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Natural Product Research 2023The aim of the present study was to explore L. seed mucilage as a natural polymer in controlled release floating drug delivery system. First, seed mucilage was...
The aim of the present study was to explore L. seed mucilage as a natural polymer in controlled release floating drug delivery system. First, seed mucilage was extracted and evaluated for phytochemical screening, solubility studies, swelling index, viscosity and surface tension. Then, Atenolol floating systems were prepared with and without the L. seed mucilage by direct compression method. Phytochemical screening resulted from the presence of secondary metabolite carbohydrates, glycosides, flavonoids and phenolic compounds in good amounts. Results of hardness, friability, drug content and swelling index were satisfactory. The floating behaviour can increase the gastric residence time and eventually improve the bioavailability of the drug as evidence from buoyancy and dissolution studies. Interestingly, developed floating system showed remarkable increase in dissolution. Conclusively, the results suggest that developed Atenolol floating system with L. seed mucilage demonstrate interesting attributes to be explored for potential pharmaceutical application.
PubMed: 36308288
DOI: 10.1080/14786419.2022.2140154 -
Heliyon Dec 2023To determine the concentrations of nine drugs used in the treatment of cardiovascular diseases in human plasma through QuEChERS pre-treatment combined with...
To determine the concentrations of nine drugs used in the treatment of cardiovascular diseases in human plasma through QuEChERS pre-treatment combined with ultra-performance liquid chromatography-tandem mass spectrometry. Plasma samples were extracted with 3 mL of acetonitrile, 400 mg of anhydrous magnesium sulfate as a salting agent, and 20 mg of C18 as a sorbent. An Agilent Poroshell 120 EC-C18 column (4.6 × 100 mm, 2.7 μm) was selected and methanol-0.1 % water was used as the mobile phase, and ESI positive ion detection mode was selected. Results: The plasma concentrations of nisoldipine, metoprolol, and prazosin exhibited good linearity within the range of 0.05-4.0 ng/mL (r > 0.99), while atenolol, bisoprolol, propranolol, rosuvastatin, and atorvastatin showed linearity within the range of 0.5-40 ng/mL (r > 0.99). Fluvastatin showed good linearity within the range of 5.0-400 ng/mL. The accuracy of the method ranged from 94.15 to 110.62 %, while the recovery levels were in the range of 85.23 %-115.13 %. The matrix effects were observed between-6.54 % and 12.43 %. The intra-day and inter-day RSD was <15 % for the three concentrations of low, medium, and high. Conclusion The proposed method is rapid, accurate, specific, simple, reproducible, and suitable for the simultaneous measurement of the concentrations of nine drugs used in the treatment of cardiovascular diseases in human plasma.
PubMed: 38094060
DOI: 10.1016/j.heliyon.2023.e22543 -
Critical Care Explorations Sep 2023We aimed to 1) describe patterns of beta-blocker utilization among critically ill patients following moderate-severe traumatic brain injury (TBI) and 2) examine the...
Association of Early Beta-Blocker Exposure and Functional Outcomes in Critically Ill Patients With Moderate to Severe Traumatic Brain Injury: A Transforming Clinical Research and Knowledge in Traumatic Brain Injury Study.
OBJECTIVES
We aimed to 1) describe patterns of beta-blocker utilization among critically ill patients following moderate-severe traumatic brain injury (TBI) and 2) examine the association of early beta-blocker exposure with functional and clinical outcomes following injury.
DESIGN
Retrospective cohort study.
SETTING
ICUs at 18 level I, U.S. trauma centers in the Transforming Clinical Research and Knowledge in TBI (TRACK-TBI) study.
PATIENTS
Greater than or equal to 17 years enrolled in the TRACK-TBI study with moderate-severe TBI (Glasgow Coma Scale of <13) were admitted to the ICU after a blunt TBI.
INTERVENTIONS
None.
MEASUREMENTS
Primary exposure was a beta blocker during the first 7 days in the ICU, with a primary outcome of 6-month Glasgow Outcome Scale-Extended (GOSE). Secondary outcomes included: length of hospital stay, in-hospital mortality, 6-month and 12-month mortality, 12-month GOSE score, and 6-month and 12-month measures of disability, well-being, quality of life, and life satisfaction.
