Binary, ternary and microencapsulated celecoxib complexes with β-cyclodextrin formulated via hydrophilic polymers
Abstract Cyclodextrins are cyclic oligosaccharides, capable of forming inclusion complexes with many active substances. This way, the aqueous solubility and rate of dissolution of active substances can be changed. For this research we have selected celecoxib as the model active substance, due to its...
Ausführliche Beschreibung
Gespeichert in:
| Autor*in: |
Vranić, Edina [verfasserIn] Grizić, Daris [verfasserIn] Planinšek, Odon [verfasserIn] Srčič, Stanko [verfasserIn] Bilensoy, Erem [verfasserIn] |
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| Format: |
E-Artikel |
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| Sprache: |
Englisch |
| Erschienen: |
2014 |
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| Schlagwörter: |
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| Übergeordnetes Werk: |
Enthalten in: Journal of inclusion phenomena and macrocyclic chemistry - Dordrecht [u.a.] : Springer Science + Business Media B.V, 1983, 80(2014), 1-2 vom: 20. Mai, Seite 139-146 |
|---|---|
| Übergeordnetes Werk: |
volume:80 ; year:2014 ; number:1-2 ; day:20 ; month:05 ; pages:139-146 |
| Links: |
|---|
| DOI / URN: |
10.1007/s10847-014-0421-7 |
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| Katalog-ID: |
SPR013722913 |
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| 520 | |a Abstract Cyclodextrins are cyclic oligosaccharides, capable of forming inclusion complexes with many active substances. This way, the aqueous solubility and rate of dissolution of active substances can be changed. For this research we have selected celecoxib as the model active substance, due to its low water solubility, high lipophilicity, and high intestinal permeability. Usually, the amount of cyclodextrin complex that can be incorporated into a pharmaceutical dosage form is limited. The usage of hydrophilic polymers can overcome this problem. In this study, we wanted to point out the potential of various types of hydrophilic polymers for enhancing the complex formation efficiencies, and to highlight the possible use of alginate as a solubility stabilizer/enhancer and as a microsphere matrix polymer. The phase solubility investigation showed greater stability constants (> 250 $ M^{−1} $) in ternary complexes than in the binary complex, which is a good indicator of the complex formation enhancer properties of these hydrophilic polymers. The relative solubilizing efficiency decreased in the next order: PVP K25 (6.49) > Sodium alginate (6.26) > PEG 6000 (5.72) > without polymer (4.81). The DSC curves showed that all samples that were prepared with β-cyclodextrin (both complexes and physical mixtures) had lower melting endotherms at 160 °C than pure celecoxib. XRD confirmed the complex formation by partial celecoxib amorphisation. The dissolution studies of the prepared microspheres revealed that all samples had different release rates (shown by the similarity factor $ f_{2} $, which was 36.37, 42.46 and 38.11 % respectively) and that the use of β-cyclodextrin increased the dissolution rate of celecoxib from alginate microspheres in a controlled manner. We concluded that sodium alginate could act as a complex stabilizing/enhancing agent and as a microsphere matrix polymer, at the same time. | ||
| 650 | 4 | |a Celecoxib |7 (dpeaa)DE-He213 | |
| 650 | 4 | |a β-cyclodextrin complex |7 (dpeaa)DE-He213 | |
| 650 | 4 | |a Complex formation efficiency |7 (dpeaa)DE-He213 | |
| 650 | 4 | |a Hydrophilic polymers |7 (dpeaa)DE-He213 | |
| 650 | 4 | |a Ternary complex formation |7 (dpeaa)DE-He213 | |
| 650 | 4 | |a Alginate microspheres |7 (dpeaa)DE-He213 | |
| 700 | 1 | |a Grizić, Daris |e verfasserin |4 aut | |
| 700 | 1 | |a Planinšek, Odon |e verfasserin |4 aut | |
| 700 | 1 | |a Srčič, Stanko |e verfasserin |4 aut | |
| 700 | 1 | |a Bilensoy, Erem |e verfasserin |4 aut | |
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10.1007/s10847-014-0421-7 doi (DE-627)SPR013722913 (SPR)s10847-014-0421-7-e DE-627 ger DE-627 rakwb eng 540 ASE 35.80 bkl 35.59 bkl Vranić, Edina verfasserin aut Binary, ternary and microencapsulated celecoxib complexes with β-cyclodextrin formulated via hydrophilic polymers 2014 Text txt rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier Abstract Cyclodextrins are cyclic oligosaccharides, capable of forming inclusion complexes with many active substances. This way, the aqueous solubility and rate of dissolution of active substances can be changed. For this research we have selected celecoxib as the model active substance, due to its low water solubility, high lipophilicity, and high intestinal permeability. Usually, the amount of cyclodextrin complex that can be incorporated into a pharmaceutical dosage form is limited. The usage of hydrophilic polymers can overcome this problem. In this study, we wanted to point out the potential of various types of hydrophilic polymers for enhancing the complex formation efficiencies, and to highlight the possible use of alginate as a solubility stabilizer/enhancer and as a microsphere matrix polymer. The phase solubility investigation showed greater stability