The Experts below are selected from a list of 303 Experts worldwide ranked by ideXlab platform

Dara Fitzpatrick - One of the best experts on this subject based on the ideXlab platform.

  • pH Dependence of the Dissolution Rate of Enteric- Coated Drug Spheres Determined by Broadband Acoustic Resonance Dissolution Spectroscopy (BARDS)
    Dissolution Technologies, 2020
    Co-Authors: Rachel Evans-hurson, Sean Mcsweeney, Jacob Kruse, John J. Keating, Dara Fitzpatrick
    Abstract:

    Enteric Coatings are widely used in formulations of drug delivery spheres. The Coating protects an active pharmaceutical ingredient (API) from acidic conditions in the low pH environment of the stomach. The Coating breaks down readily at higher pH in the lower intestine to allow absorption of the API. The thickness of the Enteric Coating is one of the factors that determine the release rate of the drug in the gastrointestinal tract. It is difficult to determine the loading of the drug layer and Enteric Coating on the core support sphere without conventional dissolution testing during and post manufacture. Broadband acoustic resonance dissolution spectroscopy (BARDS) potentially offers a new, rapid approach to characterizing Enteric Coatings during their manufacture. BARDS applications are based on reproducible changes in the compressibility of a solvent during dissolution, which is monitored acoustically via associated changes in the frequency of induced acoustic resonances. Two drug sphere formulations that yield characteristic and reproducible data were investigated. A steady-state acoustic lag time is associated with the disintegration of the Enteric Coating and drug layer in basic solution. This lag time is pH dependent and is indicative of the rate at which the Coating and layers dissolve. BARDS analysis has the potential to characterize drug sphere formulations at-line in very short timescales. BARDS represents a complementary technique to conventional dissolution testing that could be used in precompliance testing for quality assurance during manufacture. BARDS data, in the future, may also be indicative of the likely performance of a formulation under USP dissolution testing.

  • broadband acoustic resonance dissolution spectroscopy bards a rapid test for Enteric Coating thickness and integrity of controlled release pellet formulations
    International Journal of Pharmaceutics, 2018
    Co-Authors: Anas Alfarsi, Amy Dillon, Sean Mcsweeney, Jacob Kruse, Brendan T Griffin, Ken J Devine, Patricia Sherry, Stephan Henken, Stephen Fitzpatrick, Dara Fitzpatrick
    Abstract:

    Abstract There are no rapid dissolution based tests for determining Coating thickness, integrity and drug concentration in controlled release pellets either during production or post-production. The manufacture of pellets requires several Coating steps depending on the formulation. The sub-Coating and Enteric Coating steps typically take up to six hours each followed by additional drying steps. Post production regulatory dissolution testing also takes up to six hours to determine if the batch can be released for commercial sale. The thickness of the Enteric Coating is a key factor that determines the release rate of the drug in the gastro-intestinal tract. Also, the amount of drug per unit mass decreases with increasing thickness of the Enteric Coating. In this study, the Coating process is tracked from start to finish on an hourly basis by taking samples of pellets during production and testing those using BARDS (Broadband Acoustic Resonance Dissolution Spectroscopy). BARDS offers a rapid approach to characterising Enteric Coatings with measurements based on reproducible changes in the compressibility of a solvent due to the evolution of air during dissolution. This is monitored acoustically via associated changes in the frequency of induced acoustic resonances. A steady state acoustic lag time is associated with the disintegration of the Enteric Coatings in basic solution. This lag time is pH dependent and is indicative of the rate at which the Coating layer dissolves. BARDS represents a possible future surrogate test for conventional USP dissolution testing as its data correlates directly with the thickness of the Enteric Coating, its integrity and also with the drug loading as validated by HPLC.

