Structured solubility behaviour in bioequivalent fasted simulated intestinal fluids
Eur J Pharm Biopharm. 2022 May 20:S0939-6411(22)00098-4. doi: 10.1016/j.ejpb.2022.05.010. Online ahead of print.ABSTRACTDrug solubility in intestinal fluid is a key parameter controlling absorption after the administration of a solid oral dosage form. To measure solubility in vitro simulated intestinal fluids have been developed, but there are multiple recipes and the optimum is unknown. This situation creates difficulties during drug discovery and development research. A recent study characterised sampled fasted intestinal fluids using a multidimensional approach to derive nine bioequivalent fasted intestinal media that c...
Source: European Journal of Pharmaceutics and Biopharmaceutics - May 23, 2022 Category: Drugs & Pharmacology Authors: Qamar Abuhassan Ibrahim Khadra Kate Pyper Patrick Augustijns Joachim Brouwers Gavin W Halbert Source Type: research
Structured solubility behaviour in bioequivalent fasted simulated intestinal fluids
Eur J Pharm Biopharm. 2022 May 20:S0939-6411(22)00098-4. doi: 10.1016/j.ejpb.2022.05.010. Online ahead of print.ABSTRACTDrug solubility in intestinal fluid is a key parameter controlling absorption after the administration of a solid oral dosage form. To measure solubility in vitro simulated intestinal fluids have been developed, but there are multiple recipes and the optimum is unknown. This situation creates difficulties during drug discovery and development research. A recent study characterised sampled fasted intestinal fluids using a multidimensional approach to derive nine bioequivalent fasted intestinal media that c...
Source: European Journal of Pharmaceutics and Biopharmaceutics - May 23, 2022 Category: Drugs & Pharmacology Authors: Qamar Abuhassan Ibrahim Khadra Kate Pyper Patrick Augustijns Joachim Brouwers Gavin W Halbert Source Type: research
Structured solubility behaviour in bioequivalent fasted simulated intestinal fluids
Eur J Pharm Biopharm. 2022 May 20:S0939-6411(22)00098-4. doi: 10.1016/j.ejpb.2022.05.010. Online ahead of print.ABSTRACTDrug solubility in intestinal fluid is a key parameter controlling absorption after the administration of a solid oral dosage form. To measure solubility in vitro simulated intestinal fluids have been developed, but there are multiple recipes and the optimum is unknown. This situation creates difficulties during drug discovery and development research. A recent study characterised sampled fasted intestinal fluids using a multidimensional approach to derive nine bioequivalent fasted intestinal media that c...
Source: European Journal of Pharmaceutics and Biopharmaceutics - May 23, 2022 Category: Drugs & Pharmacology Authors: Qamar Abuhassan Ibrahim Khadra Kate Pyper Patrick Augustijns Joachim Brouwers Gavin W Halbert Source Type: research
Structured solubility behaviour in bioequivalent fasted simulated intestinal fluids
Eur J Pharm Biopharm. 2022 May 20:S0939-6411(22)00098-4. doi: 10.1016/j.ejpb.2022.05.010. Online ahead of print.ABSTRACTDrug solubility in intestinal fluid is a key parameter controlling absorption after the administration of a solid oral dosage form. To measure solubility in vitro simulated intestinal fluids have been developed, but there are multiple recipes and the optimum is unknown. This situation creates difficulties during drug discovery and development research. A recent study characterised sampled fasted intestinal fluids using a multidimensional approach to derive nine bioequivalent fasted intestinal media that c...