constants (> 250 $ M^{−1} $) in ternary complexes than in the binary complex, which is a good indicator of the complex formation enhancer properties of these hydrophilic polymers. The relative solubilizing efficiency decreased in the next order: PVP K25 (6.49) > Sodium alginate (6.26) > PEG 6000 (5.72) > without polymer (4.81). The DSC curves showed that all samples that were prepared with β-cyclodextrin (both complexes and physical mixtures) had lower melting endotherms at 160 °C than pure celecoxib. XRD confirmed the complex formation by partial celecoxib amorphisation. The dissolution studies of the prepared microspheres revealed that all samples had different release rates (shown by the similarity factor $ f_{2} $, which was 36.37, 42.46 and 38.11 % respectively) and that the use of β-cyclodextrin increased the dissolution rate of celecoxib from alginate microspheres in a controlled manner. We concluded that sodium alginate could act as a complex stabilizing/enhancing agent and as a microsphere matrix polymer, at the same time. Celecoxib (dpeaa)DE-He213 β-cyclodextrin complex (dpeaa)DE-He213 Complex formation efficiency (dpeaa)DE-He213 Hydrophilic polymers (dpeaa)DE-He213 Ternary complex formation (dpeaa)DE-He213 Alginate microspheres (dpeaa)DE-He213 Grizić, Daris verfasserin aut Planinšek, Odon verfasserin aut Srčič, Stanko verfasserin aut Bilensoy, Erem verfasserin aut Enthalten in Journal of inclusion phenomena and macrocyclic chemistry Dordrecht [u.a.] : Springer Science + Business Media B.V, 1983 80(2014), 1-2 vom: 20. Mai, Seite 139-146 (DE-627)315293152 (DE-600)2016909-7 1573-1111 nnns volume:80 year:2014 number:1-2 day:20 month:05 pages:139-146 https://dx.doi.org/10.1007/s10847-014-0421-7 lizenzpflichtig Volltext GBV_USEFLAG_A SYSFLAG_A GBV_SPRINGER SSG-OLC-PHA GBV_ILN_11 GBV_ILN_20 GBV_ILN_22 GBV_ILN_23 GBV_ILN_24 GBV_ILN_31 GBV_ILN_32 GBV_ILN_39 GBV_ILN_40 GBV_ILN_60 GBV_ILN_62 GBV_ILN_63 GBV_ILN_69 GBV_ILN_70 GBV_ILN_73 GBV_ILN_74 GBV_ILN_90 GBV_ILN_95 GBV_ILN_100 GBV_ILN_101 GBV_ILN_105 GBV_ILN_110 GBV_ILN_120 GBV_ILN_138 GBV_ILN_150 GBV_ILN_151 GBV_ILN_152 GBV_ILN_161 GBV_ILN_170 GBV_ILN_171 GBV_ILN_187 GBV_ILN_213 GBV_ILN_224 GBV_ILN_230 GBV_ILN_250 GBV_ILN_281 GBV_ILN_285 GBV_ILN_293 GBV_ILN_370 GBV_ILN_602 GBV_ILN_636 GBV_ILN_702 GBV_ILN_2001 GBV_ILN_2003 GBV_ILN_2004 GBV_ILN_2005 GBV_ILN_2006 GBV_ILN_2007 GBV_ILN_2008 GBV_ILN_2009 GBV_ILN_2010 GBV_ILN_2011 GBV_ILN_2014 GBV_ILN_2015 GBV_ILN_2020 GBV_ILN_2021 GBV_ILN_2025 GBV_ILN_2026 GBV_ILN_2027 GBV_ILN_2031 GBV_ILN_2034 GBV_ILN_2037 GBV_ILN_2038 GBV_ILN_2039 GBV_ILN_2044 GBV_ILN_2048 GBV_ILN_2049 GBV_ILN_2050 GBV_ILN_2055 GBV_ILN_2057 GBV_ILN_2059 GBV_ILN_2061 GBV_ILN_2064 GBV_ILN_2065 GBV_ILN_2068 GBV_ILN_2070 GBV_ILN_2086 GBV_ILN_2088 GBV_ILN_2093 GBV_ILN_2106 GBV_ILN_2107 GBV_ILN_2108 GBV_ILN_2110 GBV_ILN_2111 GBV_ILN_2112 GBV_ILN_2113 GBV_ILN_2116 GBV_ILN_2118 GBV_ILN_2119 GBV_ILN_2122 GBV_ILN_2129 GBV_ILN_2143 GBV_ILN_2144 GBV_ILN_2147 GBV_ILN_2148 GBV_ILN_2152 GBV_ILN_2153 GBV_ILN_2188 GBV_ILN_2190 GBV_ILN_2232 GBV_ILN_2336 GBV_ILN_2446 GBV_ILN_2470 GBV_ILN_2472 GBV_ILN_2507 GBV_ILN_2522 GBV_ILN_2548 GBV_ILN_4012 GBV_ILN_4035 GBV_ILN_4037 GBV_ILN_4046 GBV_ILN_4112 GBV_ILN_4125 GBV_ILN_4126 GBV_ILN_4242 GBV_ILN_4246 GBV_ILN_4249 GBV_ILN_4251 GBV_ILN_4305 GBV_ILN_4306 GBV_ILN_4307 GBV_ILN_4313 GBV_ILN_4322 GBV_ILN_4323 GBV_ILN_4324 GBV_ILN_4325 GBV_ILN_4326 GBV_ILN_4333 GBV_ILN_4334 GBV_ILN_4335 GBV_ILN_4336 GBV_ILN_4338 GBV_ILN_4393 GBV_ILN_4700 35.80 ASE 35.59 ASE AR 80 2014 1-2 20 05 139-146 |
| spelling |
10.1007/s10847-014-0421-7 doi (DE-627)SPR013722913 (SPR)s10847-014-0421-7-e DE-627 ger DE-627 rakwb eng 540 ASE 35.80 bkl 35.59 bkl Vranić, Edina verfasserin aut Binary, ternary and microencapsulated celecoxib complexes with β-cyclodextrin formulated via hydrophilic polymers 2014 Text txt rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier Abstract Cyclodextrins are cyclic oligosaccharides, capable of forming inclusion complexes with many active substances. This way, the aqueous solubility and rate of dissolution of active substances can be changed. For this research we have selected celecoxib as the model active substance, due to its low water solubility, high lipophilicity, and high intestinal permeability. Usually, the amount of cyclodextrin complex that can be incorporated into a pharmaceutical dosage form is limited. The usage of hydrophilic polymers can overcome this problem. In this study, we wanted to point out the potential of various types of hydrophilic polymers for enhancing the complex formation efficiencies, and to highlight the possible use of alginate as a solubility stabilizer/enhancer and as a microsphere matrix polymer. The phase solubility investigation showed greater stability constants (> 250 $ M^{−1} $) in ternary complexes than in the binary complex, which is a good indicator of the complex formation enhancer properties of these hydrophilic polymers. The relative solubilizing efficiency decreased in the next order: PVP K25 (6.49) > Sodium alginate (6.26) > PEG 6000 (5.72) > without polymer (4.81). The DSC curves showed that all samples that were prepared with β-cyclodextrin (both complexes and physical mixtures) had lower