Effects of polyvinylpyrrolidone both as a binder and pore-former on the release of sparingly water-soluble topiramate from ethylcellulose coated pellets
Abstract Delivering sparingly water-soluble drugs from ethylcellulose (EC) coated pellets with a controlled-release pattern remains challenging. In the present study, hydrophilic polyvinylpyrrolidone (PVP) was used both as a binder and a pore-former in EC coated pellets to deliver sparingly water-so...
Ausführliche Beschreibung
Autor*in: |
Yang, Meiyan [verfasserIn] |
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Englisch |
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2014transfer abstract |
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10 |
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Übergeordnetes Werk: |
Enthalten in: Description d’une cohorte française multicentrique de porteurs asymptomatiques d’anticorps anti-phospholipides - Nigolian, H. ELSEVIER, 2022, New York, NY [u.a.] |
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Übergeordnetes Werk: |
volume:465 ; year:2014 ; number:1 ; day:25 ; month:04 ; pages:187-196 ; extent:10 |
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DOI / URN: |
10.1016/j.ijpharm.2014.02.021 |
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ELV028133374 |
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245 | 1 | 0 | |a Effects of polyvinylpyrrolidone both as a binder and pore-former on the release of sparingly water-soluble topiramate from ethylcellulose coated pellets |
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520 | |a Abstract Delivering sparingly water-soluble drugs from ethylcellulose (EC) coated pellets with a controlled-release pattern remains challenging. In the present study, hydrophilic polyvinylpyrrolidone (PVP) was used both as a binder and a pore-former in EC coated pellets to deliver sparingly water-soluble topiramate, and the key factors that influenced drug release were identified. When the binder PVP content in drug layers below 20% w/w was decreased, the physical state of topiramate changed from amorphous to crystalline, making much difference to drug solubility and dissolution rates while modifying the drug release profile from first-order to zero-order. In addition, without PVP in drug layering solution, drug layered particles were less sticky during layering process, thus leading to a shorter process and higher loading efficiency. Furthermore, PVP level as a pore-former in EC coating layers mainly governed drug release from the coated pellets with the sensitivity ranging from 23% to 29%. PVP leaching rate and water permeability from EC/PVP film increased with the PVP level, which was perfectly correlated with drug release rate. Additionally, drug release from this formulation was independent of pH of release media or of the paddle mixing speed, but inversely proportional to the osmolality of release media above the physiological range. | ||
520 | |a Abstract Delivering sparingly water-soluble drugs from ethylcellulose (EC) coated pellets with a controlled-release pattern remains challenging. In the present study, hydrophilic polyvinylpyrrolidone (PVP) was used both as a binder and a pore-former in EC coated pellets to deliver sparingly water-soluble topiramate, and the key factors that influenced drug release were identified. When the binder PVP content in drug layers below 20% w/w was decreased, the physical state of topiramate changed from amorphous to crystalline, making much difference to drug solubility and dissolution rates while modifying the drug release profile from first-order to zero-order. In addition, without PVP in drug layering solution, drug layered particles were less sticky during layering process, thus leading to a shorter process and higher loading efficiency. Furthermore, PVP level as a pore-former in EC coating layers mainly governed drug release from the coated pellets with the sensitivity ranging from 23% to 29%. PVP leaching rate and water permeability from EC/PVP film increased with the PVP level, which was perfectly correlated with drug release rate. Additionally, drug release from this formulation was independent of pH of release media or of the paddle mixing speed, but inversely proportional to the osmolality of release media above the physiological range. | ||