Source: European Journal of Pharmaceutics and Biopharmaceutics - May 23, 2022 Category: Drugs & Pharmacology Authors: Qamar Abuhassan Ibrahim Khadra Kate Pyper Patrick Augustijns Joachim Brouwers Gavin W Halbert Source Type: research
Structured solubility behaviour in bioequivalent fasted simulated intestinal fluids
Eur J Pharm Biopharm. 2022 May 20:S0939-6411(22)00098-4. doi: 10.1016/j.ejpb.2022.05.010. Online ahead of print.ABSTRACTDrug solubility in intestinal fluid is a key parameter controlling absorption after the administration of a solid oral dosage form. To measure solubility in vitro simulated intestinal fluids have been developed, but there are multiple recipes and the optimum is unknown. This situation creates difficulties during drug discovery and development research. A recent study characterised sampled fasted intestinal fluids using a multidimensional approach to derive nine bioequivalent fasted intestinal media that c...
Source: European Journal of Pharmaceutics and Biopharmaceutics - May 23, 2022 Category: Drugs & Pharmacology Authors: Qamar Abuhassan Ibrahim Khadra Kate Pyper Patrick Augustijns Joachim Brouwers Gavin W Halbert Source Type: research
Structured solubility behaviour in bioequivalent fasted simulated intestinal fluids
Eur J Pharm Biopharm. 2022 May 20:S0939-6411(22)00098-4. doi: 10.1016/j.ejpb.2022.05.010. Online ahead of print.ABSTRACTDrug solubility in intestinal fluid is a key parameter controlling absorption after the administration of a solid oral dosage form. To measure solubility in vitro simulated intestinal fluids have been developed, but there are multiple recipes and the optimum is unknown. This situation creates difficulties during drug discovery and development research. A recent study characterised sampled fasted intestinal fluids using a multidimensional approach to derive nine bioequivalent fasted intestinal media that c...
Source: European Journal of Pharmaceutics and Biopharmaceutics - May 23, 2022 Category: Drugs & Pharmacology Authors: Qamar Abuhassan Ibrahim Khadra Kate Pyper Patrick Augustijns Joachim Brouwers Gavin W Halbert Source Type: research
Structured solubility behaviour in bioequivalent fasted simulated intestinal fluids
Eur J Pharm Biopharm. 2022 May 20:S0939-6411(22)00098-4. doi: 10.1016/j.ejpb.2022.05.010. Online ahead of print.ABSTRACTDrug solubility in intestinal fluid is a key parameter controlling absorption after the administration of a solid oral dosage form. To measure solubility in vitro simulated intestinal fluids have been developed, but there are multiple recipes and the optimum is unknown. This situation creates difficulties during drug discovery and development research. A recent study characterised sampled fasted intestinal fluids using a multidimensional approach to derive nine bioequivalent fasted intestinal media that c...
Source: European Journal of Pharmaceutics and Biopharmaceutics - May 23, 2022 Category: Drugs & Pharmacology Authors: Qamar Abuhassan Ibrahim Khadra Kate Pyper Patrick Augustijns Joachim Brouwers Gavin W Halbert Source Type: research
Choline-Amino Acid-Derived Bio-ionic Liquids for Solubility Enhancement of Zafirlukast
This study investigated the application of bio-ionic liquids (ILs) prepared from choline as cation and amino acid as anion for solubility enhancement of poorly water-soluble drug, Zafirlukast (ZFL). Herein, the solubility of ZFL in water and mixtures of water and ILs was assessed using UV spectroscopy at two temperature points 25°C and 37°C with increasing concentrations of IL. ZFL solubility was found to improve linearly with increasing concentration of [Ch][Pro] in water, representing 35- to 37-fold improvement in ZFL solubility at maximum concentration of [Ch][Pro] (1% w/v) compared to when only pure water was present...
Source: AAPS PharmSciTech - May 18, 2022 Category: Drugs & Pharmacology Authors: Namrata Gaikwad Swapna Kudal Amelia M Avachat Source Type: research
Choline-Amino Acid-Derived Bio-ionic Liquids for Solubility Enhancement of Zafirlukast
This study investigated the application of bio-ionic liquids (ILs) prepared from choline as cation and amino acid as anion for solubility enhancement of poorly water-soluble drug, Zafirlukast (ZFL). Herein, the solubility of ZFL in water and mixtures of water and ILs was assessed using UV spectroscopy at two temperature points 25°C and 37°C with increasing concentrations of IL. ZFL solubility was found to improve linearly with increasing concentration of [Ch][Pro] in water, representing 35- to 37-fold improvement in ZFL solubility at maximum concentration of [Ch][Pro] (1% w/v) compared to when only pure water was present...
