Spray coating as a powerful technique in preparation of solid dispersions with enhanced desloratadine dissolution rate
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2013
Authors
Kolasinac, NemanjaKachrimanis, Kyriakos
Đuriš, Jelena

Homšek, Irena
Grujić, Branka
Ibrić, Svetlana

Article (Published version)

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Solid dispersion systems have been widely used to enhance dissolution rate and oral bioavailability of poorly water-soluble drugs. However, the formulation process development and scale-up present a number of difficulties which has greatly limited their commercial applications. In this study, solid dispersions (SDs) of desloratadine (DSL) with povidone (PVP) and crospovidone (cPVP) were prepared by spray coating technique. The process involved the spray application of 96% ethanol solution of DSL and PVP/cPVP, and subsequent deposition of the coprecipitates onto microcrystalline cellulose pellets during drying by air flow in a mini spray coater. The results from the present study demonstrated that the spray coating process is efficient in preparing SDs with enhanced drug dissolution rate and it is highly efficient in organic solvent removal. Both PVP and cPVP greatly improved drug dissolution rate by SDs, with PVP showing better solubilization capability. Very fast drug dissolution rate... is achieved from SDs containing PVP regardless of differences in K grade. SD with smaller particles of cPVP have higher drug dissolution rate in comparison to the cPVP with larger particles. Results from physical state characterization indicate that DSL in SDs exist in the amorphous (high free-energy) state which is probably stabilized by PVP/cPVP. After 6-month accelerated stability study, DSL remains amorphous, while PVP and cPVP act as anti-plasticizing agents, offering efficient steric hindrance for nucleation and crystal growth.
Keywords:
Desloratadine / PVP / solid dispersion / spray coating / amorphous stateSource:
Drug Development and Industrial Pharmacy, 2013, 39, 7, 1020-1027Publisher:
- Taylor & Francis Ltd, Abingdon
Funding / projects:
- Ministry of Science and Technological Development, Republic of Serbia
DOI: 10.3109/03639045.2012.694890
ISSN: 0363-9045
PubMed: 22676511
WoS: 000319986900011
Scopus: 2-s2.0-84878833041
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PharmacyTY - JOUR AU - Kolasinac, Nemanja AU - Kachrimanis, Kyriakos AU - Đuriš, Jelena AU - Homšek, Irena AU - Grujić, Branka AU - Ibrić, Svetlana PY - 2013 UR - https://farfar.pharmacy.bg.ac.rs/handle/123456789/1989 AB - Solid dispersion systems have been widely used to enhance dissolution rate and oral bioavailability of poorly water-soluble drugs. However, the formulation process development and scale-up present a number of difficulties which has greatly limited their commercial applications. In this study, solid dispersions (SDs) of desloratadine (DSL) with povidone (PVP) and crospovidone (cPVP) were prepared by spray coating technique. The process involved the spray application of 96% ethanol solution of DSL and PVP/cPVP, and subsequent deposition of the coprecipitates onto microcrystalline cellulose pellets during drying by air flow in a mini spray coater. The results from the present study demonstrated that the spray coating process is efficient in preparing SDs with enhanced drug dissolution rate and it is highly efficient in organic solvent removal. Both PVP and cPVP greatly improved drug dissolution rate by SDs, with PVP showing better solubilization capability. Very fast drug dissolution rate is achieved from SDs containing PVP regardless of differences in K grade. SD with smaller particles of cPVP have higher drug dissolution rate in comparison to the cPVP with larger particles. Results from physical state characterization indicate that DSL in SDs exist in the amorphous (high free-energy) state which is probably stabilized by PVP/cPVP. After 6-month accelerated stability study, DSL remains amorphous, while PVP and cPVP act as anti-plasticizing agents, offering efficient steric hindrance for nucleation and crystal growth. PB - Taylor & Francis Ltd, Abingdon T2 - Drug Development and Industrial Pharmacy T1 - Spray coating as a powerful technique in preparation of solid dispersions with enhanced desloratadine dissolution rate VL - 39 IS - 7 SP - 1020 EP - 1027 DO - 10.3109/03639045.2012.694890 ER -
@article{ author = "Kolasinac, Nemanja and Kachrimanis, Kyriakos and Đuriš, Jelena and Homšek, Irena and Grujić, Branka and Ibrić, Svetlana", year = "2013", abstract = "Solid dispersion systems have been widely used to enhance dissolution rate and oral bioavailability of poorly water-soluble drugs. However, the formulation process development and scale-up present a number of difficulties which has greatly limited their commercial applications. In this study, solid dispersions (SDs) of desloratadine (DSL) with povidone (PVP) and crospovidone (cPVP) were prepared by spray coating technique. The process involved the spray application of 96% ethanol solution of DSL and PVP/cPVP, and subsequent deposition of the coprecipitates onto microcrystalline cellulose pellets during drying by air flow in a mini spray coater. The results from the present study demonstrated that the spray coating process is efficient in preparing SDs with enhanced drug dissolution rate and it is highly efficient in organic solvent removal. Both PVP and cPVP greatly improved drug dissolution rate by SDs, with PVP showing better solubilization capability. Very fast drug dissolution rate is achieved from SDs containing PVP regardless of differences in K grade. SD with smaller particles of cPVP have higher drug dissolution rate in comparison to the cPVP with larger particles. Results from physical state characterization indicate that DSL in SDs exist in the amorphous (high free-energy) state which is probably stabilized by PVP/cPVP. After 6-month accelerated stability study, DSL remains amorphous, while PVP and cPVP act as anti-plasticizing agents, offering efficient steric hindrance for nucleation and crystal growth.", publisher = "Taylor & Francis Ltd, Abingdon", journal = "Drug Development and Industrial Pharmacy", title = "Spray coating as a powerful technique in preparation of solid dispersions with enhanced desloratadine dissolution rate", volume = "39", number = "7", pages = "1020-1027", doi = "10.3109/03639045.2012.694890" }
Kolasinac, N., Kachrimanis, K., Đuriš, J., Homšek, I., Grujić, B.,& Ibrić, S.. (2013). Spray coating as a powerful technique in preparation of solid dispersions with enhanced desloratadine dissolution rate. in Drug Development and Industrial Pharmacy Taylor & Francis Ltd, Abingdon., 39(7), 1020-1027. https://doi.org/10.3109/03639045.2012.694890
Kolasinac N, Kachrimanis K, Đuriš J, Homšek I, Grujić B, Ibrić S. Spray coating as a powerful technique in preparation of solid dispersions with enhanced desloratadine dissolution rate. in Drug Development and Industrial Pharmacy. 2013;39(7):1020-1027. doi:10.3109/03639045.2012.694890 .
Kolasinac, Nemanja, Kachrimanis, Kyriakos, Đuriš, Jelena, Homšek, Irena, Grujić, Branka, Ibrić, Svetlana, "Spray coating as a powerful technique in preparation of solid dispersions with enhanced desloratadine dissolution rate" in Drug Development and Industrial Pharmacy, 39, no. 7 (2013):1020-1027, https://doi.org/10.3109/03639045.2012.694890 . .