650 | 7 | |a Topiramate |2 Elsevier | |
650 | 7 | |a Binder |2 Elsevier | |
650 | 7 | |a Pore-former |2 Elsevier | |
650 | 7 | |a Drug release mechanism |2 Elsevier | |
650 | 7 | |a PVP K30 |2 Elsevier | |
650 | 7 | |a Sparingly water-soluble drug |2 Elsevier | |
700 | 1 | |a Xie, Si |4 oth | |
700 | 1 | |a Li, Qiu |4 oth | |
700 | 1 | |a Wang, Yuli |4 oth | |
700 | 1 | |a Chang, Xinyi |4 oth | |
700 | 1 | |a Shan, Li |4 oth | |
700 | 1 | |a Sun, Lei |4 oth | |
700 | 1 | |a Huang, Xiaoli |4 oth | |
700 | 1 | |a Gao, Chunsheng |4 oth | |
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10.1016/j.ijpharm.2014.02.021 doi GBVA2014012000003.pica (DE-627)ELV028133374 (ELSEVIER)S0378-5173(14)00103-3 DE-627 ger DE-627 rakwb eng 610 610 DE-600 610 VZ 44.61 bkl Yang, Meiyan verfasserin aut Effects of polyvinylpyrrolidone both as a binder and pore-former on the release of sparingly water-soluble topiramate from ethylcellulose coated pellets 2014transfer abstract 10 nicht spezifiziert zzz rdacontent nicht spezifiziert z rdamedia nicht spezifiziert zu rdacarrier Abstract Delivering sparingly water-soluble drugs from ethylcellulose (EC) coated pellets with a controlled-release pattern remains challenging. In the present study, hydrophilic polyvinylpyrrolidone (PVP) was used both as a binder and a pore-former in EC coated pellets to deliver sparingly water-soluble topiramate, and the key factors that influenced drug release were identified. When the binder PVP content in drug layers below 20% w/w was decreased, the physical state of topiramate changed from amorphous to crystalline, making much difference to drug solubility and dissolution rates while modifying the drug release profile from first-order to zero-order. In addition, without PVP in drug layering solution, drug layered particles were less sticky during layering process, thus leading to a shorter process and higher loading efficiency. Furthermore, PVP level as a pore-former in EC coating layers mainly governed drug release from the coated pellets with the sensitivity ranging from 23% to 29%. PVP leaching rate and water permeability from EC/PVP film increased with the PVP level, which was perfectly correlated with drug release rate. Additionally, drug release from this formulation was independent of pH of release media or of the paddle mixing speed, but inversely proportional to the osmolality of release media above the physiological range. Abstract Delivering sparingly water-soluble drugs from ethylcellulose (EC) coated pellets with a controlled-release pattern remains challenging. In the present study, hydrophilic polyvinylpyrrolidone (PVP) was used both as a binder and a pore-former in EC coated pellets to deliver sparingly water-soluble topiramate, and the key factors that influenced drug release were identified. When the binder PVP content in drug layers below 20% w/w was decreased, the physical state of topiramate changed from amorphous to crystalline, making much difference to drug solubility and dissolution rates while modifying the drug release profile from first-order to zero-order. In addition, without PVP in drug layering solution, drug layered particles were less sticky during layering process, thus leading to a shorter process and higher loading efficiency. Furthermore, PVP level as a pore-former in EC coating layers mainly governed drug release from the coated pellets with the sensitivity ranging from 23% to 29%. PVP leaching rate and water permeability from EC/PVP film increased with the PVP level, which was perfectly correlated with drug release rate. Additionally, drug release from this formulation was independent of pH of release media or of the paddle mixing speed, but inversely proportional to the osmolality of release media above the physiological range. Topiramate Elsevier Binder Elsevier Pore-former Elsevier Drug release mechanism Elsevier PVP K30 Elsevier Sparingly water-soluble drug Elsevier Xie, Si oth Li, Qiu oth Wang, Yuli oth Chang, Xinyi oth Shan, Li oth Sun, Lei oth Huang, Xiaoli oth Gao, Chunsheng oth Enthalten in Elsevier Nigolian, H. ELSEVIER Description d’une cohorte française multicentrique de porteurs asymptomatiques d’anticorps anti-phospholipides 2022 New York, NY [u.a.] (DE-627)ELV008932840 volume:465 year:2014 number:1 day:25 month:04 pages:187-196 extent:10 https://doi.org/10.1016/j.ijpharm.2014.02.021 Volltext GBV_USEFLAG_U GBV_ELV SYSFLAG_U 44.61 Innere Medizin VZ AR 465 2014 1 25 0425 187-196 10 045F 610 |