Source: AAPS PharmSciTech - May 18, 2022 Category: Drugs & Pharmacology Authors: Namrata Gaikwad Swapna Kudal Amelia M Avachat Source Type: research
A SWELL time to develop the molecular pharmacology of the volume-regulated anion channel (VRAC)
Channels (Austin). 2022 Dec;16(1):27-36. doi: 10.1080/19336950.2022.2033511.ABSTRACTNewly emerging roles of LRRC8 volume-regulated anion channels (VRAC) raise important questions about the therapeutic potential of VRAC in the treatment of epilepsy, type 2 diabetes, and other human diseases. A critical barrier to evaluating whether VRAC represents a viable drug target is the lack of potent and specific small-molecule inhibitors and activators of the channel. Here we review recent progress in developing the molecular pharmacology of VRAC made by screening a library of FDA-approved drugs for novel channel modulators. We discu...
Source: Channels - February 4, 2022 Category: Molecular Biology Authors: Eric E Figueroa Jerod S Denton Source Type: research
A SWELL time to develop the molecular pharmacology of the volume-regulated anion channel (VRAC)
Channels (Austin). 2022 Dec;16(1):27-36. doi: 10.1080/19336950.2022.2033511.ABSTRACTNewly emerging roles of LRRC8 volume-regulated anion channels (VRAC) raise important questions about the therapeutic potential of VRAC in the treatment of epilepsy, type 2 diabetes, and other human diseases. A critical barrier to evaluating whether VRAC represents a viable drug target is the lack of potent and specific small-molecule inhibitors and activators of the channel. Here we review recent progress in developing the molecular pharmacology of VRAC made by screening a library of FDA-approved drugs for novel channel modulators. We discu...
Source: Channels - February 4, 2022 Category: Molecular Biology Authors: Eric E Figueroa Jerod S Denton Source Type: research
A SWELL time to develop the molecular pharmacology of the volume-regulated anion channel (VRAC)
Channels (Austin). 2022 Dec;16(1):27-36. doi: 10.1080/19336950.2022.2033511.ABSTRACTNewly emerging roles of LRRC8 volume-regulated anion channels (VRAC) raise important questions about the therapeutic potential of VRAC in the treatment of epilepsy, type 2 diabetes, and other human diseases. A critical barrier to evaluating whether VRAC represents a viable drug target is the lack of potent and specific small-molecule inhibitors and activators of the channel. Here we review recent progress in developing the molecular pharmacology of VRAC made by screening a library of FDA-approved drugs for novel channel modulators. We discu...
Source: Channels - February 4, 2022 Category: Molecular Biology Authors: Eric E Figueroa Jerod S Denton Source Type: research
A SWELL time to develop the molecular pharmacology of the volume-regulated anion channel (VRAC)
Channels (Austin). 2022 Dec;16(1):27-36. doi: 10.1080/19336950.2022.2033511.ABSTRACTNewly emerging roles of LRRC8 volume-regulated anion channels (VRAC) raise important questions about the therapeutic potential of VRAC in the treatment of epilepsy, type 2 diabetes, and other human diseases. A critical barrier to evaluating whether VRAC represents a viable drug target is the lack of potent and specific small-molecule inhibitors and activators of the channel. Here we review recent progress in developing the molecular pharmacology of VRAC made by screening a library of FDA-approved drugs for novel channel modulators. We discu...
Source: Channels - February 4, 2022 Category: Molecular Biology Authors: Eric E Figueroa Jerod S Denton Source Type: research