melting endotherms at 160 °C than pure celecoxib. XRD confirmed the complex formation by partial celecoxib amorphisation. The dissolution studies of the prepared microspheres revealed that all samples had different release rates (shown by the similarity factor $ f_{2} $, which was 36.37, 42.46 and 38.11 % respectively) and that the use of β-cyclodextrin increased the dissolution rate of celecoxib from alginate microspheres in a controlled manner. We concluded that sodium alginate could act as a complex stabilizing/enhancing agent and as a microsphere matrix polymer, at the same time. Celecoxib (dpeaa)DE-He213 β-cyclodextrin complex (dpeaa)DE-He213 Complex formation efficiency (dpeaa)DE-He213 Hydrophilic polymers (dpeaa)DE-He213 Ternary complex formation (dpeaa)DE-He213 Alginate microspheres (dpeaa)DE-He213 Grizić, Daris verfasserin aut Planinšek, Odon verfasserin aut Srčič, Stanko verfasserin aut Bilensoy, Erem verfasserin aut Enthalten in Journal of inclusion phenomena and macrocyclic chemistry Dordrecht [u.a.] : Springer Science + Business Media B.V, 1983 80(2014), 1-2 vom: 20. Mai, Seite 139-146 (DE-627)315293152 (DE-600)2016909-7 1573-1111 nnns volume:80 year:2014 number:1-2 day:20 month:05 pages:139-146 https://dx.doi.org/10.1007/s10847-014-0421-7 lizenzpflichtig Volltext GBV_USEFLAG_A SYSFLAG_A GBV_SPRINGER SSG-OLC-PHA GBV_ILN_11 GBV_ILN_20 GBV_ILN_22 GBV_ILN_23 GBV_ILN_24 GBV_ILN_31 GBV_ILN_32 GBV_ILN_39 GBV_ILN_40 GBV_ILN_60 GBV_ILN_62 GBV_ILN_63 GBV_ILN_69 GBV_ILN_70 GBV_ILN_73 GBV_ILN_74 GBV_ILN_90 GBV_ILN_95 GBV_ILN_100 GBV_ILN_101 GBV_ILN_105 GBV_ILN_110 GBV_ILN_120 GBV_ILN_138 GBV_ILN_150 GBV_ILN_151 GBV_ILN_152 GBV_ILN_161 GBV_ILN_170 GBV_ILN_171 GBV_ILN_187 GBV_ILN_213 GBV_ILN_224 GBV_ILN_230 GBV_ILN_250 GBV_ILN_281 GBV_ILN_285 GBV_ILN_293 GBV_ILN_370 GBV_ILN_602 GBV_ILN_636 GBV_ILN_702 GBV_ILN_2001 GBV_ILN_2003 GBV_ILN_2004 GBV_ILN_2005 GBV_ILN_2006 GBV_ILN_2007 GBV_ILN_2008 GBV_ILN_2009 GBV_ILN_2010 GBV_ILN_2011 GBV_ILN_2014 GBV_ILN_2015 GBV_ILN_2020 GBV_ILN_2021 GBV_ILN_2025 GBV_ILN_2026 GBV_ILN_2027 GBV_ILN_2031 GBV_ILN_2034 GBV_ILN_2037 GBV_ILN_2038 GBV_ILN_2039 GBV_ILN_2044 GBV_ILN_2048 GBV_ILN_2049 GBV_ILN_2050 GBV_ILN_2055 GBV_ILN_2057 GBV_ILN_2059 GBV_ILN_2061 GBV_ILN_2064 GBV_ILN_2065 GBV_ILN_2068 GBV_ILN_2070 GBV_ILN_2086 GBV_ILN_2088 GBV_ILN_2093 GBV_ILN_2106 GBV_ILN_2107 GBV_ILN_2108 GBV_ILN_2110 GBV_ILN_2111 GBV_ILN_2112 GBV_ILN_2113 GBV_ILN_2116 GBV_ILN_2118 GBV_ILN_2119 GBV_ILN_2122 GBV_ILN_2129 GBV_ILN_2143 GBV_ILN_2144 GBV_ILN_2147 GBV_ILN_2148 GBV_ILN_2152 GBV_ILN_2153 GBV_ILN_2188 GBV_ILN_2190 GBV_ILN_2232 GBV_ILN_2336 GBV_ILN_2446 GBV_ILN_2470 GBV_ILN_2472 GBV_ILN_2507 GBV_ILN_2522 GBV_ILN_2548 GBV_ILN_4012 GBV_ILN_4035 GBV_ILN_4037 GBV_ILN_4046 GBV_ILN_4112 GBV_ILN_4125 GBV_ILN_4126 GBV_ILN_4242 GBV_ILN_4246 GBV_ILN_4249 GBV_ILN_4251 GBV_ILN_4305 GBV_ILN_4306 GBV_ILN_4307 GBV_ILN_4313 GBV_ILN_4322 GBV_ILN_4323 GBV_ILN_4324 GBV_ILN_4325 GBV_ILN_4326 GBV_ILN_4333 GBV_ILN_4334 GBV_ILN_4335 GBV_ILN_4336 GBV_ILN_4338 GBV_ILN_4393 GBV_ILN_4700 35.80 ASE 35.59 ASE AR 80 2014 1-2 20 05 139-146 |
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10.1007/s10847-014-0421-7 doi (DE-627)SPR013722913 (SPR)s10847-014-0421-7-e DE-627 ger DE-627 rakwb eng 540 ASE 35.80 bkl 35.59 bkl Vranić, Edina verfasserin aut Binary, ternary and microencapsulated celecoxib complexes with β-cyclodextrin formulated via hydrophilic polymers 2014 Text txt rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier Abstract Cyclodextrins are cyclic oligosaccharides, capable of forming inclusion complexes with many active substances. This way, the aqueous solubility and rate of dissolution of active substances can be changed. For this research we have selected celecoxib as the model active substance, due to its low water solubility, high lipophilicity, and high intestinal permeability. Usually, the amount of cyclodextrin complex that can be incorporated into a pharmaceutical dosage form is limited. The usage of hydrophilic polymers can overcome this problem. In this study, we wanted to point out the potential of various types of hydrophilic polymers for enhancing the complex formation efficiencies, and to highlight the possible use of alginate as a solubility stabilizer/enhancer and as a microsphere matrix polymer. The phase solubility investigation showed greater stability constants (> 250 $ M^{−1} $) in ternary complexes than in the binary complex, which is a good indicator of the complex formation enhancer properties of these hydrophilic polymers. The relative solubilizing efficiency decreased in the next order: PVP K25 (6.49) > Sodium alginate (6.26) > PEG 6000 (5.72) > without polymer (4.81). The DSC curves showed that all samples that were prepared with β-cyclodextrin (both complexes and physical mixtures) had lower melting endotherms at 160 °C than pure celecoxib. XRD confirmed the complex formation by partial celecoxib amorphisation. The dissolution studies of the prepared microspheres revealed that all samples had different release rates (shown by the similarity factor $ f_{2} $, which was 36.37, 42.46 and 38.11 % respectively) and that the use of β-cyclodextrin increased the dissolution rate of celecoxib from alginate