spelling |
10.1016/j.ijpharm.2014.02.021 doi GBVA2014012000003.pica (DE-627)ELV028133374 (ELSEVIER)S0378-5173(14)00103-3 DE-627 ger DE-627 rakwb eng 610 610 DE-600 610 VZ 44.61 bkl Yang, Meiyan verfasserin aut Effects of polyvinylpyrrolidone both as a binder and pore-former on the release of sparingly water-soluble topiramate from ethylcellulose coated pellets 2014transfer abstract 10 nicht spezifiziert zzz rdacontent nicht spezifiziert z rdamedia nicht spezifiziert zu rdacarrier Abstract Delivering sparingly water-soluble drugs from ethylcellulose (EC) coated pellets with a controlled-release pattern remains challenging. In the present study, hydrophilic polyvinylpyrrolidone (PVP) was used both as a binder and a pore-former in EC coated pellets to deliver sparingly water-soluble topiramate, and the key factors that influenced drug release were identified. When the binder PVP content in drug layers below 20% w/w was decreased, the physical state of topiramate changed from amorphous to crystalline, making much difference to drug solubility and dissolution rates while modifying the drug release profile from first-order to zero-order. In addition, without PVP in drug layering solution, drug layered particles were less sticky during layering process, thus leading to a shorter process and higher loading efficiency. Furthermore, PVP level as a pore-former in EC coating layers mainly governed drug release from the coated pellets with the sensitivity ranging from 23% to 29%. PVP leaching rate and water permeability from EC/PVP film increased with the PVP level, which was perfectly correlated with drug release rate. Additionally, drug release from this formulation was independent of pH of release media or of the paddle mixing speed, but inversely proportional to the osmolality of release media above the physiological range. Abstract Delivering sparingly water-soluble drugs from ethylcellulose (EC) coated pellets with a controlled-release pattern remains challenging. In the present study, hydrophilic polyvinylpyrrolidone (PVP) was used both as a binder and a pore-former in EC coated pellets to deliver sparingly water-soluble topiramate, and the key factors that influenced drug release were identified. When the binder PVP content in drug layers below 20% w/w was decreased, the physical state of topiramate changed from amorphous to crystalline, making much difference to drug solubility and dissolution rates while modifying the drug release profile from first-order to zero-order. In addition, without PVP in drug layering solution, drug layered particles were less sticky during layering process, thus leading to a shorter process and higher loading efficiency. Furthermore, PVP level as a pore-former in EC coating layers mainly governed drug release from the coated pellets with the sensitivity ranging from 23% to 29%. PVP leaching rate and water permeability from EC/PVP film increased with the PVP level, which was perfectly correlated with drug release rate. Additionally, drug release from this formulation was independent of pH of release media or of the paddle mixing speed, but inversely proportional to the osmolality of release media above the physiological range. Topiramate Elsevier Binder Elsevier Pore-former Elsevier Drug release mechanism Elsevier PVP K30 Elsevier Sparingly water-soluble drug Elsevier Xie, Si oth Li, Qiu oth Wang, Yuli oth Chang, Xinyi oth Shan, Li oth Sun, Lei oth Huang, Xiaoli oth Gao, Chunsheng oth Enthalten in Elsevier Nigolian, H. ELSEVIER Description d’une cohorte française multicentrique de porteurs asymptomatiques d’anticorps anti-phospholipides 2022 New York, NY [u.a.] (DE-627)ELV008932840 volume:465 year:2014 number:1 day:25 month:04 pages:187-196 extent:10 https://doi.org/10.1016/j.ijpharm.2014.02.021 Volltext GBV_USEFLAG_U GBV_ELV SYSFLAG_U 44.61 Innere Medizin VZ AR 465 2014 1 25 0425 187-196 10 045F 610 |