  • Rapid profiling of Enteric coated drug delivery spheres via broadband acoustic resonance dissolution spectroscopy (BARDS).
    Analyst, 2014
    Co-Authors: Dara Fitzpatrick, Sean Mcsweeney, Jacob Kruse, Rachel Evans-hurson, Y. Fu, T. Burke, P. Casaubieilh, John J. Keating
    Abstract:

    There is an increased trend towards the use of drug and Enteric coated sugar spheres for controlled oral delivery of active pharmaceutical ingredients (API). This trend is driven by increased efficacy and ease of formulation of different dosage levels. However, difficulties exist in determining the thickness of drug and Enteric Coatings in a time efficient manner during manufacture, quality assurance and stability testing. The thickness of the Coating determines the dosage of the API and the thickness of the Enteric Coating determines the release rate of the drug in the gastro-intestinal tract. Broadband Acoustic Resonance Dissolution Spectroscopy (BARDS) offers a rapid new approach to characterising the Enteric Coating thickness and the raw materials used in their manufacture. BARDS applications are based on reproducible changes in the compressibility of a solvent during dissolution which is monitored acoustically due to associated changes in the speed of sound in solution. It is demonstrated how core delivery sugar spheres have unique acoustic spectra attributable to the mean size distribution of the spheres. A steady state acoustic lag time is associated with the disintegration of the Enteric Coating, in basic solution. This lag time can be manipulated by varying the concentration of the base which affects the rate at which the Coating dissolves. It is anticipated that the thickness/loading of the spheres can be estimated from the lag time.

Sean Mcsweeney - One of the best experts on this subject based on the ideXlab platform.

  • pH Dependence of the Dissolution Rate of Enteric- Coated Drug Spheres Determined by Broadband Acoustic Resonance Dissolution Spectroscopy (BARDS)
    Dissolution Technologies, 2020
    Co-Authors: Rachel Evans-hurson, Sean Mcsweeney, Jacob Kruse, John J. Keating, Dara Fitzpatrick
    Abstract:

    Enteric Coatings are widely used in formulations of drug delivery spheres. The Coating protects an active pharmaceutical ingredient (API) from acidic conditions in the low pH environment of the stomach. The Coating breaks down readily at higher pH in the lower intestine to allow absorption of the API. The thickness of the Enteric Coating is one of the factors that determine the release rate of the drug in the gastrointestinal tract. It is difficult to determine the loading of the drug layer and Enteric Coating on the core support sphere without conventional dissolution testing during and post manufacture. Broadband acoustic resonance dissolution spectroscopy (BARDS) potentially offers a new, rapid approach to characterizing Enteric Coatings during their manufacture. BARDS applications are based on reproducible changes in the compressibility of a solvent during dissolution, which is monitored acoustically via associated changes in the frequency of induced acoustic resonances. Two drug sphere formulations that yield characteristic and reproducible data were investigated. A steady-state acoustic lag time is associated with the disintegration of the Enteric Coating and drug layer in basic solution. This lag time is pH dependent and is indicative of the rate at which the Coating and layers dissolve. BARDS analysis has the potential to characterize drug sphere formulations at-line in very short timescales. BARDS represents a complementary technique to conventional dissolution testing that could be used in precompliance testing for quality assurance during manufacture. BARDS data, in the future, may also be indicative of the likely performance of a formulation under USP dissolution testing.

  • broadband acoustic resonance dissolution spectroscopy bards a rapid test for Enteric Coating thickness and integrity of controlled release pellet formulations
    International Journal of Pharmaceutics, 2018
    Co-Authors: Anas Alfarsi, Amy Dillon, Sean Mcsweeney, Jacob Kruse, Brendan T Griffin, Ken J Devine, Patricia Sherry, Stephan Henken, Stephen Fitzpatrick, Dara Fitzpatrick
    Abstract:

    Abstract There are no rapid dissolution based tests for determining Coating thickness, integrity and drug concentration in controlled release pellets either during production or post-production. The manufacture of pellets requires several Coating steps depending on the formulation. The sub-Coating and Enteric Coating steps typically take up to six hours each followed by additional drying steps. Post production regulatory dissolution testing also takes up to six hours to determine if the batch can be released for commercial sale. The thickness of the Enteric Coating is a key factor that determines the release rate of the drug in the gastro-intestinal tract. Also, the amount of drug per unit mass decreases with increasing thickness of the Enteric Coating. In this study, the Coating process is tracked from start to finish on an hourly basis by taking samples of pellets during production and testing those using BARDS (Broadband Acoustic Resonance Dissolution Spectroscopy). BARDS offers a rapid approach to characterising Enteric Coatings with measurements based on reproducible changes in the compressibility of a solvent due to the evolution of air during dissolution. This is monitored acoustically via associated changes in the frequency of induced acoustic resonances. A steady state acoustic lag time is associated with the disintegration of the Enteric Coatings in basic solution. This lag time is pH dependent and is indicative of the rate at which the Coating layer dissolves. BARDS represents a possible future surrogate test for conventional USP dissolution testing as its data correlates directly with the thickness of the Enteric Coating, its integrity and also with the drug loading as validated by HPLC.

  • Rapid profiling of Enteric coated drug delivery spheres via broadband acoustic resonance dissolution spectroscopy (BARDS).
    Analyst, 2014
    Co-Authors: Dara Fitzpatrick, Sean Mcsweeney, Jacob Kruse, Rachel Evans-hurson, Y. Fu, T. Burke, P. Casaubieilh, John J. Keating
    Abstract:

    There is an increased trend towards the use of drug and Enteric coated sugar spheres for controlled oral delivery of active pharmaceutical ingredients (API). This trend is driven by increased efficacy and ease of formulation of different dosage levels. However, difficulties exist in determining the thickness of drug and Enteric Coatings in a time efficient manner during manufacture, quality assurance and stability testing. The thickness of the Coating determines the dosage of the API and the thickness of the Enteric Coating determines the release rate of the drug in the gastro-intestinal tract. Broadband Acoustic Resonance Dissolution Spectroscopy (BARDS) offers a rapid new approach to characterising the Enteric Coating thickness and the raw materials used in their manufacture. BARDS applications are based on reproducible changes in the compressibility of a solvent during dissolution which is monitored acoustically due to associated changes in the speed of sound in solution. It is demonstrated how core delivery sugar spheres have unique acoustic spectra attributable to the mean size distribution of the spheres. A steady state acoustic lag time is associated with the disintegration of the Enteric Coating, in basic solution. This lag time can be manipulated by varying the concentration of the base which affects the rate at which the Coating dissolves. It is anticipated that the thickness/loading of the spheres can be estimated from the lag time.

Jacob Kruse - One of the best experts on this subject based on the ideXlab platform.

  • pH Dependence of the Dissolution Rate of Enteric- Coated Drug Spheres Determined by Broadband Acoustic Resonance Dissolution Spectroscopy (BARDS)
    Dissolution Technologies, 2020
    Co-Authors: Rachel Evans-hurson, Sean Mcsweeney, Jacob Kruse, John J. Keating, Dara Fitzpatrick
    Abstract:

    Enteric Coatings are widely used in formulations of drug delivery spheres. The Coating protects an active pharmaceutical ingredient (API) from acidic conditions in the low pH environment of the stomach. The Coating breaks down readily at higher pH in the lower intestine to allow absorption of the API. The thickness of the Enteric Coating is one of the factors that determine the release rate of the drug in the gastrointestinal tract. It is difficult to determine the loading of the drug layer and Enteric Coating on the core support sphere without conventional dissolution testing during and post manufacture. Broadband acoustic resonance dissolution spectroscopy (BARDS) potentially offers a new, rapid approach to characterizing Enteric Coatings during their manufacture. BARDS applications are based on reproducible changes in the compressibility of a solvent during dissolution, which is monitored acoustically via associated changes in the frequency of induced acoustic resonances. Two drug sphere formulations that yield characteristic and reproducible data were investigated. A steady-state acoustic lag time is associated with the disintegration of the Enteric Coating and drug layer in basic solution. This lag time is pH dependent and is indicative of the rate at which the Coating and layers dissolve. BARDS analysis has the potential to characterize drug sphere formulations at-line in very short timescales. BARDS represents a complementary technique to conventional dissolution testing that could be used in precompliance testing for quality assurance during manufacture. BARDS data, in the future, may also be indicative of the likely performance of a formulation under USP dissolution testing.