microspheres in a controlled manner. We concluded that sodium alginate could act as a complex stabilizing/enhancing agent and as a microsphere matrix polymer, at the same time. Celecoxib (dpeaa)DE-He213 β-cyclodextrin complex (dpeaa)DE-He213 Complex formation efficiency (dpeaa)DE-He213 Hydrophilic polymers (dpeaa)DE-He213 Ternary complex formation (dpeaa)DE-He213 Alginate microspheres (dpeaa)DE-He213 Grizić, Daris verfasserin aut Planinšek, Odon verfasserin aut Srčič, Stanko verfasserin aut Bilensoy, Erem verfasserin aut Enthalten in Journal of inclusion phenomena and macrocyclic chemistry Dordrecht [u.a.] : Springer Science + Business Media B.V, 1983 80(2014), 1-2 vom: 20. Mai, Seite 139-146 (DE-627)315293152 (DE-600)2016909-7 1573-1111 nnns volume:80 year:2014 number:1-2 day:20 month:05 pages:139-146 https://dx.doi.org/10.1007/s10847-014-0421-7 lizenzpflichtig Volltext GBV_USEFLAG_A SYSFLAG_A GBV_SPRINGER SSG-OLC-PHA GBV_ILN_11 GBV_ILN_20 GBV_ILN_22 GBV_ILN_23 GBV_ILN_24 GBV_ILN_31 GBV_ILN_32 GBV_ILN_39 GBV_ILN_40 GBV_ILN_60 GBV_ILN_62 GBV_ILN_63 GBV_ILN_69 GBV_ILN_70 GBV_ILN_73 GBV_ILN_74 GBV_ILN_90 GBV_ILN_95 GBV_ILN_100 GBV_ILN_101 GBV_ILN_105 GBV_ILN_110 GBV_ILN_120 GBV_ILN_138 GBV_ILN_150 GBV_ILN_151 GBV_ILN_152 GBV_ILN_161 GBV_ILN_170 GBV_ILN_171 GBV_ILN_187 GBV_ILN_213 GBV_ILN_224 GBV_ILN_230 GBV_ILN_250 GBV_ILN_281 GBV_ILN_285 GBV_ILN_293 GBV_ILN_370 GBV_ILN_602 GBV_ILN_636 GBV_ILN_702 GBV_ILN_2001 GBV_ILN_2003 GBV_ILN_2004 GBV_ILN_2005 GBV_ILN_2006 GBV_ILN_2007 GBV_ILN_2008 GBV_ILN_2009 GBV_ILN_2010 GBV_ILN_2011 GBV_ILN_2014 GBV_ILN_2015 GBV_ILN_2020 GBV_ILN_2021 GBV_ILN_2025 GBV_ILN_2026 GBV_ILN_2027 GBV_ILN_2031 GBV_ILN_2034 GBV_ILN_2037 GBV_ILN_2038 GBV_ILN_2039 GBV_ILN_2044 GBV_ILN_2048 GBV_ILN_2049 GBV_ILN_2050 GBV_ILN_2055 GBV_ILN_2057 GBV_ILN_2059 GBV_ILN_2061 GBV_ILN_2064 GBV_ILN_2065 GBV_ILN_2068 GBV_ILN_2070 GBV_ILN_2086 GBV_ILN_2088 GBV_ILN_2093 GBV_ILN_2106 GBV_ILN_2107 GBV_ILN_2108 GBV_ILN_2110 GBV_ILN_2111 GBV_ILN_2112 GBV_ILN_2113 GBV_ILN_2116 GBV_ILN_2118 GBV_ILN_2119 GBV_ILN_2122 GBV_ILN_2129 GBV_ILN_2143 GBV_ILN_2144 GBV_ILN_2147 GBV_ILN_2148 GBV_ILN_2152 GBV_ILN_2153 GBV_ILN_2188 GBV_ILN_2190 GBV_ILN_2232 GBV_ILN_2336 GBV_ILN_2446 GBV_ILN_2470 GBV_ILN_2472 GBV_ILN_2507 GBV_ILN_2522 GBV_ILN_2548 GBV_ILN_4012 GBV_ILN_4035 GBV_ILN_4037 GBV_ILN_4046 GBV_ILN_4112 GBV_ILN_4125 GBV_ILN_4126 GBV_ILN_4242 GBV_ILN_4246 GBV_ILN_4249 GBV_ILN_4251 GBV_ILN_4305 GBV_ILN_4306 GBV_ILN_4307 GBV_ILN_4313 GBV_ILN_4322 GBV_ILN_4323 GBV_ILN_4324 GBV_ILN_4325 GBV_ILN_4326 GBV_ILN_4333 GBV_ILN_4334 GBV_ILN_4335 GBV_ILN_4336 GBV_ILN_4338 GBV_ILN_4393 GBV_ILN_4700 35.80 ASE 35.59 ASE AR 80 2014 1-2 20 05 139-146 |
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10.1007/s10847-014-0421-7 doi (DE-627)SPR013722913 (SPR)s10847-014-0421-7-e DE-627 ger DE-627 rakwb eng 540 ASE 35.80 bkl 35.59 bkl Vranić, Edina verfasserin aut Binary, ternary and microencapsulated celecoxib complexes with β-cyclodextrin formulated via hydrophilic polymers 2014 Text txt rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier Abstract Cyclodextrins are cyclic oligosaccharides, capable of forming inclusion complexes with many active substances. This way, the aqueous solubility and rate of dissolution of active substances can be changed. For this research we have selected celecoxib as the model active substance, due to its low water solubility, high lipophilicity, and high intestinal permeability. Usually, the amount of cyclodextrin complex that can be incorporated into a pharmaceutical dosage form is limited. The usage of hydrophilic polymers can overcome this problem. In this study, we wanted to point out the potential of various types of hydrophilic polymers for enhancing the complex formation efficiencies, and to highlight the possible use of alginate as a solubility stabilizer/enhancer and as a microsphere matrix polymer. The phase solubility investigation showed greater stability constants (> 250 $ M^{−1} $) in ternary complexes than in the binary complex, which is a good indicator of the complex formation enhancer properties of these hydrophilic polymers. The relative solubilizing efficiency decreased in the next order: PVP K25 (6.49) > Sodium alginate (6.26) > PEG 6000 (5.72) > without polymer (4.81). The DSC curves showed that all samples that were prepared with β-cyclodextrin (both complexes and physical mixtures) had lower melting endotherms at 160 °C than pure celecoxib. XRD confirmed the complex formation by partial celecoxib amorphisation. The dissolution studies of the prepared microspheres revealed that all samples had different release rates (shown by the similarity factor $ f_{2} $, which was 36.37, 42.46 and 38.11 % respectively) and that the use of β-cyclodextrin increased the dissolution rate of celecoxib from alginate microspheres in a controlled manner. We concluded that sodium alginate could act as a complex stabilizing/enhancing agent and as a microsphere matrix polymer, at the same time. Celecoxib (dpeaa)DE-He213 β-cyclodextrin complex (dpeaa)DE-He213 Complex formation efficiency (dpeaa)DE-He213 Hydrophilic polymers (dpeaa)DE-He213 Ternary complex formation (dpeaa)DE-He213 Alginate microspheres (dpeaa)DE-He213 Grizić, Daris