allfields_unstemmed |
10.1016/j.ijpharm.2014.02.021 doi GBVA2014012000003.pica (DE-627)ELV028133374 (ELSEVIER)S0378-5173(14)00103-3 DE-627 ger DE-627 rakwb eng 610 610 DE-600 610 VZ 44.61 bkl Yang, Meiyan verfasserin aut Effects of polyvinylpyrrolidone both as a binder and pore-former on the release of sparingly water-soluble topiramate from ethylcellulose coated pellets 2014transfer abstract 10 nicht spezifiziert zzz rdacontent nicht spezifiziert z rdamedia nicht spezifiziert zu rdacarrier Abstract Delivering sparingly water-soluble drugs from ethylcellulose (EC) coated pellets with a controlled-release pattern remains challenging. In the present study, hydrophilic polyvinylpyrrolidone (PVP) was used both as a binder and a pore-former in EC coated pellets to deliver sparingly water-soluble topiramate, and the key factors that influenced drug release were identified. When the binder PVP content in drug layers below 20% w/w was decreased, the physical state of topiramate changed from amorphous to crystalline, making much difference to drug solubility and dissolution rates while modifying the drug release profile from first-order to zero-order. In addition, without PVP in drug layering solution, drug layered particles were less sticky during layering process, thus leading to a shorter process and higher loading efficiency. Furthermore, PVP level as a pore-former in EC coating layers mainly governed drug release from the coated pellets with the sensitivity ranging from 23% to 29%. PVP leaching rate and water permeability from EC/PVP film increased with the PVP level, which was perfectly correlated with drug release rate. Additionally, drug release from this formulation was independent of pH of release media or of the paddle mixing speed, but inversely proportional to the osmolality of release media above the physiological range. Abstract Delivering sparingly water-soluble drugs from ethylcellulose (EC) coated pellets with a controlled-release pattern remains challenging. In the present study, hydrophilic polyvinylpyrrolidone (PVP) was used both as a binder and a pore-former in EC coated pellets to deliver sparingly water-soluble topiramate, and the key factors that influenced drug release were identified. When the binder PVP content in drug layers below 20% w/w was decreased, the physical state of topiramate changed from amorphous to crystalline, making much difference to drug solubility and dissolution rates while modifying the drug release profile from first-order to zero-order. In addition, without PVP in drug layering solution, drug layered particles were less sticky during layering process, thus leading to a shorter process and higher loading efficiency. Furthermore, PVP level as a pore-former in EC coating layers mainly governed drug release from the coated pellets with the sensitivity ranging from 23% to 29%. PVP leaching rate and water permeability from EC/PVP film increased with the PVP level, which was perfectly correlated with drug release rate. Additionally, drug release from this formulation was independent of pH of release media or of the paddle mixing speed, but inversely proportional to the osmolality of release media above the physiological range. Topiramate Elsevier Binder Elsevier Pore-former Elsevier Drug release mechanism Elsevier PVP K30 Elsevier Sparingly water-soluble drug Elsevier Xie, Si oth Li, Qiu oth Wang, Yuli oth Chang, Xinyi oth Shan, Li oth Sun, Lei oth Huang, Xiaoli oth Gao, Chunsheng oth Enthalten in Elsevier Nigolian, H. ELSEVIER Description d’une cohorte française multicentrique de porteurs asymptomatiques d’anticorps anti-phospholipides 2022 New York, NY [u.a.] (DE-627)ELV008932840 volume:465 year:2014 number:1 day:25 month:04 pages:187-196 extent:10 https://doi.org/10.1016/j.ijpharm.2014.02.021 Volltext GBV_USEFLAG_U GBV_ELV SYSFLAG_U 44.61 Innere Medizin VZ AR 465 2014 1 25 0425 187-196 10 045F 610 |
allfieldsGer |
