The Physical Stability of Felodipine and Its Recrystallization from an Amorphous Solid Dispersion Studied by NMR Relaxometry
AAPS PharmSciTech. 2022 Mar 21;23(4):93. doi: 10.1208/s12249-022-02234-8.ABSTRACTThe 1H nuclear magnetic resonance (NMR) relaxometry method was applied to investigate the physical stability of an active pharmaceutical ingredient (API) and, for the first time, its recrystallization process in an amorphous solid dispersion system (ASD). The ASD of felodipine and polyvinylpyrrolidone (PVP) was prepared using the solvent evaporation method in a mass ratio of 50:50. In the first stage of the study (250 days), the sample was stored at 0% relative humidity (RH). The recovery of magnetization was described by one-exponential funct...
Source: AAPS PharmSciTech - March 22, 2022 Category: Drugs & Pharmacology Authors: A Pajzderska J Mielcarek J W ąsicki Source Type: research
Structural basis of Klotho binding to VEGFR2 and TRPC1 and repurposing calcium channel blockers as TRPC1 antagonists for the treatment of age-related cardiac hypertrophy
Arch Biochem Biophys. 2022 Mar 3:109171. doi: 10.1016/j.abb.2022.109171. Online ahead of print.ABSTRACTCardiac hypertrophy results in the higher rate of heart failures among aged groups. Klotho is an anti-aging protein that is involved in the regulation of VEGF-mediated Ca2+ entry by direct interaction with Vascular endothelial growth factor receptor 2 (VEGFR2) and transient receptor potential canonical Ca2+ channel 1 (TRPC1). Here, in this study, through in silico analysis, we modeled TRPC1 3-dimensional structure and followed by its optimization, characterized the interaction pattern of TRPC1, Klotho and VEGFR2. Subseque...
Source: Archives of Biochemistry and Biophysics - March 6, 2022 Category: Biochemistry Authors: Muhammad Fakhar None Najumuddin Sana Zahid Sajid Rashid Source Type: research
Structural basis of Klotho binding to VEGFR2 and TRPC1 and repurposing calcium channel blockers as TRPC1 antagonists for the treatment of age-related cardiac hypertrophy
Arch Biochem Biophys. 2022 Mar 3:109171. doi: 10.1016/j.abb.2022.109171. Online ahead of print.ABSTRACTCardiac hypertrophy results in the higher rate of heart failures among aged groups. Klotho is an anti-aging protein that is involved in the regulation of VEGF-mediated Ca2+ entry by direct interaction with Vascular endothelial growth factor receptor 2 (VEGFR2) and transient receptor potential canonical Ca2+ channel 1 (TRPC1). Here, in this study, through in silico analysis, we modeled TRPC1 3-dimensional structure and followed by its optimization, characterized the interaction pattern of TRPC1, Klotho and VEGFR2. Subseque...
Source: Archives of Biochemistry and Biophysics - March 6, 2022 Category: Biochemistry Authors: Muhammad Fakhar None Najumuddin Sana Zahid Sajid Rashid Source Type: research
Structural basis of Klotho binding to VEGFR2 and TRPC1 and repurposing calcium channel blockers as TRPC1 antagonists for the treatment of age-related cardiac hypertrophy
Arch Biochem Biophys. 2022 Mar 4;719:109171. doi: 10.1016/j.abb.2022.109171. Online ahead of print.ABSTRACTCardiac hypertrophy results in the higher rate of heart failures among aged groups. Klotho is an anti-aging protein that is involved in the regulation of VEGF-mediated Ca2+ entry by direct interaction with Vascular endothelial growth factor receptor 2 (VEGFR2) and transient receptor potential canonical Ca2+ channel 1 (TRPC1). Here, in this study, through in silico analysis, we modeled TRPC1 3-dimensional structure and followed by its optimization, characterized the interaction pattern of TRPC1, Klotho and VEGFR2. Subs...
Source: Archives of Biochemistry and Biophysics - March 6, 2022 Category: Biochemistry Authors: Muhammad Fakhar None Najumuddin Sana Zahid Sajid Rashid Source Type: research
Structural basis of Klotho binding to VEGFR2 and TRPC1 and repurposing calcium channel blockers as TRPC1 antagonists for the treatment of age-related cardiac hypertrophy
Arch Biochem Biophys. 2022 Mar 4;719:109171. doi: 10.1016/j.abb.2022.109171. Online ahead of print.ABSTRACTCardiac hypertrophy results in the higher rate of heart failures among aged groups. Klotho is an anti-aging protein that is involved in the regulation of VEGF-mediated Ca2+ entry by direct interaction with Vascular endothelial growth factor receptor 2 (VEGFR2) and transient receptor potential canonical Ca2+ channel 1 (TRPC1). Here, in this study, through in silico analysis, we modeled TRPC1 3-dimensional structure and followed by its optimization, characterized the interaction pattern of TRPC1, Klotho and VEGFR2. Subs...
