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Toshikiro Kimura - One of the best experts on this subject based on the ideXlab platform.
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development of novel sustained release system disintegration controlled Matrix Tablet dcmt with solid dispersion granules of nilvadipine ii in vivo evaluation
Journal of Controlled Release, 2006Co-Authors: Nobuyuki Tanaka, Keiji Imai, Kazuto Okimoto, Satoshi Ueda, Yuji Tokunaga, Rinta Ibuki, Kazutaka Higaki, Toshikiro KimuraAbstract:A novel sustained-release (SR) system, disintegration-controlled Matrix Tablet (DCMT), was developed for poorly water-soluble drugs. DCMT, consisting of wax and solid dispersion (SD) granules containing a disintegrant, could control the release of nilvadipine (NiD), a model compound, by its disintegration. In the present study, two DCMTs (DCMT-1 and DCMT-2) with different release rates of NiD were orally administered to beagle dogs, and in vivo absorption of NiD from DCMTs was compared with that from immediate-release (IR) Tablets. DCMTs successfully sustained the absorption of NiD longer than IR Tablets, while they did not decrease the bioavailability of NiD. DCMT-2, providing the slower release of NiD than DCMT-1, prolonged the absorption longer than DCMT-1. In vivo absorption profiles of NiD from DCMTs were significantly correlated with in vitro release profiles, suggesting that the release property from DCMTs would maintain regardless of the change in physiological condition through the gastrointestinal tract. Furthermore, the food intake did not affect the absorption of NiD after oral administration of DCMT-2. The present results strongly indicate that the DCMT system would be a promising SR system, which could improve the solubility and sustain the absorption of poorly water-soluble drugs.
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development of novel sustained release system disintegration controlled Matrix Tablet dcmt with solid dispersion granules of nilvadipine
Journal of Controlled Release, 2005Co-Authors: Nobuyuki Tanaka, Keiji Imai, Kazuto Okimoto, Satoshi Ueda, Yuji Tokunaga, Atsuo Ohike, Rinta Ibuki, Kazutaka Higaki, Toshikiro KimuraAbstract:Abstract The goal of this study is to develop a novel sustained-release (SR) system for poorly water-soluble drugs by applying solid dispersion (SD) technique for improving the solubility. The developed SR system, disintegration-controlled Matrix Tablet (DCMT), consists of hydrogenated soybean oil (HSO) as wax and SD granules containing low-substituted hydroxypropylcellulose (L-HPC) as a disintegrant. In this study, nilvadipine (NiD) was chosen as a model compound. Sustained-release profiles of NiD from DCMT were identically controlled in several dissolution mediums in spite of varying pH and agitation speed. The release of NiD from DCMT was sustained more effectively by increasing the amount of wax or by decreasing the amount of disintegrant, and supersaturation of NiD was achieved without any re-crystallization in dissolution medium. The release rate of NiD from DCMT was controlled by the disintegration rate of Tablet. The release profile of NiD was described by the Hixson–Crowell's model better than zero-order kinetics, first-order kinetics and Higuchi's model, which supports that the release of NiD from DCMT is regulated by the disintegration of the Tablet. From this study, it was clarified that DCMT was one of the promising SR systems applying SD for the poorly water-soluble drugs.
Nobuyuki Tanaka - One of the best experts on this subject based on the ideXlab platform.
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development of novel sustained release system disintegration controlled Matrix Tablet dcmt with solid dispersion granules of nilvadipine ii in vivo evaluation
Journal of Controlled Release, 2006Co-Authors: Nobuyuki Tanaka, Keiji Imai, Kazuto Okimoto, Satoshi Ueda, Yuji Tokunaga, Rinta Ibuki, Kazutaka Higaki, Toshikiro KimuraAbstract:A novel sustained-release (SR) system, disintegration-controlled Matrix Tablet (DCMT), was developed for poorly water-soluble drugs. DCMT, consisting of wax and solid dispersion (SD) granules containing a disintegrant, could control the release of nilvadipine (NiD), a model compound, by its disintegration. In the present study, two DCMTs (DCMT-1 and DCMT-2) with different release rates of NiD were orally administered to beagle dogs, and in vivo absorption of NiD from DCMTs was compared with that from immediate-release (IR) Tablets. DCMTs successfully sustained the absorption of NiD longer than IR Tablets, while they did not decrease the bioavailability of NiD. DCMT-2, providing the slower release of NiD than DCMT-1, prolonged the absorption longer than DCMT-1. In vivo absorption profiles of NiD from DCMTs were significantly correlated with in vitro release profiles, suggesting that the release property from DCMTs would maintain regardless of the change in physiological condition through the gastrointestinal tract. Furthermore, the food intake did not affect the absorption of NiD after oral administration of DCMT-2. The present results strongly indicate that the DCMT system would be a promising SR system, which could improve the solubility and sustain the absorption of poorly water-soluble drugs.