MAIN RESULTS
Of the 450 eligible participants, 57 (13%) received early beta blockers (BB group). The BB group was on average older, more likely to be on a preinjury beta blocker, and more likely to have a history of hypertension. In the BB group, 34 participants (60%) received metoprolol only, 19 participants (33%) received propranolol only, 3 participants (5%) received both, and 1 participant (2%) received atenolol only. In multivariable regression, there was no difference in the odds of a higher GOSE score at 6 months between the BB group and BB group (odds ratio = 0.86; 95% CI, 0.48-1.53). There was no association between BB exposure and secondary outcomes.
CONCLUSIONS
About one-sixth of subjects in our study received early beta blockers, and within this group, dose, and timing of beta-blocker administration varied substantially. No significant differences in GOSE score at 6 months were demonstrated, although our ability to draw conclusions is limited by overall low total doses administered compared with prior studies.
PubMed: 37693305
DOI: 10.1097/CCE.0000000000000958 -
Spectrochimica Acta. Part A, Molecular... Dec 2023Novel spectrophotometric and smartphone-based colorimetric methods were developed and validated for the estimation of atenolol (ATE) in pharmaceutical formulations. The...
Novel spectrophotometric and smartphone-based colorimetric methods were developed and validated for the estimation of atenolol (ATE) in pharmaceutical formulations. The measurement procedure is based on the de-diazotization reaction, in which ATE is able to inhibit the diazotized sulfanilic acid from reacting with 8-hydroxy quinoline (8-HQ) in a basic medium. As a result, the formation of red-orange color azo-dye is hindered, and the color intensity is decreased proportionally to concentration of ATE. In spectrophotometric method the azo-dye color fate was monitored at 495 nm. While in smartphone-based colorimetric (SBC) method the captured image in the design processed by RGB App and transferred to the absorbance. The reactant concentrations were optimized using a central composite design (CCD) and response surface method. The methods exhibit good linearity in the 8.0 to 60.0 µg mL range with no significant effect of interferences. The spectrophotometric method yields a linear equation with a slope of 0.0187 (R = 0.9993), a limit of detection (LOD) of 1.28 µg mL, and a limit of quantification (LOQ) of 4.28 µg mL. On the other hand, the smartphone-based colorimetric (SBC) method demonstrates a linear equation with a slope of 0.0127 (R = 0.9965), an LOD of 2.13 µg mL, and an LOQ of 7.09 µg mL. Analyzing ATE in pharmaceutical tablets was utilized to validate the applicability of the developed methods, and the results were statistically compared with those obtained by the HPLC method using the t-test and F-test.
Topics: Atenolol; Colorimetry; Drug Compounding; Smartphone; Tablets
PubMed: 37330334
DOI: 10.1016/j.saa.2023.123009 -
Life (Basel, Switzerland) Oct 20236-nitrodopamine released from rat isolated atria exerts positive chronotropic action, being more potent than noradrenaline, adrenaline, and dopamine. Here, we determined...
BACKGROUND
6-nitrodopamine released from rat isolated atria exerts positive chronotropic action, being more potent than noradrenaline, adrenaline, and dopamine. Here, we determined whether 6-nitrodopamine is released from rat isolated ventricles (RIV) and modulates heart inotropism.
METHODS
Catecholamines released from RIV were quantified by LC-MS/MS and their effects on heart inotropism were evaluated by measuring left ventricular developed pressure (LVDP) in Langendorff's preparation.
RESULTS
6-nitrodopamine was the major released catecholamine from RIV. Incubation with L-NAME (100 µM), but not with tetrodotoxin (1 µM), caused a significant reduction in 6-nitrodopamine basal release. 6-nitrodopamine release was significantly reduced in ventricles obtained from L-NAME chronically treated animals. 6-nitrodopamine (0.01 pmol) caused significant increases in LVDP and dP/dt, whereas dopamine and noradrenaline required 10 pmol, and adrenaline required 100 pmol, to induce similar increases in LVDP and dP/dt. The infusion of atenolol (10 nM) reduced basal LVDP and blocked the increases in LVDP induced by 6-ND (0.01 pmol), without affecting the increases in LVDP induced by 10 nmol of dopamine and noradrenaline and that induced by adrenaline (100 nmol).
CONCLUSIONS
6-nitrodopamine is the major catecholamine released from rat isolated ventricles. It is 1000 times more potent than dopamine and noradrenaline and is selectively blocked by atenolol, indicating that 6-ND is a main regulator of heart inotropism.
