablets with acceptable tensile strength (>2 MPa) and good lubricating properties (ejection and detachment stress values below 5 MPa) in a wide range of compression pressures. While the best lubricating properties were observed when glyceryl palmitostearate was used as meltable binder, obtained tablets failed to fulfil required mechanical characteristics. Although addition of meltable binder improves interparticle bonding, disintegration time was not prolonged compared to commercial excipient Ludipress®. Co-processed mixtures containing 20% of either PEG 4000 or poloxamer 188 showed superior tabletability and lubricant properties relative to LMH and Ludipress® and can be good candidates for tablet production by direct compression. PB - MDPI T2 - Pharmaceutics T1 - Improving tableting performance of lactose monohydrate by fluid-bed melt granulation co-processing VL - 13 IS - 12 DO - 10.3390/pharmaceutics13122165 ER -
@article{ author = "Medarević, Đorđe and Đuriš, Jelena and Krkobabić, Mirjana and Ibrić, Svetlana", year = "2021", abstract = "Co-processing is commonly used approach to improve functional characteristics of pharmaceutical excipients to become suitable for tablet production by direct compression. This study aimed to improve tableting characteristics of lactose monohydrate (LMH) by co-processing by fluid-bed melt granulation with addition of hydrophilic (PEG 4000 and poloxamer 188) and lipophilic (glyceryl palmitostearate) meltable binders. In addition to binding purpose, hydrophilic and lipophilic excipients were added to achieve self-lubricating properties of mixture. Co-processed mixtures exhibit superior flow properties compared to pure LMH and comparable or better flowability relative to commercial excipient Ludipress®. Compaction of mixtures co-processed with 20% PEG 4000 and 20% poloxamer 188 resulted in tablets with acceptable tensile strength (>2 MPa) and good lubricating properties (ejection and detachment stress values below 5 MPa) in a wide range of compression pressures. While the best lubricating properties were observed when glyceryl palmitostearate was used as meltable binder, obtained tablets failed to fulfil required mechanical characteristics. Although addition of meltable binder improves interparticle bonding, disintegration time was not prolonged compared to commercial excipient Ludipress®. Co-processed mixtures containing 20% of either PEG 4000 or poloxamer 188 showed superior tabletability and lubricant properties relative to LMH and Ludipress® and can be good candidates for tablet production by direct compression.", publisher = "MDPI", journal = "Pharmaceutics", title = "Improving tableting performance of lactose monohydrate by fluid-bed melt granulation co-processing", volume = "13", number = "12", doi = "10.3390/pharmaceutics13122165" }
Medarević, Đ., Đuriš, J., Krkobabić, M.,& Ibrić, S.. (2021). Improving tableting performance of lactose monohydrate by fluid-bed melt granulation co-processing. in Pharmaceutics MDPI., 13(12). https://doi.org/10.3390/pharmaceutics13122165
Medarević Đ, Đuriš J, Krkobabić M, Ibrić S. Improving tableting performance of lactose monohydrate by fluid-bed melt granulation co-processing. in Pharmaceutics. 2021;13(12). doi:10.3390/pharmaceutics13122165 .
Medarević, Đorđe, Đuriš, Jelena, Krkobabić, Mirjana, Ibrić, Svetlana, "Improving tableting performance of lactose monohydrate by fluid-bed melt granulation co-processing" in Pharmaceutics, 13, no. 12 (2021), https://doi.org/10.3390/pharmaceutics13122165 . .