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development of novel sustained release system disintegration controlled Matrix Tablet dcmt with solid dispersion granules of nilvadipine
Journal of Controlled Release, 2005Co-Authors: Nobuyuki Tanaka, Keiji Imai, Kazuto Okimoto, Satoshi Ueda, Yuji Tokunaga, Atsuo Ohike, Rinta Ibuki, Kazutaka Higaki, Toshikiro KimuraAbstract:Abstract The goal of this study is to develop a novel sustained-release (SR) system for poorly water-soluble drugs by applying solid dispersion (SD) technique for improving the solubility. The developed SR system, disintegration-controlled Matrix Tablet (DCMT), consists of hydrogenated soybean oil (HSO) as wax and SD granules containing low-substituted hydroxypropylcellulose (L-HPC) as a disintegrant. In this study, nilvadipine (NiD) was chosen as a model compound. Sustained-release profiles of NiD from DCMT were identically controlled in several dissolution mediums in spite of varying pH and agitation speed. The release of NiD from DCMT was sustained more effectively by increasing the amount of wax or by decreasing the amount of disintegrant, and supersaturation of NiD was achieved without any re-crystallization in dissolution medium. The release rate of NiD from DCMT was controlled by the disintegration rate of Tablet. The release profile of NiD was described by the Hixson–Crowell's model better than zero-order kinetics, first-order kinetics and Higuchi's model, which supports that the release of NiD from DCMT is regulated by the disintegration of the Tablet. From this study, it was clarified that DCMT was one of the promising SR systems applying SD for the poorly water-soluble drugs.
V Satyanarayana - One of the best experts on this subject based on the ideXlab platform.
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a three layer guar gum Matrix Tablet for oral controlled delivery of highly soluble metoprolol tartrate
International Journal of Pharmaceutics, 2002Co-Authors: Y S R Krishnaiah, R S Karthikeyan, V SatyanarayanaAbstract:Abstract The objective of the study is to design oral controlled drug delivery systems for highly water-soluble drugs using guar gum as a carrier in the form of a three-layer Matrix Tablet. Metoprolol tartrate was chosen as a model drug because of its high water solubility. Matrix Tablets containing either 30 (M1), 40 (M2) or 50% (M3) of guar gum were prepared by wet granulation technique using starch paste as a binder. Three-layer Matrix Tablets of metoprolol tartrate were prepared by compressing on both sides of guar gum Matrix Tablet granules of metoprolol tartrate M1, M2 or M3 with either 50 (TL1M1, TL1M2 or TL1M3) or 75 mg (TL2M1, TL2M2 or TL2M3) of guar gum granules as release retardant layers. Both the Matrix and three-layer Matrix Tablets were evaluated for hardness, thickness, drug content uniformity, and subjected to in vitro drug release studies. The amount of metoprolol tartrate released from the Matrix and three-layer Matrix Tablets at different time intervals was estimated by using a HPLC method. Matrix Tablets of metoprolol tartrate were unable to provide the required drug release rate. However, the three-layer guar gum Matrix Tablets (TL2M3) provided the required release rate on par with the theoretical release rate for metoprolol tartrate formulations meant for twice daily administration. The three-layer guar gum Matrix Tablet (TL2M3) showed no change either in physical appearance, drug content or in dissolution pattern after storage at 40 °C/75% RH for 6 months. The FT-IR study did not show any possibility of metoprolol tartrate/guar gum interaction with the formulation excipients used in the study. The results indicated that guar gum, in the form of three-layer Matrix Tablets, is a potential carrier in the design of oral controlled drug delivery systems for highly water-soluble drugs such as metoprolol tartrate.