verfasserin aut Planinšek, Odon verfasserin aut Srčič, Stanko verfasserin aut Bilensoy, Erem verfasserin aut Enthalten in Journal of inclusion phenomena and macrocyclic chemistry Dordrecht [u.a.] : Springer Science + Business Media B.V, 1983 80(2014), 1-2 vom: 20. Mai, Seite 139-146 (DE-627)315293152 (DE-600)2016909-7 1573-1111 nnns volume:80 year:2014 number:1-2 day:20 month:05 pages:139-146 https://dx.doi.org/10.1007/s10847-014-0421-7 lizenzpflichtig Volltext GBV_USEFLAG_A SYSFLAG_A GBV_SPRINGER SSG-OLC-PHA GBV_ILN_11 GBV_ILN_20 GBV_ILN_22 GBV_ILN_23 GBV_ILN_24 GBV_ILN_31 GBV_ILN_32 GBV_ILN_39 GBV_ILN_40 GBV_ILN_60 GBV_ILN_62 GBV_ILN_63 GBV_ILN_69 GBV_ILN_70 GBV_ILN_73 GBV_ILN_74 GBV_ILN_90 GBV_ILN_95 GBV_ILN_100 GBV_ILN_101 GBV_ILN_105 GBV_ILN_110 GBV_ILN_120 GBV_ILN_138 GBV_ILN_150 GBV_ILN_151 GBV_ILN_152 GBV_ILN_161 GBV_ILN_170 GBV_ILN_171 GBV_ILN_187 GBV_ILN_213 GBV_ILN_224 GBV_ILN_230 GBV_ILN_250 GBV_ILN_281 GBV_ILN_285 GBV_ILN_293 GBV_ILN_370 GBV_ILN_602 GBV_ILN_636 GBV_ILN_702 GBV_ILN_2001 GBV_ILN_2003 GBV_ILN_2004 GBV_ILN_2005 GBV_ILN_2006 GBV_ILN_2007 GBV_ILN_2008 GBV_ILN_2009 GBV_ILN_2010 GBV_ILN_2011 GBV_ILN_2014 GBV_ILN_2015 GBV_ILN_2020 GBV_ILN_2021 GBV_ILN_2025 GBV_ILN_2026 GBV_ILN_2027 GBV_ILN_2031 GBV_ILN_2034 GBV_ILN_2037 GBV_ILN_2038 GBV_ILN_2039 GBV_ILN_2044 GBV_ILN_2048 GBV_ILN_2049 GBV_ILN_2050 GBV_ILN_2055 GBV_ILN_2057 GBV_ILN_2059 GBV_ILN_2061 GBV_ILN_2064 GBV_ILN_2065 GBV_ILN_2068 GBV_ILN_2070 GBV_ILN_2086 GBV_ILN_2088 GBV_ILN_2093 GBV_ILN_2106 GBV_ILN_2107 GBV_ILN_2108 GBV_ILN_2110 GBV_ILN_2111 GBV_ILN_2112 GBV_ILN_2113 GBV_ILN_2116 GBV_ILN_2118 GBV_ILN_2119 GBV_ILN_2122 GBV_ILN_2129 GBV_ILN_2143 GBV_ILN_2144 GBV_ILN_2147 GBV_ILN_2148 GBV_ILN_2152 GBV_ILN_2153 GBV_ILN_2188 GBV_ILN_2190 GBV_ILN_2232 GBV_ILN_2336 GBV_ILN_2446 GBV_ILN_2470 GBV_ILN_2472 GBV_ILN_2507 GBV_ILN_2522 GBV_ILN_2548 GBV_ILN_4012 GBV_ILN_4035 GBV_ILN_4037 GBV_ILN_4046 GBV_ILN_4112 GBV_ILN_4125 GBV_ILN_4126 GBV_ILN_4242 GBV_ILN_4246 GBV_ILN_4249 GBV_ILN_4251 GBV_ILN_4305 GBV_ILN_4306 GBV_ILN_4307 GBV_ILN_4313 GBV_ILN_4322 GBV_ILN_4323 GBV_ILN_4324 GBV_ILN_4325 GBV_ILN_4326 GBV_ILN_4333 GBV_ILN_4334 GBV_ILN_4335 GBV_ILN_4336 GBV_ILN_4338 GBV_ILN_4393 GBV_ILN_4700 35.80 ASE 35.59 ASE AR 80 2014 1-2 20 05 139-146 |
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10.1007/s10847-014-0421-7 doi (DE-627)SPR013722913 (SPR)s10847-014-0421-7-e DE-627 ger DE-627 rakwb eng 540 ASE 35.80 bkl 35.59 bkl Vranić, Edina verfasserin aut Binary, ternary and microencapsulated celecoxib complexes with β-cyclodextrin formulated via hydrophilic polymers 2014 Text txt rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier Abstract Cyclodextrins are cyclic oligosaccharides, capable of forming inclusion complexes with many active substances. This way, the aqueous solubility and rate of dissolution of active substances can be changed. For this research we have selected celecoxib as the model active substance, due to its low water solubility, high lipophilicity, and high intestinal permeability. Usually, the amount of cyclodextrin complex that can be incorporated into a pharmaceutical dosage form is limited. The usage of hydrophilic polymers can overcome this problem. In this study, we wanted to point out the potential of various types of hydrophilic polymers for enhancing the complex formation efficiencies, and to highlight the possible use of alginate as a solubility stabilizer/enhancer and as a microsphere matrix polymer. The phase solubility investigation showed greater stability constants (> 250 $ M^{−1} $) in ternary complexes than in the binary complex, which is a good indicator of the complex formation enhancer properties of these hydrophilic polymers. The relative solubilizing efficiency decreased in the next order: PVP K25 (6.49) > Sodium alginate (6.26) > PEG 6000 (5.72) > without polymer (4.81). The DSC curves showed that all samples that were prepared with β-cyclodextrin (both complexes and physical mixtures) had lower melting endotherms at 160 °C than pure celecoxib. XRD confirmed the complex formation by partial celecoxib amorphisation. The dissolution studies of the prepared microspheres revealed that all samples had different release rates (shown by the similarity factor $ f_{2} $, which was 36.37, 42.46 and 38.11 % respectively) and that the use of β-cyclodextrin increased the dissolution rate of celecoxib from alginate microspheres in a controlled manner. We concluded that sodium alginate could act as a complex stabilizing/enhancing agent and as a microsphere matrix polymer, at the same time. Celecoxib (dpeaa)DE-He213 β-cyclodextrin complex (dpeaa)DE-He213 Complex formation efficiency (dpeaa)DE-He213 Hydrophilic polymers (dpeaa)DE-He213 Ternary complex formation (dpeaa)DE-He213 Alginate microspheres (dpeaa)DE-He213 Grizić, Daris verfasserin aut Planinšek, Odon verfasserin aut Srčič, Stanko verfasserin aut Bilensoy, Erem verfasserin aut Enthalten in Journal of inclusion phenomena and macrocyclic chemistry Dordrecht [u.a.] : Springer Science + Business Media B.V, 1983 80(2014), 1-2 vom: 20. Mai, Seite 139-146 (DE-627)315293152 (DE-600)2016909-7 1573-1111 nnns volume:80 year:2014 number:1-2 day:20 month:05 pages:139-146 https://dx.doi.org/10.1007/s10847-014-0421-7 