TY  - 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 . .

TY  - JOUR
AU  - Kolasinac, Nemanja
AU  - Kachrimanis, Kyriakos
AU  - Homšek, Irena
AU  - Grujić, Branka
AU  - Đurić, Zorica
AU  - Ibrić, Svetlana
PY  - 2012
UR  - https://farfar.pharmacy.bg.ac.rs/handle/123456789/1640
AB  - The present study investigates the possibility of using poloxamers as solubility and dissolution rate enhancing agents of the poorly water soluble drug substance desloratadine that can be used for the preparation of immediate release tablet formulation. Two commercially available poloxamer grades (poloxamer P 188 and poloxamer P 407) were selected, and solid dispersions (SDs) containing different weight ratio of poloxamers and desloratadine were prepared by a low temperature melting method. All SDs were subjected to basic physicochemical characterization by thermal and vibrational spectroscopy methods in order to evaluate the efficiency of poloxamers as solubility enhancers. Immediate release tablets were prepared by direct compression of powdered solid dispersions according to a General Factorial Design, in order to evaluate the statistical significance of two formulation (X-1 - type of poloxamer in SD and X-2 - poloxamer ratio in SD) and one process variable (X-3 - compression force) on the drug dissolution rate. It was found that desloratadine in SDs existed in the amorphous state, and that can be largely responsible for the enhanced intrinsic solubility, which was more pronounced in SDs containing poloxamer 188. Statistical analysis of the factorial design revealed that both investigated formulation variables exert a significant effect on the drug dissolution rate. Increased poloxamer ratio in SDs resulted in increased drug dissolution rate, with poloxamer 188 contributing to a faster dissolution rate than poloxamer 407, in accordance with the results of intrinsic dissolution tests. Moreover, there is a significant interaction between poloxamer ratio in SD and compression force. Higher poloxamer ratio in SDs and higher compression force results in a significant decrease of the drug dissolution rate, which can be attributed to the lower porosity of the tablets and more pronounced bonding between poloxamer particles.
PB  - Elsevier Science BV, Amsterdam
T2  - International Journal of Pharmaceutics
T1  - Solubility enhancement of desloratadine by solid dispersion in poloxamers
VL  - 436
IS  - 1-2
SP  - 161
EP  - 170
DO  - 10.1016/j.ijpharm.2012.06.060
ER  - 

@article{
author = "Kolasinac, Nemanja and Kachrimanis, Kyriakos and Homšek, Irena and Grujić, Branka and Đurić, Zorica and Ibrić, Svetlana",
year = "2012",
abstract = "The present study investigates the possibility of using poloxamers as solubility and dissolution rate enhancing agents of the poorly water soluble drug substance desloratadine that can be used for the preparation of immediate release tablet formulation. Two commercially available poloxamer grades (poloxamer P 188 and poloxamer P 407) were selected, and solid dispersions (SDs) containing different weight ratio of poloxamers and desloratadine were prepared by a low temperature melting method. All SDs were subjected to basic physicochemical characterization by thermal and vibrational spectroscopy methods in order to evaluate the efficiency of poloxamers as solubility enhancers. Immediate release tablets were prepared by direct compression of powdered solid dispersions according to a General Factorial Design, in order to evaluate the statistical significance of two formulation (X-1 - type of poloxamer in SD and X-2 - poloxamer ratio in SD) and one process variable (X-3 - compression force) on the drug dissolution rate. It was found that desloratadine in SDs existed in the amorphous state, and that can be largely responsible for the enhanced intrinsic solubility, which was more pronounced in SDs containing poloxamer 188. Statistical analysis of the factorial design revealed that both investigated formulation variables exert a significant effect on the drug dissolution rate. Increased poloxamer ratio in SDs resulted in increased drug dissolution rate, with poloxamer 188 contributing to a faster dissolution rate than poloxamer 407, in accordance with the results of intrinsic dissolution tests. Moreover, there is a significant interaction between poloxamer ratio in SD and compression force. Higher poloxamer ratio in SDs and higher compression force results in a significant decrease of the drug dissolution rate, which can be attributed to the lower porosity of the tablets and more pronounced bonding between poloxamer particles.",
publisher = "Elsevier Science BV, Amsterdam",
journal = "International Journal of Pharmaceutics",
title = "Solubility enhancement of desloratadine by solid dispersion in poloxamers",
volume = "436",
number = "1-2",
pages = "161-170",
doi = "10.1016/j.ijpharm.2012.06.060"
}

Kolasinac, N., Kachrimanis, K., Homšek, I., Grujić, B., Đurić, Z.,& Ibrić, S.. (2012). Solubility enhancement of desloratadine by solid dispersion in poloxamers. in International Journal of Pharmaceutics
Elsevier Science BV, Amsterdam., 436(1-2), 161-170.
https://doi.org/10.1016/j.ijpharm.2012.06.060

Kolasinac N, Kachrimanis K, Homšek I, Grujić B, Đurić Z, Ibrić S. Solubility enhancement of desloratadine by solid dispersion in poloxamers. in International Journal of Pharmaceutics. 2012;436(1-2):161-170.
doi:10.1016/j.ijpharm.2012.06.060 .

Kolasinac, Nemanja, Kachrimanis, Kyriakos, Homšek, Irena, Grujić, Branka, Đurić, Zorica, Ibrić, Svetlana, "Solubility enhancement of desloratadine by solid dispersion in poloxamers" in International Journal of Pharmaceutics, 436, no. 1-2 (2012):161-170,
https://doi.org/10.1016/j.ijpharm.2012.06.060 . .