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three layer guar gum Matrix Tablet formulations for oral controlled delivery of highly soluble trimetazidine dihydrochloride
Journal of Controlled Release, 2002Co-Authors: Y S R Krishnaiah, R S Karthikeyan, Gouri V Sankar, V SatyanarayanaAbstract:Abstract The present study is carried out to design oral controlled drug delivery systems for highly water-soluble drugs using guar gum as a carrier in the form of three-layer Matrix Tablets. Trimetazidine dihydrochloride was chosen as a model drug because of its high water solubility. Matrix Tablet granules containing 30% (M1), 40% (M2) or 50% (M3) of guar gum were prepared by the wet granulation technique using starch paste as a binder. Three-layer Matrix Tablets of trimetazidine dihydrochloride were prepared by compressing on either side of guar gum Matrix Tablet granules of trimetazidine dihydrochloride M1, M2 or M3 with 200 mg of guar gum granules containing either 65% of guar gum (T1M1, T1M2 or T1M3), 75% of guar gum (T2M1, T2M2 or T2M3) or 85% of guar gum (T3M1, T3M2 or T3M3) as release retardant layers. The three-layer Matrix Tablets were evaluated for hardness, thickness, drug content uniformity, and were subjected to in vitro drug release studies. The amount of trimetazidine dihydrochloride released from the Matrix and three-layer Matrix Tablets at different time intervals was estimated using a HPLC method. The three-layer guar gum Matrix Tablet (T3M3) provided the required release rate on par with the theoretical release rate for guar gum formulations meant for twice daily administration. The three-layer guar gum Matrix Tablet (T3M3) showed no change either in physical appearance, drug content or in dissolution pattern after storage at 40 °C/RH 75% for 6 months. The DSC study did not show any possibility of interaction between trimetazidine dihydrochloride and guar gum/other formulation excipients used in the study. The results indicated that guar gum, in the form of three-layer Matrix Tablets, is a potential carrier in the design of oral controlled drug delivery systems for highly water-soluble drugs such as trimetazidine dihydrochloride.
Satoshi Ueda - One of the best experts on this subject based on the ideXlab platform.
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development of novel sustained release system disintegration controlled Matrix Tablet dcmt with solid dispersion granules of nilvadipine ii in vivo evaluation
Journal of Controlled Release, 2006Co-Authors: Nobuyuki Tanaka, Keiji Imai, Kazuto Okimoto, Satoshi Ueda, Yuji Tokunaga, Rinta Ibuki, Kazutaka Higaki, Toshikiro KimuraAbstract:A novel sustained-release (SR) system, disintegration-controlled Matrix Tablet (DCMT), was developed for poorly water-soluble drugs. DCMT, consisting of wax and solid dispersion (SD) granules containing a disintegrant, could control the release of nilvadipine (NiD), a model compound, by its disintegration. In the present study, two DCMTs (DCMT-1 and DCMT-2) with different release rates of NiD were orally administered to beagle dogs, and in vivo absorption of NiD from DCMTs was compared with that from immediate-release (IR) Tablets. DCMTs successfully sustained the absorption of NiD longer than IR Tablets, while they did not decrease the bioavailability of NiD. DCMT-2, providing the slower release of NiD than DCMT-1, prolonged the absorption longer than DCMT-1. In vivo absorption profiles of NiD from DCMTs were significantly correlated with in vitro release profiles, suggesting that the release property from DCMTs would maintain regardless of the change in physiological condition through the gastrointestinal tract. Furthermore, the food intake did not affect the absorption of NiD after oral administration of DCMT-2. The present results strongly indicate that the DCMT system would be a promising SR system, which could improve the solubility and sustain the absorption of poorly water-soluble drugs.