lizenzpflichtig Volltext GBV_USEFLAG_A SYSFLAG_A GBV_SPRINGER SSG-OLC-PHA GBV_ILN_11 GBV_ILN_20 GBV_ILN_22 GBV_ILN_23 GBV_ILN_24 GBV_ILN_31 GBV_ILN_32 GBV_ILN_39 GBV_ILN_40 GBV_ILN_60 GBV_ILN_62 GBV_ILN_63 GBV_ILN_69 GBV_ILN_70 GBV_ILN_73 GBV_ILN_74 GBV_ILN_90 GBV_ILN_95 GBV_ILN_100 GBV_ILN_101 GBV_ILN_105 GBV_ILN_110 GBV_ILN_120 GBV_ILN_138 GBV_ILN_150 GBV_ILN_151 GBV_ILN_152 GBV_ILN_161 GBV_ILN_170 GBV_ILN_171 GBV_ILN_187 GBV_ILN_213 GBV_ILN_224 GBV_ILN_230 GBV_ILN_250 GBV_ILN_281 GBV_ILN_285 GBV_ILN_293 GBV_ILN_370 GBV_ILN_602 GBV_ILN_636 GBV_ILN_702 GBV_ILN_2001 GBV_ILN_2003 GBV_ILN_2004 GBV_ILN_2005 GBV_ILN_2006 GBV_ILN_2007 GBV_ILN_2008 GBV_ILN_2009 GBV_ILN_2010 GBV_ILN_2011 GBV_ILN_2014 GBV_ILN_2015 GBV_ILN_2020 GBV_ILN_2021 GBV_ILN_2025 GBV_ILN_2026 GBV_ILN_2027 GBV_ILN_2031 GBV_ILN_2034 GBV_ILN_2037 GBV_ILN_2038 GBV_ILN_2039 GBV_ILN_2044 GBV_ILN_2048 GBV_ILN_2049 GBV_ILN_2050 GBV_ILN_2055 GBV_ILN_2057 GBV_ILN_2059 GBV_ILN_2061 GBV_ILN_2064 GBV_ILN_2065 GBV_ILN_2068 GBV_ILN_2070 GBV_ILN_2086 GBV_ILN_2088 GBV_ILN_2093 GBV_ILN_2106 GBV_ILN_2107 GBV_ILN_2108 GBV_ILN_2110 GBV_ILN_2111 GBV_ILN_2112 GBV_ILN_2113 GBV_ILN_2116 GBV_ILN_2118 GBV_ILN_2119 GBV_ILN_2122 GBV_ILN_2129 GBV_ILN_2143 GBV_ILN_2144 GBV_ILN_2147 GBV_ILN_2148 GBV_ILN_2152 GBV_ILN_2153 GBV_ILN_2188 GBV_ILN_2190 GBV_ILN_2232 GBV_ILN_2336 GBV_ILN_2446 GBV_ILN_2470 GBV_ILN_2472 GBV_ILN_2507 GBV_ILN_2522 GBV_ILN_2548 GBV_ILN_4012 GBV_ILN_4035 GBV_ILN_4037 GBV_ILN_4046 GBV_ILN_4112 GBV_ILN_4125 GBV_ILN_4126 GBV_ILN_4242 GBV_ILN_4246 GBV_ILN_4249 GBV_ILN_4251 GBV_ILN_4305 GBV_ILN_4306 GBV_ILN_4307 GBV_ILN_4313 GBV_ILN_4322 GBV_ILN_4323 GBV_ILN_4324 GBV_ILN_4325 GBV_ILN_4326 GBV_ILN_4333 GBV_ILN_4334 GBV_ILN_4335 GBV_ILN_4336 GBV_ILN_4338 GBV_ILN_4393 GBV_ILN_4700 35.80 ASE 35.59 ASE AR 80 2014 1-2 20 05 139-146 |
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Enthalten in Journal of inclusion phenomena and macrocyclic chemistry 80(2014), 1-2 vom: 20. Mai, Seite 139-146 volume:80 year:2014 number:1-2 day:20 month:05 pages:139-146 |
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Enthalten in Journal of inclusion phenomena and macrocyclic chemistry 80(2014), 1-2 vom: 20. Mai, Seite 139-146 volume:80 year:2014 number:1-2 day:20 month:05 pages:139-146 |
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Celecoxib β-cyclodextrin complex Complex formation efficiency Hydrophilic polymers Ternary complex formation Alginate microspheres |
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Journal of inclusion phenomena and macrocyclic chemistry |
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Vranić, Edina @@aut@@ Grizić, Daris @@aut@@ Planinšek, Odon @@aut@@ Srčič, Stanko @@aut@@ Bilensoy, Erem @@aut@@ |
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<?xml version="1.0" encoding="UTF-8"?><collection xmlns="http://www.loc.gov/MARC21/slim"><record><leader>01000caa a22002652 4500</leader><controlfield tag="001">SPR013722913</controlfield><controlfield tag="003">DE-627</controlfield><controlfield tag="005">20230519072248.0</controlfield><controlfield tag="007">cr uuu---uuuuu</controlfield><controlfield tag="008">201006s2014 xx |||||o 00| ||eng c</controlfield><datafield tag="024" ind1="7" ind2=" "><subfield code="a">10.1007/s10847-014-0421-7</subfield><subfield code="2">doi</subfield></datafield><datafield tag="035" ind1=" " ind2=" "><subfield code="a">(DE-627)SPR013722913</subfield></datafield><datafield tag="035" ind1=" " ind2=" "><subfield code="a">(SPR)s10847-014-0421-7-e</subfield></datafield><datafield tag="040" ind1=" " ind2=" "><subfield code="a">DE-627</subfield><subfield code="b">ger</subfield><subfield code="c">DE-627</subfield><subfield code="e">rakwb</subfield></datafield><datafield tag="041" ind1=" " ind2=" "><subfield code="a">eng</subfield></datafield><datafield tag="082" ind1="0" ind2="4"><subfield code="a">540</subfield><subfield code="q">ASE</subfield></datafield><datafield tag="084" ind1=" " ind2=" "><subfield code="a">35.80</subfield><subfield code="2">bkl</subfield></datafield><datafield tag="084" ind1=" " ind2=" "><subfield code="a">35.59</subfield><subfield code="2">bkl</subfield></datafield><datafield tag="100" ind1="1" ind2=" "><subfield code="a">Vranić, Edina</subfield><subfield code="e">verfasserin</subfield><subfield code="4">aut</subfield></datafield><datafield tag="245" ind1="1" ind2="0"><subfield code="a">Binary, ternary and microencapsulated celecoxib complexes with β-cyclodextrin formulated via hydrophilic polymers</subfield></datafield><datafield tag="264" ind1=" " ind2="1"><subfield code="c">2014</subfield></datafield><datafield tag="336" ind1=" " ind2=" "><subfield code="a">Text</subfield><subfield code="b">txt</subfield><subfield code="2">rdacontent</subfield></datafield><datafield tag="337" ind1=" " ind2=" "><subfield code="a">Computermedien</subfield><subfield code="b">c</subfield><subfield code="2">rdamedia</subfield></datafield><datafield tag="338" ind1=" " ind2=" "><subfield code="a">Online-Ressource</subfield><subfield code="b">cr</subfield><subfield code="2">rdacarrier</subfield></datafield><datafield tag="520" ind1=" " ind2=" "><subfield code="a">Abstract Cyclodextrins are cyclic