Source: Archives of Biochemistry and Biophysics - March 6, 2022 Category: Biochemistry Authors: Muhammad Fakhar None Najumuddin Sana Zahid Sajid Rashid Source Type: research
Structural basis of Klotho binding to VEGFR2 and TRPC1 and repurposing calcium channel blockers as TRPC1 antagonists for the treatment of age-related cardiac hypertrophy
Arch Biochem Biophys. 2022 Mar 4;719:109171. doi: 10.1016/j.abb.2022.109171. Online ahead of print.ABSTRACTCardiac hypertrophy results in the higher rate of heart failures among aged groups. Klotho is an anti-aging protein that is involved in the regulation of VEGF-mediated Ca2+ entry by direct interaction with Vascular endothelial growth factor receptor 2 (VEGFR2) and transient receptor potential canonical Ca2+ channel 1 (TRPC1). Here, in this study, through in silico analysis, we modeled TRPC1 3-dimensional structure and followed by its optimization, characterized the interaction pattern of TRPC1, Klotho and VEGFR2. Subs...
Source: Archives of Biochemistry and Biophysics - March 6, 2022 Category: Biochemistry Authors: Muhammad Fakhar None Najumuddin Sana Zahid Sajid Rashid Source Type: research
Structural basis of Klotho binding to VEGFR2 and TRPC1 and repurposing calcium channel blockers as TRPC1 antagonists for the treatment of age-related cardiac hypertrophy
Arch Biochem Biophys. 2022 Mar 4;719:109171. doi: 10.1016/j.abb.2022.109171. Online ahead of print.ABSTRACTCardiac hypertrophy results in the higher rate of heart failures among aged groups. Klotho is an anti-aging protein that is involved in the regulation of VEGF-mediated Ca2+ entry by direct interaction with Vascular endothelial growth factor receptor 2 (VEGFR2) and transient receptor potential canonical Ca2+ channel 1 (TRPC1). Here, in this study, through in silico analysis, we modeled TRPC1 3-dimensional structure and followed by its optimization, characterized the interaction pattern of TRPC1, Klotho and VEGFR2. Subs...
Source: Archives of Biochemistry and Biophysics - March 6, 2022 Category: Biochemistry Authors: Muhammad Fakhar None Najumuddin Sana Zahid Sajid Rashid Source Type: research
Structural basis of Klotho binding to VEGFR2 and TRPC1 and repurposing calcium channel blockers as TRPC1 antagonists for the treatment of age-related cardiac hypertrophy
Arch Biochem Biophys. 2022 Mar 4;719:109171. doi: 10.1016/j.abb.2022.109171. Online ahead of print.ABSTRACTCardiac hypertrophy results in the higher rate of heart failures among aged groups. Klotho is an anti-aging protein that is involved in the regulation of VEGF-mediated Ca2+ entry by direct interaction with Vascular endothelial growth factor receptor 2 (VEGFR2) and transient receptor potential canonical Ca2+ channel 1 (TRPC1). Here, in this study, through in silico analysis, we modeled TRPC1 3-dimensional structure and followed by its optimization, characterized the interaction pattern of TRPC1, Klotho and VEGFR2. Subs...