10.1016/j.ijpharm.2014.02.021 doi GBVA2014012000003.pica (DE-627)ELV028133374 (ELSEVIER)S0378-5173(14)00103-3 DE-627 ger DE-627 rakwb eng 610 610 DE-600 610 VZ 44.61 bkl Yang, Meiyan verfasserin aut Effects of polyvinylpyrrolidone both as a binder and pore-former on the release of sparingly water-soluble topiramate from ethylcellulose coated pellets 2014transfer abstract 10 nicht spezifiziert zzz rdacontent nicht spezifiziert z rdamedia nicht spezifiziert zu rdacarrier Abstract Delivering sparingly water-soluble drugs from ethylcellulose (EC) coated pellets with a controlled-release pattern remains challenging. In the present study, hydrophilic polyvinylpyrrolidone (PVP) was used both as a binder and a pore-former in EC coated pellets to deliver sparingly water-soluble topiramate, and the key factors that influenced drug release were identified. When the binder PVP content in drug layers below 20% w/w was decreased, the physical state of topiramate changed from amorphous to crystalline, making much difference to drug solubility and dissolution rates while modifying the drug release profile from first-order to zero-order. In addition, without PVP in drug layering solution, drug layered particles were less sticky during layering process, thus leading to a shorter process and higher loading efficiency. Furthermore, PVP level as a pore-former in EC coating layers mainly governed drug release from the coated pellets with the sensitivity ranging from 23% to 29%. PVP leaching rate and water permeability from EC/PVP film increased with the PVP level, which was perfectly correlated with drug release rate. Additionally, drug release from this formulation was independent of pH of release media or of the paddle mixing speed, but inversely proportional to the osmolality of release media above the physiological range. Abstract Delivering sparingly water-soluble drugs from ethylcellulose (EC) coated pellets with a controlled-release pattern remains challenging. In the present study, hydrophilic polyvinylpyrrolidone (PVP) was used both as a binder and a pore-former in EC coated pellets to deliver sparingly water-soluble topiramate, and the key factors that influenced drug release were identified. When the binder PVP content in drug layers below 20% w/w was decreased, the physical state of topiramate changed from amorphous to crystalline, making much difference to drug solubility and dissolution rates while modifying the drug release profile from first-order to zero-order. In addition, without PVP in drug layering solution, drug layered particles were less sticky during layering process, thus leading to a shorter process and higher loading efficiency. Furthermore, PVP level as a pore-former in EC coating layers mainly governed drug release from the coated pellets with the sensitivity ranging from 23% to 29%. PVP leaching rate and water permeability from EC/PVP film increased with the PVP level, which was perfectly correlated with drug release rate. Additionally, drug release from this formulation was independent of pH of release media or of the paddle mixing speed, but inversely proportional to the osmolality of release media above the physiological range. Topiramate Elsevier Binder Elsevier Pore-former Elsevier Drug release mechanism Elsevier PVP K30 Elsevier Sparingly water-soluble drug Elsevier Xie, Si oth Li, Qiu oth Wang, Yuli oth Chang, Xinyi oth Shan, Li oth Sun, Lei oth Huang, Xiaoli oth Gao, Chunsheng oth Enthalten in Elsevier Nigolian, H. ELSEVIER Description d’une cohorte française multicentrique de porteurs asymptomatiques d’anticorps anti-phospholipides 2022 New York, NY [u.a.] (DE-627)ELV008932840 volume:465 year:2014 number:1 day:25 month:04 pages:187-196 extent:10 https://doi.org/10.1016/j.ijpharm.2014.02.021 Volltext GBV_USEFLAG_U GBV_ELV SYSFLAG_U 44.61 Innere Medizin VZ AR 465 2014 1 25 0425 187-196 10 045F 610 |
allfieldsSound |