PubMed: 37895394
DOI: 10.3390/life13102012 -
Chemosphere Sep 2023In this study, the removal efficiency of chemicals of emerging concerns (CECs) was evaluated under exposure to various doses of UV/HO-based oxidation processes in...
In this study, the removal efficiency of chemicals of emerging concerns (CECs) was evaluated under exposure to various doses of UV/HO-based oxidation processes in combination with membrane filtration for three cleaning cycles. Polyethersulphone (PES) and polyvinylidene fluoride (PVDF) materials based membranes were used for this study. The chemical cleaning of the membranes was performed by immersion of the membranes into 1 N HCl followed by adding 3000 mg.L NaOCl for 1hr. Degradation and filtration performance was evaluated using Liquid Chromatography with tandem mass spectrometry (LC-MS/MS) and total organic carbon (TOC) analysis. Membrane fouling analysis for assessing the comparative performance of PES and PVDF membranes was determined by specific fouling and fouling indices evaluation. Membrane characterization results show that the alkynes and carbonyl group formation are due to dehydrofluorination and oxidation of PVDF and PES membranes under the attack of foulants and cleaning chemicals, which resulted in a reduction of fluoride percentage and an increase in sulfur percentage in the PVDF and PES membranes. A decrease in the hydrophilicity of the membranes in underexposed conditions was observed and is consistent with an increase in dose. Degradation results of CECs follow with the highest removal efficiency of chlortetracycline (CTC) followed by atenolol (ATL), acetaminophen (ACT), and caffeine (CAF) degradation due to attack on the aromatic ring and the carbonyl group of CECs by OH exposure. Membrane exposed at 3 mg.L-1 dose of UV/HO-based CECs shows minimum alteration with higher filtration efficiency and lower fouling, particularly in PES membranes.
Topics: Water; Chromatography, Liquid; Hydrogen Peroxide; Membranes, Artificial; Tandem Mass Spectrometry
PubMed: 37295688
DOI: 10.1016/j.chemosphere.2023.139096 -
International Journal of Molecular... Mar 2024()-Atenolol (()-2-(4-(2-Hydroxy-3-(isopropylamino)propoxy)phenyl)acetamide) has been synthesized in >99% enantiomeric excess () with the use of lipase B from Syncozymes...
()-Atenolol (()-2-(4-(2-Hydroxy-3-(isopropylamino)propoxy)phenyl)acetamide) has been synthesized in >99% enantiomeric excess () with the use of lipase B from Syncozymes (Shanghai, China), in a kinetic resolution of the corresponding racemic chlorohydrin. A catalytic amount of base was used in deprotonation of the phenol building block. The enantiopurity of the chlorohydrin building block remained unchanged upon subsequent amination to yield the final drug. All four steps in the synthesis protocol have been optimized compared to previously reported methods, which makes this new protocol more sustainable and in accordance with green chemistry principles. The overall yield of ()-atenolol was 9.9%, which will be further optimized.
Topics: Atenolol; China; Lipase; Fungal Proteins; Catalysis; Chlorohydrins; Stereoisomerism; Kinetics
PubMed: 38542467
DOI: 10.3390/ijms25063497 -
Environmental risk assessment of selected pharmaceuticals in hospital wastewater in nothern Vietnam.Chemosphere May 2024Pharmaceuticals are progressively employed in both human and veterinary medicine and increasingly recognized as environmental contaminants. This study investigated the...
Pharmaceuticals are progressively employed in both human and veterinary medicine and increasingly recognized as environmental contaminants. This study investigated the occurrence of selected pharmaceuticals in influent and effluent of wastewater treatment plants of 12 hospitals in Hanoi and 3 northern cities of Vietnam during dry and rainy seasons. In addition, environmental risk of pharmaceuticals in both hospital influents and effluents were evaluated based on risk quotients (RQs). Nine selected pharmaceutical compounds including sulfamethoxazole (SMX), naproxen (NPX), diclofenac (DCF), ibuprofen (IBU), acetaminophen (ACT), carbamazepine (CBM), iopromide (IOP), atenolol (ATN), and caffeine (CAF) were frequently detected in most influent and effluent wastewaters of 12 investigated hospitals. Detected compound levels exhibited a wide range, from as low as 1 ng/L for DCF to as high as 61,772 ng/L for ACT. Among these compounds, ACT, CAF, SMX, and IOP were consistently detected at substantial concentrations in both influents and effluents. This investigation also highlighted potential risks posed by SMX, ACT, and CAF residues present in influents and effluents of hospital wastewater treatment plants (WWTPs) to aquatic ecosystem. These finding are expected to provide scientific-based evidence for the development of hospital waste management and environmental management programs in Vietnam.