oligosaccharides, capable of forming inclusion complexes with many active substances. This way, the aqueous solubility and rate of dissolution of active substances can be changed. For this research we have selected celecoxib as the model active substance, due to its low water solubility, high lipophilicity, and high intestinal permeability. Usually, the amount of cyclodextrin complex that can be incorporated into a pharmaceutical dosage form is limited. The usage of hydrophilic polymers can overcome this problem. In this study, we wanted to point out the potential of various types of hydrophilic polymers for enhancing the complex formation efficiencies, and to highlight the possible use of alginate as a solubility stabilizer/enhancer and as a microsphere matrix polymer. The phase solubility investigation showed greater stability constants (> 250 $ M^{−1} $) in ternary complexes than in the binary complex, which is a good indicator of the complex formation enhancer properties of these hydrophilic polymers. The relative solubilizing efficiency decreased in the next order: PVP K25 (6.49) > Sodium alginate (6.26) > PEG 6000 (5.72) > without polymer (4.81). The DSC curves showed that all samples that were prepared with β-cyclodextrin (both complexes and physical mixtures) had lower melting endotherms at 160 °C than pure celecoxib. XRD confirmed the complex formation by partial celecoxib amorphisation. The dissolution studies of the prepared microspheres revealed that all samples had different release rates (shown by the similarity factor $ f_{2} $, which was 36.37, 42.46 and 38.11 % respectively) and that the use of β-cyclodextrin increased the dissolution rate of celecoxib from alginate microspheres in a controlled manner. 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Vranić, Edina |
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Vranić, Edina ddc 540 bkl 35.80 bkl 35.59 misc Celecoxib misc β-cyclodextrin complex misc Complex formation efficiency misc Hydrophilic polymers misc Ternary complex formation misc Alginate microspheres Binary, ternary and microencapsulated celecoxib complexes with β-cyclodextrin formulated via hydrophilic polymers |
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540 ASE 35.80 bkl 35.59 bkl Binary, ternary and microencapsulated celecoxib complexes with β-cyclodextrin formulated via hydrophilic polymers Celecoxib (dpeaa)DE-He213 β-cyclodextrin complex (dpeaa)DE-He213 Complex formation efficiency (dpeaa)DE-He213 Hydrophilic polymers (dpeaa)DE-He213 Ternary complex formation (dpeaa)DE-He213 Alginate microspheres (dpeaa)DE-He213 |
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ddc 540 bkl 35.80 bkl 35.59 misc Celecoxib misc β-cyclodextrin complex misc Complex formation efficiency misc Hydrophilic polymers misc Ternary complex formation misc Alginate microspheres |
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ddc 540 bkl 35.80 bkl 35.59 misc Celecoxib misc β-cyclodextrin complex misc Complex formation efficiency misc Hydrophilic polymers misc Ternary complex formation misc Alginate microspheres |
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ddc 540 bkl 35.80 bkl 35.59 misc Celecoxib misc β-cyclodextrin complex misc Complex formation efficiency misc Hydrophilic polymers misc Ternary complex formation misc Alginate microspheres |
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Binary, ternary and microencapsulated celecoxib complexes with β-cyclodextrin formulated via hydrophilic polymers |
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Binary, ternary and microencapsulated celecoxib complexes with β-cyclodextrin formulated via hydrophilic polymers |
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Vranić, Edina |
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Journal of inclusion phenomena and macrocyclic chemistry |
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Vranić, Edina Grizić, Daris Planinšek, Odon Srčič, Stanko Bilensoy, Erem |
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Vranić, Edina |
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binary, ternary and microencapsulated celecoxib complexes with β-cyclodextrin formulated via hydrophilic polymers |
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Binary, ternary and microencapsulated celecoxib complexes with β-cyclodextrin formulated via hydrophilic polymers |
| abstract |
Abstract Cyclodextrins are cyclic oligosaccharides, capable of forming inclusion complexes with many active substances. This way, the aqueous solubility and rate of dissolution of active substances can be changed. For this research we have selected celecoxib as the model active substance, due to its low water solubility, high lipophilicity, and high intestinal permeability. Usually, the amount of cyclodextrin complex that can be incorporated into a pharmaceutical dosage form is limited. The usage of hydrophilic polymers can overcome this problem. In this study, we wanted to point out the potential of various types of hydrophilic polymers for enhancing the complex formation efficiencies, and to highlight the possible use of alginate as a solubility stabilizer/enhancer and as a microsphere matrix polymer. The phase