10.1016/j.ijpharm.2014.02.021 doi GBVA2014012000003.pica (DE-627)ELV028133374 (ELSEVIER)S0378-5173(14)00103-3 DE-627 ger DE-627 rakwb eng 610 610 DE-600 610 VZ 44.61 bkl Yang, Meiyan verfasserin aut Effects of polyvinylpyrrolidone both as a binder and pore-former on the release of sparingly water-soluble topiramate from ethylcellulose coated pellets 2014transfer abstract 10 nicht spezifiziert zzz rdacontent nicht spezifiziert z rdamedia nicht spezifiziert zu rdacarrier Abstract Delivering sparingly water-soluble drugs from ethylcellulose (EC) coated pellets with a controlled-release pattern remains challenging. In the present study, hydrophilic polyvinylpyrrolidone (PVP) was used both as a binder and a pore-former in EC coated pellets to deliver sparingly water-soluble topiramate, and the key factors that influenced drug release were identified. When the binder PVP content in drug layers below 20% w/w was decreased, the physical state of topiramate changed from amorphous to crystalline, making much difference to drug solubility and dissolution rates while modifying the drug release profile from first-order to zero-order. In addition, without PVP in drug layering solution, drug layered particles were less sticky during layering process, thus leading to a shorter process and higher loading efficiency. Furthermore, PVP level as a pore-former in EC coating layers mainly governed drug release from the coated pellets with the sensitivity ranging from 23% to 29%. PVP leaching rate and water permeability from EC/PVP film increased with the PVP level, which was perfectly correlated with drug release rate. Additionally, drug release from this formulation was independent of pH of release media or of the paddle mixing speed, but inversely proportional to the osmolality of release media above the physiological range. Abstract Delivering sparingly water-soluble drugs from ethylcellulose (EC) coated pellets with a controlled-release pattern remains challenging. In the present study, hydrophilic polyvinylpyrrolidone (PVP) was used both as a binder and a pore-former in EC coated pellets to deliver sparingly water-soluble topiramate, and the key factors that influenced drug release were identified. When the binder PVP content in drug layers below 20% w/w was decreased, the physical state of topiramate changed from amorphous to crystalline, making much difference to drug solubility and dissolution rates while modifying the drug release profile from first-order to zero-order. In addition, without PVP in drug layering solution, drug layered particles were less sticky during layering process, thus leading to a shorter process and higher loading efficiency. Furthermore, PVP level as a pore-former in EC coating layers mainly governed drug release from the coated pellets with the sensitivity ranging from 23% to 29%. PVP leaching rate and water permeability from EC/PVP film increased with the PVP level, which was perfectly correlated with drug release rate. Additionally, drug release from this formulation was independent of pH of release media or of the paddle mixing speed, but inversely proportional to the osmolality of release media above the physiological range. Topiramate Elsevier Binder Elsevier Pore-former Elsevier Drug release mechanism Elsevier PVP K30 Elsevier Sparingly water-soluble drug Elsevier Xie, Si oth Li, Qiu oth Wang, Yuli oth Chang, Xinyi oth Shan, Li oth Sun, Lei oth Huang, Xiaoli oth Gao, Chunsheng oth Enthalten in Elsevier Nigolian, H. ELSEVIER Description d’une cohorte française multicentrique de porteurs asymptomatiques d’anticorps anti-phospholipides 2022 New York, NY [u.a.] (DE-627)ELV008932840 volume:465 year:2014 number:1 day:25 month:04 pages:187-196 extent:10 https://doi.org/10.1016/j.ijpharm.2014.02.021 Volltext GBV_USEFLAG_U GBV_ELV SYSFLAG_U 44.61 Innere Medizin VZ AR 465 2014 1 25 0425 187-196 10 045F 610 |
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Enthalten in Description d’une cohorte française multicentrique de porteurs asymptomatiques d’anticorps anti-phospholipides New York, NY [u.a.] volume:465 year:2014 number:1 day:25 month:04 pages:187-196 extent:10 |
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effects of polyvinylpyrrolidone both as a binder and pore-former on the release of sparingly water-soluble topiramate from ethylcellulose coated pellets |
title_auth |
Effects of polyvinylpyrrolidone both as a binder and pore-former on the release of sparingly water-soluble topiramate from ethylcellulose coated pellets |
abstract |
