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

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

Solvent influence on manufacturability, phase behavior and morphology of amorphous solid dispersions prepared via bead coating
This study therefore aims to investigate the influence of the solvent on the bead coating process itself (i.e. manufacturability) and on solid-state characteristics of the resulting ASDs coated onto beads. For this purpose, the drug-polymer system felodipine (FEL)-poly(vinylpyrrolidone-co-vinyl acetate) (PVP-VA) was coated onto microcrystalline cellulose (MCC) beads from acetonitrile (ACN), methanol (MeOH), ethanol (EtOH), acetone (Ac), 2-propanol (PrOH), dichloromethane (DCM) and ethyl acetate (EthAc). A drug loading screening approach with bead coating revealed analogous ability to manufacture high drug-loaded ASDs from ...
Source: European Journal of Pharmaceutics and Biopharmaceutics - July 29, 2021 Category: Drugs & Pharmacology Authors: Eline Boel Flavia Giacomini Guy Van den Mooter Source Type: research

Solvent influence on manufacturability, phase behavior and morphology of amorphous solid dispersions prepared via bead coating
This study therefore aims to investigate the influence of the solvent on the bead coating process itself (i.e. manufacturability) and on solid-state characteristics of the resulting ASDs coated onto beads. For this purpose, the drug-polymer system felodipine (FEL)-poly(vinylpyrrolidone-co-vinyl acetate) (PVP-VA) was coated onto microcrystalline cellulose (MCC) beads from acetonitrile (ACN), methanol (MeOH), ethanol (EtOH), acetone (Ac), 2-propanol (PrOH), dichloromethane (DCM) and ethyl acetate (EthAc). A drug loading screening approach with bead coating revealed analogous ability to manufacture high drug-loaded ASDs from ...
Source: European Journal of Pharmaceutics and Biopharmaceutics - July 29, 2021 Category: Drugs & Pharmacology Authors: Eline Boel Flavia Giacomini Guy Van den Mooter Source Type: research

Model ‐based meta‐analysis of changes in circulatory system physiology in patients with chronic heart failure
AbstractTo characterize and compare various medicines for chronic heart failure (CHF), changes in circulatory physiological parameter during pharmacotherapy were investigated by a model-based meta-analysis (MBMA) of circulatory physiology. The clinical data from 61 studies mostly in patients with heart failure with reduced ejection fraction (HFrEF), reporting changes in heart rate, blood pressure, or ventricular volumes after treatment with carvedilol, metoprolol, bisoprolol, bucindolol, enalapril, aliskiren, or felodipine, were analyzed. Seven cardiac and vasculature function indices were estimated without invasive measur...
Source: CPT: Pharmacometrics and Systems Pharmacology - July 16, 2021 Category: Drugs & Pharmacology Authors: Ryota Takaoka, Yukako Soejima, Sayuri Guro, Hideki Yoshioka, Hiromi Sato, Hiroshi Suzuki, Akihiro Hisaka Tags: ARTICLE Source Type: research

Model ‐based meta‐analysis of changes in circulatory system physiology in patients with chronic heart failure: MBMA of circulatory system physiology in CHF
ABSTRACTTo characterize and compare various medicines for chronic heart failure (CHF), changes in circulatory physiological parameter during pharmacotherapy were investigated by a model-based meta-analysis (MBMA) of circulatory physiology. The clinical data from 61 studies mostly in HFrEF patients, reporting changes in heart rate, blood pressure, or ventricular volumes after treatment with carvedilol, metoprolol, bisoprolol, bucindolol, enalapril, aliskiren, or felodipine, were analyzed. Seven cardiac and vasculature function indices were estimated without invasive measurements using models based on appropriate assumptions...
Source: CPT: Pharmacometrics and Systems Pharmacology - July 6, 2021 Category: Drugs & Pharmacology Authors: Ryota Takaoka, Yukako Soejima, Sayuri Guro, Hideki Yoshioka, Hiromi Sato, Hiroshi Suzuki, Akihiro Hisaka Tags: ARTICLE Source Type: research

"Felodipine-indomethacin" co-amorphous supersaturating drug delivery systems: "Spring-parachute" process, stability, in vivo bioavailability, and underlying molecular mechanisms
Eur J Pharm Biopharm. 2021 Jun 10:S0939-6411(21)00169-7. doi: 10.1016/j.ejpb.2021.05.030. Online ahead of print.ABSTRACTAmorphous solid dispersions (ASD) are one of most commonly used supersaturating drug delivery systems (SDDS) to formulate insoluble active pharmaceutical ingredients. However, the development of polymer-guided stabilization of ASD systems faces many obstacles. To overcome these shortcomings, co-amorphous supersaturable formulations have emerged as an alternative formulation strategy for poorly soluble compounds. Noteworthily, current researches around co-amorphous system (CAS) are mostly focused on prepar...
Source: European Journal of Pharmaceutics and Biopharmaceutics - June 13, 2021 Category: Drugs & Pharmacology Authors: Ya-Wei Li Hong-Mei Zhang Bai-Ji Cui Cheng-Yi Hao He-Yun Zhu Jiao Guan Dan Wang Ying Jin Bo Feng Jian-Hui Cai Xian-Rong Qi Nian-Qiu Shi Source Type: research