  • broadband acoustic resonance dissolution spectroscopy bards a rapid test for Enteric Coating thickness and integrity of controlled release pellet formulations
    International Journal of Pharmaceutics, 2018
    Co-Authors: Anas Alfarsi, Amy Dillon, Sean Mcsweeney, Jacob Kruse, Brendan T Griffin, Ken J Devine, Patricia Sherry, Stephan Henken, Stephen Fitzpatrick, Dara Fitzpatrick
    Abstract:

    Abstract There are no rapid dissolution based tests for determining Coating thickness, integrity and drug concentration in controlled release pellets either during production or post-production. The manufacture of pellets requires several Coating steps depending on the formulation. The sub-Coating and Enteric Coating steps typically take up to six hours each followed by additional drying steps. Post production regulatory dissolution testing also takes up to six hours to determine if the batch can be released for commercial sale. The thickness of the Enteric Coating is a key factor that determines the release rate of the drug in the gastro-intestinal tract. Also, the amount of drug per unit mass decreases with increasing thickness of the Enteric Coating. In this study, the Coating process is tracked from start to finish on an hourly basis by taking samples of pellets during production and testing those using BARDS (Broadband Acoustic Resonance Dissolution Spectroscopy). BARDS offers a rapid approach to characterising Enteric Coatings with measurements based on reproducible changes in the compressibility of a solvent due to the evolution of air during dissolution. This is monitored acoustically via associated changes in the frequency of induced acoustic resonances. A steady state acoustic lag time is associated with the disintegration of the Enteric Coatings in basic solution. This lag time is pH dependent and is indicative of the rate at which the Coating layer dissolves. BARDS represents a possible future surrogate test for conventional USP dissolution testing as its data correlates directly with the thickness of the Enteric Coating, its integrity and also with the drug loading as validated by HPLC.

  • Rapid profiling of Enteric coated drug delivery spheres via broadband acoustic resonance dissolution spectroscopy (BARDS).
    Analyst, 2014
    Co-Authors: Dara Fitzpatrick, Sean Mcsweeney, Jacob Kruse, Rachel Evans-hurson, Y. Fu, T. Burke, P. Casaubieilh, John J. Keating
    Abstract:

    There is an increased trend towards the use of drug and Enteric coated sugar spheres for controlled oral delivery of active pharmaceutical ingredients (API). This trend is driven by increased efficacy and ease of formulation of different dosage levels. However, difficulties exist in determining the thickness of drug and Enteric Coatings in a time efficient manner during manufacture, quality assurance and stability testing. The thickness of the Coating determines the dosage of the API and the thickness of the Enteric Coating determines the release rate of the drug in the gastro-intestinal tract. Broadband Acoustic Resonance Dissolution Spectroscopy (BARDS) offers a rapid new approach to characterising the Enteric Coating thickness and the raw materials used in their manufacture. BARDS applications are based on reproducible changes in the compressibility of a solvent during dissolution which is monitored acoustically due to associated changes in the speed of sound in solution. It is demonstrated how core delivery sugar spheres have unique acoustic spectra attributable to the mean size distribution of the spheres. A steady state acoustic lag time is associated with the disintegration of the Enteric Coating, in basic solution. This lag time can be manipulated by varying the concentration of the base which affects the rate at which the Coating dissolves. It is anticipated that the thickness/loading of the spheres can be estimated from the lag time.

Hiroyasu Kokubo - One of the best experts on this subject based on the ideXlab platform.