Source: Archives of Biochemistry and Biophysics - March 6, 2022 Category: Biochemistry Authors: Muhammad Fakhar None Najumuddin Sana Zahid Sajid Rashid Source Type: research
Clinical Outcome and Medical Cost of Originator and Generic Antihypertensive Drugs: A Population-Based Study in Yinzhou, China
Conclusion: We observed comparable or even better clinical outcomes and less medical cost associated with the use of antihypertensive generics compared to originator counterparts. This could help increase patient and provider confidence in the efficacy of generic medicines to manage hypertension diseases. (Source: Frontiers in Pharmacology)
Source: Frontiers in Pharmacology - February 22, 2022 Category: Drugs & Pharmacology Source Type: research
[ASAP] SolidLiquid Phase Equilibrium and the Thermodynamic Correlation of Felodipine Form I in Pure and Mixed Solvents
Journal of Chemical& Engineering DataDOI: 10.1021/acs.jced.1c00566 (Source: Journal of Chemical and Engineering Data)
Source: Journal of Chemical and Engineering Data - January 18, 2022 Category: Chemistry Authors: Shasha Li, Xiaqing Nie, Chao Liu, and Danhong Zhou Source Type: research
Small scale in vitro method to determine a bioequivalent equilibrium solubility range for fasted human intestinal fluid
This study demonstrates that it is possible to assess the fasted intestinal equilibrium solubility envelope using a small number of bioequivalent media recipes obtained from a multi-dimensional analysis of fasted HIF. The derivation of the nine bioequivalent SIF media coupled with the lower measured solubility range indicate that the solubility results are more likely to reflect the fasted intestinal solubility envelope than previous DoE studies and highlight that intestinal solubility is a range and not a single value.PMID:34419602 | DOI:10.1016/j.ejpb.2021.08.002 (Source: European Journal of Pharmaceutics and Biopharmaceutics)
Source: European Journal of Pharmaceutics and Biopharmaceutics - August 22, 2021 Category: Drugs & Pharmacology Authors: Qamar Abuhassan Ibrahim Khadra Kate Pyper Gavin W Halbert Source Type: research
Small scale in vitro method to determine a bioequivalent equilibrium solubility range for fasted human intestinal fluid
This study demonstrates that it is possible to assess the fasted intestinal equilibrium solubility envelope using a small number of bioequivalent media recipes obtained from a multi-dimensional analysis of fasted HIF. The derivation of the nine bioequivalent SIF media coupled with the lower measured solubility range indicate that the solubility results are more likely to reflect the fasted intestinal solubility envelope than previous DoE studies and highlight that intestinal solubility is a range and not a single value.PMID:34419602 | DOI:10.1016/j.ejpb.2021.08.002 (Source: European Journal of Pharmaceutics and Biopharmaceutics)
Source: European Journal of Pharmaceutics and Biopharmaceutics - August 22, 2021 Category: Drugs & Pharmacology Authors: Qamar Abuhassan Ibrahim Khadra Kate Pyper Gavin W Halbert Source Type: research
Small scale in vitro method to determine a bioequivalent equilibrium solubility range for fasted human intestinal fluid
This study demonstrates that it is possible to assess the fasted intestinal equilibrium solubility envelope using a small number of bioequivalent media recipes obtained from a multi-dimensional analysis of fasted HIF. The derivation of the nine bioequivalent SIF media coupled with the lower measured solubility range indicate that the solubility results are more likely to reflect the fasted intestinal solubility envelope than previous DoE studies and highlight that intestinal solubility is a range and not a single value.PMID:34419602 | DOI:10.1016/j.ejpb.2021.08.002 (Source: European Journal of Pharmaceutics and Biopharmaceutics)
Source: European Journal of Pharmaceutics and Biopharmaceutics - August 22, 2021 Category: Drugs & Pharmacology Authors: Qamar Abuhassan Ibrahim Khadra Kate Pyper Gavin W Halbert Source Type: research
Appraisal of Felodipine nanocrystals for solubility enhancement and pharmacodynamic parameters on cadmium chloride induced hypertension in rats
CONCLUSION: The crystalline nature and improved solubility of FDP-NC improve the dissolution profile and pharmacodynamic data. The stability study data ensures that FDP-NC can be safely stored at 25℃. It is revealed that FDP-NC had a better release profile and improved pharmacodynamic effects as evident from better control over heart rate than FDP.PMID:34325637 | DOI:10.2174/1567201818666210729104351 (Source: Current Drug Delivery)
Source: Current Drug Delivery - July 30, 2021 Category: Drugs & Pharmacology Authors: Priyanka Maurya Pawan Pandey Samipta Singh Alka Sonkar Sonali Singh Shubhini Saraf Source Type: research
Appraisal of Felodipine nanocrystals for solubility enhancement and pharmacodynamic parameters on cadmium chloride induced hypertension in rats
CONCLUSION: The crystalline nature and improved solubility of FDP-NC improve the dissolution profile and pharmacodynamic data. The stability study data ensures that FDP-NC can be safely stored at 25℃. It is revealed that FDP-NC had a better release profile and improved pharmacodynamic effects as evident from better control over heart rate than FDP.PMID:34325637 | DOI:10.2174/1567201818666210729104351 (Source: Current Drug Delivery)
Source: Current Drug Delivery - July 30, 2021 Category: Drugs & Pharmacology Authors: Priyanka Maurya Pawan Pandey Samipta Singh Alka Sonkar Sonali Singh Shubhini Saraf Source Type: research