solubility investigation showed greater stability constants (> 250 $ M^{−1} $) in ternary complexes than in the binary complex, which is a good indicator of the complex formation enhancer properties of these hydrophilic polymers. The relative solubilizing efficiency decreased in the next order: PVP K25 (6.49) > Sodium alginate (6.26) > PEG 6000 (5.72) > without polymer (4.81). The DSC curves showed that all samples that were prepared with β-cyclodextrin (both complexes and physical mixtures) had lower melting endotherms at 160 °C than pure celecoxib. XRD confirmed the complex formation by partial celecoxib amorphisation. The dissolution studies of the prepared microspheres revealed that all samples had different release rates (shown by the similarity factor $ f_{2} $, which was 36.37, 42.46 and 38.11 % respectively) and that the use of β-cyclodextrin increased the dissolution rate of celecoxib from alginate microspheres in a controlled manner. We concluded that sodium alginate could act as a complex stabilizing/enhancing agent and as a microsphere matrix polymer, at the same time. |
| abstractGer |
Abstract Cyclodextrins are cyclic oligosaccharides, capable of forming inclusion complexes with many active substances. This way, the aqueous solubility and rate of dissolution of active substances can be changed. For this research we have selected celecoxib as the model active substance, due to its low water solubility, high lipophilicity, and high intestinal permeability. Usually, the amount of cyclodextrin complex that can be incorporated into a pharmaceutical dosage form is limited. The usage of hydrophilic polymers can overcome this problem. In this study, we wanted to point out the potential of various types of hydrophilic polymers for enhancing the complex formation efficiencies, and to highlight the possible use of alginate as a solubility stabilizer/enhancer and as a microsphere matrix polymer. The phase solubility investigation showed greater stability constants (> 250 $ M^{−1} $) in ternary complexes than in the binary complex, which is a good indicator of the complex formation enhancer properties of these hydrophilic polymers. The relative solubilizing efficiency decreased in the next order: PVP K25 (6.49) > Sodium alginate (6.26) > PEG 6000 (5.72) > without polymer (4.81). The DSC curves showed that all samples that were prepared with β-cyclodextrin (both complexes and physical mixtures) had lower melting endotherms at 160 °C than pure celecoxib. XRD confirmed the complex formation by partial celecoxib amorphisation. The dissolution studies of the prepared microspheres revealed that all samples had different release rates (shown by the similarity factor $ f_{2} $, which was 36.37, 42.46 and 38.11 % respectively) and that the use of β-cyclodextrin increased the dissolution rate of celecoxib from alginate microspheres in a controlled manner. We concluded that sodium alginate could act as a complex stabilizing/enhancing agent and as a microsphere matrix polymer, at the same time. |
| abstract_unstemmed |
Abstract Cyclodextrins are cyclic oligosaccharides, capable of forming inclusion complexes with many active substances. This way, the aqueous solubility and rate of dissolution of active substances can be changed. For this research we have selected celecoxib as the model active substance, due to its low water solubility, high lipophilicity, and high intestinal permeability. Usually, the amount of cyclodextrin complex that can be incorporated into a pharmaceutical dosage form is limited. The usage of hydrophilic polymers can overcome this problem. In this study, we wanted to point out the potential of various types of hydrophilic polymers for enhancing the complex formation efficiencies, and to highlight the possible use of alginate as a solubility stabilizer/enhancer and as a microsphere matrix polymer. The phase solubility investigation showed greater stability constants (> 250 $ M^{−1} $) in ternary complexes than in the binary complex, which is a good indicator of the complex formation enhancer properties of these hydrophilic polymers. The relative solubilizing efficiency decreased in the next order: PVP K25 (6.49) > Sodium alginate (6.26) > PEG 6000 (5.72) > without polymer (4.81). The DSC curves showed that all samples that were prepared with β-cyclodextrin (both complexes and physical mixtures) had lower melting endotherms at 160 °C than pure celecoxib. XRD confirmed the complex formation by partial celecoxib amorphisation. The dissolution studies of the prepared microspheres revealed that all samples had different release rates (shown by the similarity factor $ f_{2} $, which was 36.37, 42.46 and 38.11 % respectively) and that the use of β-cyclodextrin increased the dissolution rate of celecoxib from alginate microspheres in a controlled manner. We concluded that sodium alginate could act as a complex stabilizing/enhancing agent and as a microsphere matrix polymer, at the same time. |
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Binary, ternary and microencapsulated celecoxib complexes with β-cyclodextrin formulated via hydrophilic polymers |
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| score |
7.401513 |