  • site specific drug delivery to the middle region of the small intestine by application of Enteric Coating with hypromellose acetate succinate hpmcas
    Journal of Pharmaceutical Sciences, 2008
    Co-Authors: Fumie Tanno, Hiroyasu Kokubo, Shinji Sakuma, Yoshie Masaoka, Makoto Kataoka, Toshio Kozaki, Ryosei Kamaguchi, Yutaka Ikeda, Shinji Yamashita
    Abstract:

    Enteric Coatings that deliver drugs to specific regions of the small intestine were examined. Hypromellose acetate succinate (HPMCAS) with different values of succinoyl group contents was used. Decreasing the succinoyl group content resulted in an increase in the pH at which HPMCAS started to dissolve. Drug-containing granules with or without Enteric Coating were prepared and their in vitro dissolution in a simulated intestinal fluid of pH 6.8 was examined. Granules coated with HPMCAS having the succinoyl group content of 6.2% showed a lag time of about 30 min, although drug release from granules without Coating was completed within 20 min. The time lag and dissolution rate were extended and reduced, respectively, as the succinoyl group content was decreased. Rat experiments indicated that Enteric-coated granules disintegrated and the bulk of the drugs was immediately released when the granules reached a specific site of the small intestine where the pH corresponded to the pH at which the Enteric Coating agent started to dissolve. Similar results were observed in monkey experiments. It was suggested that HPMCAS with the succinoyl group content of about 5% was suitable as an Enteric Coating agent for delivering drugs to the middle-to-lower region of the small intestine.

  • Site‐specific drug delivery to the middle region of the small intestine by application of Enteric Coating with hypromellose acetate succinate (HPMCAS)
    Journal of Pharmaceutical Sciences, 2008
    Co-Authors: Fumie Tanno, Hiroyasu Kokubo, Shinji Sakuma, Yoshie Masaoka, Makoto Kataoka, Toshio Kozaki, Ryosei Kamaguchi, Yutaka Ikeda, Shinji Yamashita
    Abstract:

    Enteric Coatings that deliver drugs to specific regions of the small intestine were examined. Hypromellose acetate succinate (HPMCAS) with different values of succinoyl group contents was used. Decreasing the succinoyl group content resulted in an increase in the pH at which HPMCAS started to dissolve. Drug-containing granules with or without Enteric Coating were prepared and their in vitro dissolution in a simulated intestinal fluid of pH 6.8 was examined. Granules coated with HPMCAS having the succinoyl group content of 6.2% showed a lag time of about 30 min, although drug release from granules without Coating was completed within 20 min. The time lag and dissolution rate were extended and reduced, respectively, as the succinoyl group content was decreased. Rat experiments indicated that Enteric-coated granules disintegrated and the bulk of the drugs was immediately released when the granules reached a specific site of the small intestine where the pH corresponded to the pH at which the Enteric Coating agent started to dissolve. Similar results were observed in monkey experiments. It was suggested that HPMCAS with the succinoyl group content of about 5% was suitable as an Enteric Coating agent for delivering drugs to the middle-to-lower region of the small intestine.

  • dry Coating an innovative Enteric Coating method using a cellulose derivative
    European Journal of Pharmaceutics and Biopharmaceutics, 1999
    Co-Authors: Sakae Obara, Naosuke Maruyama, Yuichi Nishiyama, Hiroyasu Kokubo
    Abstract:

    Abstract A novel Enteric Coating method was developed. This method involves direct feeding of Coating polymer powder and simultaneous spraying of plasticizing agent, without either organic solvent or water, using a centrifugal granulator, fluidized bed, or tablet-Coating machine. For film formation, a curing step was then necessary; this involved spraying a small amount (3–8% of core weight) of water or hydroxypropyl methylcellulose solution, followed by heating. Hydroxypropyl methylcellulose acetate succinate was used as the Enteric Coating polymer, and a combination of triethyl citrate and acetylated monoglyceride was used for plasticization. The coated beads and tablets were evaluated for gastric resistance, intestinal disintegration, and stability, in comparison with beads and tablets from a conventional aqueous Coating with the same Enteric polymer. The new method required a higher Coating amount for gastric resistance compared with the conventional Coating, but the processing time was dramatically reduced. The results show that this dry Coating method is applicable to the preparation of Enteric-coated beads and tablets using commercially available lab-scale apparatus.