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development of novel sustained release system disintegration controlled Matrix Tablet dcmt with solid dispersion granules of nilvadipine
Journal of Controlled Release, 2005Co-Authors: Nobuyuki Tanaka, Keiji Imai, Kazuto Okimoto, Satoshi Ueda, Yuji Tokunaga, Atsuo Ohike, Rinta Ibuki, Kazutaka Higaki, Toshikiro KimuraAbstract:Abstract The goal of this study is to develop a novel sustained-release (SR) system for poorly water-soluble drugs by applying solid dispersion (SD) technique for improving the solubility. The developed SR system, disintegration-controlled Matrix Tablet (DCMT), consists of hydrogenated soybean oil (HSO) as wax and SD granules containing low-substituted hydroxypropylcellulose (L-HPC) as a disintegrant. In this study, nilvadipine (NiD) was chosen as a model compound. Sustained-release profiles of NiD from DCMT were identically controlled in several dissolution mediums in spite of varying pH and agitation speed. The release of NiD from DCMT was sustained more effectively by increasing the amount of wax or by decreasing the amount of disintegrant, and supersaturation of NiD was achieved without any re-crystallization in dissolution medium. The release rate of NiD from DCMT was controlled by the disintegration rate of Tablet. The release profile of NiD was described by the Hixson–Crowell's model better than zero-order kinetics, first-order kinetics and Higuchi's model, which supports that the release of NiD from DCMT is regulated by the disintegration of the Tablet. From this study, it was clarified that DCMT was one of the promising SR systems applying SD for the poorly water-soluble drugs.
Rinta Ibuki - One of the best experts on this subject based on the ideXlab platform.
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development of novel sustained release system disintegration controlled Matrix Tablet dcmt with solid dispersion granules of nilvadipine ii in vivo evaluation
Journal of Controlled Release, 2006Co-Authors: Nobuyuki Tanaka, Keiji Imai, Kazuto Okimoto, Satoshi Ueda, Yuji Tokunaga, Rinta Ibuki, Kazutaka Higaki, Toshikiro KimuraAbstract:A novel sustained-release (SR) system, disintegration-controlled Matrix Tablet (DCMT), was developed for poorly water-soluble drugs. DCMT, consisting of wax and solid dispersion (SD) granules containing a disintegrant, could control the release of nilvadipine (NiD), a model compound, by its disintegration. In the present study, two DCMTs (DCMT-1 and DCMT-2) with different release rates of NiD were orally administered to beagle dogs, and in vivo absorption of NiD from DCMTs was compared with that from immediate-release (IR) Tablets. DCMTs successfully sustained the absorption of NiD longer than IR Tablets, while they did not decrease the bioavailability of NiD. DCMT-2, providing the slower release of NiD than DCMT-1, prolonged the absorption longer than DCMT-1. In vivo absorption profiles of NiD from DCMTs were significantly correlated with in vitro release profiles, suggesting that the release property from DCMTs would maintain regardless of the change in physiological condition through the gastrointestinal tract. Furthermore, the food intake did not affect the absorption of NiD after oral administration of DCMT-2. The present results strongly indicate that the DCMT system would be a promising SR system, which could improve the solubility and sustain the absorption of poorly water-soluble drugs.
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development of novel sustained release system disintegration controlled Matrix Tablet dcmt with solid dispersion granules of nilvadipine
Journal of Controlled Release, 2005Co-Authors: Nobuyuki Tanaka, Keiji Imai, Kazuto Okimoto, Satoshi Ueda, Yuji Tokunaga, Atsuo Ohike, Rinta Ibuki, Kazutaka Higaki, Toshikiro KimuraAbstract:Abstract The goal of this study is to develop a novel sustained-release (SR) system for poorly water-soluble drugs by applying solid dispersion (SD) technique for improving the solubility. The developed SR system, disintegration-controlled Matrix Tablet (DCMT), consists of hydrogenated soybean oil (HSO) as wax and SD granules containing low-substituted hydroxypropylcellulose (L-HPC) as a disintegrant. In this study, nilvadipine (NiD) was chosen as a model compound. Sustained-release profiles of NiD from DCMT were identically controlled in several dissolution mediums in spite of varying pH and agitation speed. The release of NiD from DCMT was sustained more effectively by increasing the amount of wax or by decreasing the amount of disintegrant, and supersaturation of NiD was achieved without any re-crystallization in dissolution medium. The release rate of NiD from DCMT was controlled by the disintegration rate of Tablet. The release profile of NiD was described by the Hixson–Crowell's model better than zero-order kinetics, first-order kinetics and Higuchi's model, which supports that the release of NiD from DCMT is regulated by the disintegration of the Tablet. From this study, it was clarified that DCMT was one of the promising SR systems applying SD for the poorly water-soluble drugs.