Topics: Wastewater; Vietnam; Water Pollutants, Chemical; Pharmaceutical Preparations; Hospitals; Risk Assessment; Environmental Monitoring; Waste Disposal, Fluid; Humans
PubMed: 38608777
DOI: 10.1016/j.chemosphere.2024.141973 -
Water Research Oct 2023Electrocatalytic oxidation is commonly restricted by low degradation efficiency, slow mass transfer, and high energy consumption. Herein, a synergetic electrocatalysis...
Electrocatalytic oxidation is commonly restricted by low degradation efficiency, slow mass transfer, and high energy consumption. Herein, a synergetic electrocatalysis system was developed for removal of various drugs, i.e., atenolol, florfenicol, and diclofenac sodium, as well as actual pharmaceutical wastewater, where the newly-designed single-atom Zr embedded TiO (Zr/TiO) and hierarchical CuFeO (CFO) microspheres were used as anode and microelectrodes, respectively. In the optimal reaction system, the degradation efficiencies of 40 mg L atenolol, florfenicol, and diclofenac sodium could achieve up to 98.8%, 93.4%, and 85.5% in 120 min with 0.1 g L CFO at current density of 25 mA cm. More importantly, in the flow-through reactor, the electrooxidation lasting for 150 min could reduce the COD of actual pharmaceutical wastewater from 432 to 88.6 mg L, with a lower energy consumption (25.67 kWh/m). Meanwhile, the electrooxidation system maintained superior stability and environmental adaptability. DFT theory calculations revealed that the excellent performance of this electrooxidation system could be ascribed to the striking features of the reduced reaction energy barrier by single-atom Zr loading and abundant oxygen vacancies on the Zr/TiO surface. Moreover, the characterization and experimental results demonstrated that the CFO unique hierarchical structure and synergistic effect between electrodes were also the important factors that could improve the system performance. The findings shed light on the single-atom material design for boosting electrochemical oxidation performance.
Topics: Wastewater; Titanium; Atenolol; Diclofenac; Water Pollutants, Chemical; Electrodes; Microelectrodes; Oxidation-Reduction; Pharmaceutical Preparations
PubMed: 37717331
DOI: 10.1016/j.watres.2023.120596 -
Current Drug Safety 2024Spasticity is a common sequelae of stroke, and often these patients receive anti-spastic drugs such as baclofen or tizanidine. Stroke patients have multiple... (Review)
Review
INTRODUCTION
Spasticity is a common sequelae of stroke, and often these patients receive anti-spastic drugs such as baclofen or tizanidine. Stroke patients have multiple co-morbidities such as hypertension, diabetes, and seizure. Tizanidine is an α2 and imidazole receptor agonist at a spinal and supraspinal level resulting in reduced central sympathetic outflow and causing hypotension rarely, especially in those receiving beta-blockers or angiotensin-converting enzyme inhibitors.
CASE PRESENTATION
We report a 56-year-old hypertensive male presenting with altered sensorium who had recurrent intracerebral hemorrhage with left spastic hemiplegia and focal seizures. He was on amlodipine, atenolol, telmisartan and oxcarbazepine. After 3 doses of tizanidine 2mg, his blood pressure dropped from 140/90 to 80/40 mmHg and pulse from 82 bpm to 44 bpm. His blood counts, serum chemistry, procalcitonin, and Trop I were normal. ECG revealed sinus bradycardia. After 8 hours of withdrawing tizanidine, his blood pressure became 110/70 mmHg, and on the next day, it became 140/82 mmHg. His attendants were taught physiotherapy to minimize spasticity.
CONCLUSION
This patient highlights the need for close monitoring of patients receiving tizanidine co-medication with angiotensin-converting enzyme inhibitors and angiotensin receptor blockers. These drugs have a synergistic effect on reducing the renin-angiotensin-aldosterone system, thereby hypotension and bradycardia.
Topics: Humans; Male; Middle Aged; Bradycardia; Hypotension, Controlled; Hypertension; Angiotensin-Converting Enzyme Inhibitors; Hypotension; Stroke; Seizures
PubMed: 37489780
DOI: 10.2174/1574886318666230725113855