Abstract Delivering sparingly water-soluble drugs from ethylcellulose (EC) coated pellets with a controlled-release pattern remains challenging. In the present study, hydrophilic polyvinylpyrrolidone (PVP) was used both as a binder and a pore-former in EC coated pellets to deliver sparingly water-soluble topiramate, and the key factors that influenced drug release were identified. When the binder PVP content in drug layers below 20% w/w was decreased, the physical state of topiramate changed from amorphous to crystalline, making much difference to drug solubility and dissolution rates while modifying the drug release profile from first-order to zero-order. In addition, without PVP in drug layering solution, drug layered particles were less sticky during layering process, thus leading to a shorter process and higher loading efficiency. Furthermore, PVP level as a pore-former in EC coating layers mainly governed drug release from the coated pellets with the sensitivity ranging from 23% to 29%. PVP leaching rate and water permeability from EC/PVP film increased with the PVP level, which was perfectly correlated with drug release rate. Additionally, drug release from this formulation was independent of pH of release media or of the paddle mixing speed, but inversely proportional to the osmolality of release media above the physiological range. |
abstractGer |
Abstract Delivering sparingly water-soluble drugs from ethylcellulose (EC) coated pellets with a controlled-release pattern remains challenging. In the present study, hydrophilic polyvinylpyrrolidone (PVP) was used both as a binder and a pore-former in EC coated pellets to deliver sparingly water-soluble topiramate, and the key factors that influenced drug release were identified. When the binder PVP content in drug layers below 20% w/w was decreased, the physical state of topiramate changed from amorphous to crystalline, making much difference to drug solubility and dissolution rates while modifying the drug release profile from first-order to zero-order. In addition, without PVP in drug layering solution, drug layered particles were less sticky during layering process, thus leading to a shorter process and higher loading efficiency. Furthermore, PVP level as a pore-former in EC coating layers mainly governed drug release from the coated pellets with the sensitivity ranging from 23% to 29%. PVP leaching rate and water permeability from EC/PVP film increased with the PVP level, which was perfectly correlated with drug release rate. Additionally, drug release from this formulation was independent of pH of release media or of the paddle mixing speed, but inversely proportional to the osmolality of release media above the physiological range. |
abstract_unstemmed |
Abstract Delivering sparingly water-soluble drugs from ethylcellulose (EC) coated pellets with a controlled-release pattern remains challenging. In the present study, hydrophilic polyvinylpyrrolidone (PVP) was used both as a binder and a pore-former in EC coated pellets to deliver sparingly water-soluble topiramate, and the key factors that influenced drug release were identified. When the binder PVP content in drug layers below 20% w/w was decreased, the physical state of topiramate changed from amorphous to crystalline, making much difference to drug solubility and dissolution rates while modifying the drug release profile from first-order to zero-order. In addition, without PVP in drug layering solution, drug layered particles were less sticky during layering process, thus leading to a shorter process and higher loading efficiency. Furthermore, PVP level as a pore-former in EC coating layers mainly governed drug release from the coated pellets with the sensitivity ranging from 23% to 29%. PVP leaching rate and water permeability from EC/PVP film increased with the PVP level, which was perfectly correlated with drug release rate. Additionally, drug release from this formulation was independent of pH of release media or of the paddle mixing speed, but inversely proportional to the osmolality of release media above the physiological range. |
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Effects of polyvinylpyrrolidone both as a binder and pore-former on the release of sparingly water-soluble topiramate from ethylcellulose coated pellets |
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