Comparative evaluation of mechanical properties of lactose-based excipients co-processed with lipophilic glycerides as meltable binders
Само за регистроване кориснике
2021
Аутори
Ćirin-Varađan, SlobodankaĐuriš, Jelena
Mirković, Miljana M.
Ivanović, Marija M.
Parojčić, Jelena
Aleksić, Ivana
Чланак у часопису (Објављена верзија)
Метаподаци
Приказ свих података о документуАпстракт
The introduction of the high-speed tableting machines and the lack of excipients with good flow and compaction properties required for direct compression process have increased research interest in the development of co-processed excipients. Melt granulation, as an environmentally friendly and cost-effective method, has recently been recognized as a promising co-processing technique. The aim of the present study was to prepare lipid-based co-processed excipients by in situ fluidized bed melt granulation and to investigated their suitability for direct compression process. Lactose monohydrate was co-processed with glyceryl dibehenate (Compritol® 888 ATO) or glyceryl palmitostearate (Precirol® ATO 5), as lipophilic meltable binders. Besides the flowability testing, dynamic compaction analysis was applied for thorough investigation into the tableting properties of developed co-processed excipients. Solid state characterization, performed by means of XRPD and DRIFT, confirmed the absence o...f chemical changes of the single components of co-processed excipients. Co-processed excipients showed improved flowability in comparison with single ingredients and corresponding physical mixtures. Novel co-processed excipients were found to have better tabletability profiles than physical mixtures of the ingredients, and were able to retain acceptable tensile strength values at high content of paracetamol in tableting mixture. Tablets with high tensile strength could be obtained with less work of compression needed in comparison with the commercial lactose-based excipients. Furthermore, novel lipid-based co-processed excipients were found to be highly superior regarding the antiadhesive and lubricating properties, with no additional lubricants required.
Кључне речи:
Compritol® 888 ATO / Fluid bed / Melt granulation / Novel co-processed excipient / Precirol® ATO 5Извор:
Journal of Drug Delivery Science and Technology, 2021, 102981-Финансирање / пројекти:
- Министарство науке, технолошког развоја и иновација Републике Србије, институционално финансирање - 200161 (Универзитет у Београду, Фармацеутски факултет) (RS-MESTD-inst-2020-200161)
DOI: 10.1016/j.jddst.2021.102981
ISSN: 1773-2247
WoS: 00078809020000
Scopus: 2-s2.0-85119904365
Колекције
Институција/група
VinčaTY - JOUR AU - Ćirin-Varađan, Slobodanka AU - Đuriš, Jelena AU - Mirković, Miljana M. AU - Ivanović, Marija M. AU - Parojčić, Jelena AU - Aleksić, Ivana PY - 2021 UR - https://vinar.vin.bg.ac.rs/handle/123456789/10074 AB - The introduction of the high-speed tableting machines and the lack of excipients with good flow and compaction properties required for direct compression process have increased research interest in the development of co-processed excipients. Melt granulation, as an environmentally friendly and cost-effective method, has recently been recognized as a promising co-processing technique. The aim of the present study was to prepare lipid-based co-processed excipients by in situ fluidized bed melt granulation and to investigated their suitability for direct compression process. Lactose monohydrate was co-processed with glyceryl dibehenate (Compritol® 888 ATO) or glyceryl palmitostearate (Precirol® ATO 5), as lipophilic meltable binders. Besides the flowability testing, dynamic compaction analysis was applied for thorough investigation into the tableting properties of developed co-processed excipients. Solid state characterization, performed by means of XRPD and DRIFT, confirmed the absence of chemical changes of the single components of co-processed excipients. Co-processed excipients showed improved flowability in comparison with single ingredients and corresponding physical mixtures. Novel co-processed excipients were found to have better tabletability profiles than physical mixtures of the ingredients, and were able to retain acceptable tensile strength values at high content of paracetamol in tableting mixture. Tablets with high tensile strength could be obtained with less work of compression needed in comparison with the commercial lactose-based excipients. Furthermore, novel lipid-based co-processed excipients were found to be highly superior regarding the antiadhesive and lubricating properties, with no additional lubricants required. T2 - Journal of Drug Delivery Science and Technology T1 - Comparative evaluation of mechanical properties of lactose-based excipients co-processed with lipophilic glycerides as meltable binders SP - 102981 DO - 10.1016/j.jddst.2021.102981 ER -
@article{ author = "Ćirin-Varađan, Slobodanka and Đuriš, Jelena and Mirković, Miljana M. and Ivanović, Marija M. and Parojčić, Jelena and Aleksić, Ivana", year = "2021", abstract = "The introduction of the high-speed tableting machines and the lack of excipients with good flow and compaction properties required for direct compression process have increased research interest in the development of co-processed excipients. Melt granulation, as an environmentally friendly and cost-effective method, has recently been recognized as a promising co-processing technique. The aim of the present study was to prepare lipid-based co-processed excipients by in situ fluidized bed melt granulation and to investigated their suitability for direct compression process. Lactose monohydrate was co-processed with glyceryl dibehenate (Compritol® 888 ATO) or glyceryl palmitostearate (Precirol® ATO 5), as lipophilic meltable binders. Besides the flowability testing, dynamic compaction analysis was applied for thorough investigation into the tableting properties of developed co-processed excipients. Solid state characterization, performed by means of XRPD and DRIFT, confirmed the absence of chemical changes of the single components of co-processed excipients. Co-processed excipients showed improved flowability in comparison with single ingredients and corresponding physical mixtures. Novel co-processed excipients were found to have better tabletability profiles than physical mixtures of the ingredients, and were able to retain acceptable tensile strength values at high content of paracetamol in tableting mixture. Tablets with high tensile strength could be obtained with less work of compression needed in comparison with the commercial lactose-based excipients. Furthermore, novel lipid-based co-processed excipients were found to be highly superior regarding the antiadhesive and lubricating properties, with no additional lubricants required.", journal = "Journal of Drug Delivery Science and Technology", title = "Comparative evaluation of mechanical properties of lactose-based excipients co-processed with lipophilic glycerides as meltable binders", pages = "102981", doi = "10.1016/j.jddst.2021.102981" }
Ćirin-Varađan, S., Đuriš, J., Mirković, M. M., Ivanović, M. M., Parojčić, J.,& Aleksić, I.. (2021). Comparative evaluation of mechanical properties of lactose-based excipients co-processed with lipophilic glycerides as meltable binders. in Journal of Drug Delivery Science and Technology, 102981. https://doi.org/10.1016/j.jddst.2021.102981
Ćirin-Varađan S, Đuriš J, Mirković MM, Ivanović MM, Parojčić J, Aleksić I. Comparative evaluation of mechanical properties of lactose-based excipients co-processed with lipophilic glycerides as meltable binders. in Journal of Drug Delivery Science and Technology. 2021;:102981. doi:10.1016/j.jddst.2021.102981 .
Ćirin-Varađan, Slobodanka, Đuriš, Jelena, Mirković, Miljana M., Ivanović, Marija M., Parojčić, Jelena, Aleksić, Ivana, "Comparative evaluation of mechanical properties of lactose-based excipients co-processed with lipophilic glycerides as meltable binders" in Journal of Drug Delivery Science and Technology (2021):102981, https://doi.org/10.1016/j.jddst.2021.102981 . .