"Felodipine-indomethacin" co-amorphous supersaturating drug delivery systems: "Spring-parachute" process, stability, in vivo bioavailability, and underlying molecular mechanisms
Eur J Pharm Biopharm. 2021 Jun 10:S0939-6411(21)00169-7. doi: 10.1016/j.ejpb.2021.05.030. Online ahead of print.ABSTRACTAmorphous solid dispersions (ASD) are one of most commonly used supersaturating drug delivery systems (SDDS) to formulate insoluble active pharmaceutical ingredients. However, the development of polymer-guided stabilization of ASD systems faces many obstacles. To overcome these shortcomings, co-amorphous supersaturable formulations have emerged as an alternative formulation strategy for poorly soluble compounds. Noteworthily, current researches around co-amorphous system (CAS) are mostly focused on prepar...
Source: European Journal of Pharmaceutics and Biopharmaceutics - June 13, 2021 Category: Drugs & Pharmacology Authors: Ya-Wei Li Hong-Mei Zhang Bai-Ji Cui Cheng-Yi Hao He-Yun Zhu Jiao Guan Dan Wang Ying Jin Bo Feng Jian-Hui Cai Xian-Rong Qi Nian-Qiu Shi Source Type: research

"Felodipine-indomethacin" co-amorphous supersaturating drug delivery systems: "Spring-parachute" process, stability, in vivo bioavailability, and underlying molecular mechanisms
Eur J Pharm Biopharm. 2021 Jun 10:S0939-6411(21)00169-7. doi: 10.1016/j.ejpb.2021.05.030. Online ahead of print.ABSTRACTAmorphous solid dispersions (ASD) are one of most commonly used supersaturating drug delivery systems (SDDS) to formulate insoluble active pharmaceutical ingredients. However, the development of polymer-guided stabilization of ASD systems faces many obstacles. To overcome these shortcomings, co-amorphous supersaturable formulations have emerged as an alternative formulation strategy for poorly soluble compounds. Noteworthily, current researches around co-amorphous system (CAS) are mostly focused on prepar...
Source: European Journal of Pharmaceutics and Biopharmaceutics - June 13, 2021 Category: Drugs & Pharmacology Authors: Ya-Wei Li Hong-Mei Zhang Bai-Ji Cui Cheng-Yi Hao He-Yun Zhu Jiao Guan Dan Wang Ying Jin Bo Feng Jian-Hui Cai Xian-Rong Qi Nian-Qiu Shi Source Type: research

Insights into the Ameliorating Ability of Mesoporous Silica in Modulating Drug Release in Ternary Amorphous Solid Dispersion Prepared by Hot Melt Extrusion
Eur J Pharm Biopharm. 2021 May 18:S0939-6411(21)00109-0. doi: 10.1016/j.ejpb.2021.04.017. Online ahead of print.ABSTRACTIn this work, the application of various mesoporous silica grades in the preparation of stabilized ternary amorphous solid dispersions of Felodipine using hot melt extrusion was explored. We have demonstrated the effectiveness of mesoporous silica in these dispersions without the need for any organic solvents i.e., no pre-loading or immersion steps required. The physical and chemical properties, release profiles of the prepared formulations and the surface concentrations of the various molecular species w...
Source: European Journal of Pharmaceutics and Biopharmaceutics - May 21, 2021 Category: Drugs & Pharmacology Authors: Samuel Solomon Javed Iqbal Ahmad B Albadarin Source Type: research

Insights into the Ameliorating Ability of Mesoporous Silica in Modulating Drug Release in Ternary Amorphous Solid Dispersion Prepared by Hot Melt Extrusion
Eur J Pharm Biopharm. 2021 May 18:S0939-6411(21)00109-0. doi: 10.1016/j.ejpb.2021.04.017. Online ahead of print.ABSTRACTIn this work, the application of various mesoporous silica grades in the preparation of stabilized ternary amorphous solid dispersions of Felodipine using hot melt extrusion was explored. We have demonstrated the effectiveness of mesoporous silica in these dispersions without the need for any organic solvents i.e., no pre-loading or immersion steps required. The physical and chemical properties, release profiles of the prepared formulations and the surface concentrations of the various molecular species w...
Source: European Journal of Pharmaceutics and Biopharmaceutics - May 21, 2021 Category: Drugs & Pharmacology Authors: Samuel Solomon Javed Iqbal Ahmad B Albadarin Source Type: research

Insights into the Ameliorating Ability of Mesoporous Silica in Modulating Drug Release in Ternary Amorphous Solid Dispersion Prepared by Hot Melt Extrusion
Eur J Pharm Biopharm. 2021 May 18:S0939-6411(21)00109-0. doi: 10.1016/j.ejpb.2021.04.017. Online ahead of print.ABSTRACTIn this work, the application of various mesoporous silica grades in the preparation of stabilized ternary amorphous solid dispersions of Felodipine using hot melt extrusion was explored. We have demonstrated the effectiveness of mesoporous silica in these dispersions without the need for any organic solvents i.e., no pre-loading or immersion steps required. The physical and chemical properties, release profiles of the prepared formulations and the surface concentrations of the various molecular species w...
Source: European Journal of Pharmaceutics and Biopharmaceutics - May 21, 2021 Category: Drugs & Pharmacology Authors: Samuel Solomon Javed Iqbal Ahmad B Albadarin Source Type: research

Identification of novel pregnane X receptor (PXR) agonists by In silico and biological activity analyses and reversal of cigarette smoke-induced PXR downregulation
Biochem Biophys Res Commun. 2021 Mar 30;555:1-6. doi: 10.1016/j.bbrc.2021.02.145. Online ahead of print.ABSTRACTCigarette smoke (CS) contains many toxins that collectively harm nearly every organ in the body, and smoking is a key risk factor for many chronic diseases. Aside from its toxic actions, CS may alter expression of the drug- and steroid-binding pregnane X receptor (PXR), which when activated upregulates expression of cytochrome P450 (CYP) enzymes, glutathione transferases (GSTs), and multidrug resistance protein 1 (MDR1), an adaptive metabolic array that mediates clearance of CS component toxins. We sought to iden...
Source: Biochemical and Biophysical Research communications - April 3, 2021 Category: Biochemistry Authors: Rajan T Reddy Toru Nyunoya Source Type: research