  • development of cellulose derivatives as novel Enteric Coating agents soluble at ph 3 5 4 5 and higher
    Chemical & Pharmaceutical Bulletin, 1997
    Co-Authors: Hiroyasu Kokubo, Sakae Obara, Katsuyoshi Minemura, Takashi Tanaka
    Abstract:

    Hydroxypropyl methylcellulose (HPMC) was selected as a base polymer to develop novel Enteric Coating agents for acid protection which can dissolve at pH around 4, and was modified with trimellitic acid or maleic acid at various degrees of substitution. These carboxylic acids have higher dissociation constants and higher solubility in water than the carboxylic acids of existing Enteric Coating polymers. The synthesized polymers were micronized and dispersed in aqueous medium to determine their pKa values by potentiometric titration. The pH of dissolution and the water vapor permeability of the cast films prepared from organic solutions were also evaluated. Hydroxypropyl methylcellulose trimellitate (HPMCT) showed good acid resistance, and the pH at which it dissolves can be controlled in the range of pH 3.5 to 4.5 by varying the content of trimellityl groups and the methoxyl substitution of the base polymer.

Shinji Yamashita - One of the best experts on this subject based on the ideXlab platform.

  • site specific drug delivery to the middle region of the small intestine by application of Enteric Coating with hypromellose acetate succinate hpmcas
    Journal of Pharmaceutical Sciences, 2008
    Co-Authors: Fumie Tanno, Hiroyasu Kokubo, Shinji Sakuma, Yoshie Masaoka, Makoto Kataoka, Toshio Kozaki, Ryosei Kamaguchi, Yutaka Ikeda, Shinji Yamashita
    Abstract:

    Enteric Coatings that deliver drugs to specific regions of the small intestine were examined. Hypromellose acetate succinate (HPMCAS) with different values of succinoyl group contents was used. Decreasing the succinoyl group content resulted in an increase in the pH at which HPMCAS started to dissolve. Drug-containing granules with or without Enteric Coating were prepared and their in vitro dissolution in a simulated intestinal fluid of pH 6.8 was examined. Granules coated with HPMCAS having the succinoyl group content of 6.2% showed a lag time of about 30 min, although drug release from granules without Coating was completed within 20 min. The time lag and dissolution rate were extended and reduced, respectively, as the succinoyl group content was decreased. Rat experiments indicated that Enteric-coated granules disintegrated and the bulk of the drugs was immediately released when the granules reached a specific site of the small intestine where the pH corresponded to the pH at which the Enteric Coating agent started to dissolve. Similar results were observed in monkey experiments. It was suggested that HPMCAS with the succinoyl group content of about 5% was suitable as an Enteric Coating agent for delivering drugs to the middle-to-lower region of the small intestine.

  • Site‐specific drug delivery to the middle region of the small intestine by application of Enteric Coating with hypromellose acetate succinate (HPMCAS)
    Journal of Pharmaceutical Sciences, 2008
    Co-Authors: Fumie Tanno, Hiroyasu Kokubo, Shinji Sakuma, Yoshie Masaoka, Makoto Kataoka, Toshio Kozaki, Ryosei Kamaguchi, Yutaka Ikeda, Shinji Yamashita
    Abstract:

    Enteric Coatings that deliver drugs to specific regions of the small intestine were examined. Hypromellose acetate succinate (HPMCAS) with different values of succinoyl group contents was used. Decreasing the succinoyl group content resulted in an increase in the pH at which HPMCAS started to dissolve. Drug-containing granules with or without Enteric Coating were prepared and their in vitro dissolution in a simulated intestinal fluid of pH 6.8 was examined. Granules coated with HPMCAS having the succinoyl group content of 6.2% showed a lag time of about 30 min, although drug release from granules without Coating was completed within 20 min. The time lag and dissolution rate were extended and reduced, respectively, as the succinoyl group content was decreased. Rat experiments indicated that Enteric-coated granules disintegrated and the bulk of the drugs was immediately released when the granules reached a specific site of the small intestine where the pH corresponded to the pH at which the Enteric Coating agent started to dissolve. Similar results were observed in monkey experiments. It was suggested that HPMCAS with the succinoyl group content of about 5% was suitable as an Enteric Coating agent for delivering drugs to the middle-to-lower region of the small intestine.