Category: 72509-76-3

Boel, Eline published the artcileSolvent influence on manufacturability, phase behavior and morphology of amorphous solid dispersions prepared via bead coating, Related Products of pyridine-derivatives, the main research area is solvent manufacturability phase behavior morphol amorphous solid dispersion bead; Amorphous solid dispersion; Bead coating; Drug loading screening; Morphology; Solvent.

Bead coating or fluid-bed coating serves as an auspicious solvent-based amorphous solid dispersion (ASD) manufacturing technique in respect of minimization of potential phys. stability issues. However, the impact of solvent selection on the bead coating process and its resulting pellet formulation is, to the best of our knowledge, never investigated before. 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 Et acetate (EthAc). A drug loading screening approach with bead coating revealed analogus ability to manufacture high drug-loaded ASDs from the different organic solvents. The results show no correlation with crystallization tendency or with equilibrium solubility of the drug in the different solvents, nor with the solvent-dependent drug-polymer miscibility obtained from film casting experiments Distinct coating morphologies were however observed for PVP-VA and FEL-PVP-VA ASDs deposited onto beads from the various solvents, which is attributed to differences in solvent evaporation kinetics.

European Journal of Pharmaceutics and Biopharmaceutics published new progress about Coating materials. 72509-76-3 belongs to class pyridine-derivatives, name is 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C18H19Cl2NO4, Related Products of pyridine-derivatives.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Luczynska, Katarzyna published the artcileVibrational Response of Felodipine in the THz Domain: Optical and Neutron Spectroscopy Versus Plane-Wave DFT Modeling, Application In Synthesis of 72509-76-3, the main research area is felodipine plane wave DFT modeling optical neutron spectrum review.

We present a joint exptl. and computational terahertz (THz) spectroscopy study of the most stable polymorph (form I) of an antihypertensive pharmaceutical solid, felodipine (FLD). The vibrational response has been analyzed at room temperature by combining optical (THz-TDS, FT-IR, THz-Raman) and neutron (INS) terahertz spectroscopy. With the challenging example of a large and flexible mol. solid, we illustrate the complementarity of the exptl. techniques. We show how the results can be understood by employing ab initio modeling and discuss current progress in the field. To this end, we employ plane wave formulation of d. functional theory (plane wave DFT) along with harmonic lattice dynamics calculations (HLD) and ab initio mol. dynamics (AIMD) simulations. Based on a comprehensive theor. anal., we discover an inconsistency in the commonly accepted structural model, which can be linked to a distinct librational dynamics of the side ester chains. As a result, only a moderate agreement with the exptl. spectra can be achieved. We, therefore, propose an alternative structural model, effectively accounting for the influence of the large-amplitude librations and allowing for a comprehensive anal. of the vibrational resonances up to 4.5 THz. In that way, we illustrate the applicability of the computationally supported THz spectroscopy to detect subtle structural issues in mol. solids. While the provided structural model can be treated as a guess, the problem calls for further revision by means of high-resolution crystallog. The problem also draws a need of extending the THz experiments toward low-temperature conditions and single-crystal samples. On the other hand, the studied system emerges as a challenge for the DFT modeling, being extremely sensitive to the level of the theory used and the resulting description of the intermol. forces. FLD form I can be, hence, considered as a testbed for the use of more sophisticated theor. approaches, particularly relying on an advanced treatment of the van der Walls forces and going beyond zero-temperature conditions and harmonic approximation

Journal of Infrared, Millimeter, and Terahertz Waves published new progress about Crystal structure. 72509-76-3 belongs to class pyridine-derivatives, name is 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C18H19Cl2NO4, Application In Synthesis of 72509-76-3.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Zhang, Hongwei published the artcileThe preparation of felodipine/zein amorphous solid dispersions and in vitro evaluation using a dynamic gastrointestinal system, Application In Synthesis of 72509-76-3, the main research area is felodipine zein amorphous solid dispersion spray drying gastrointestinal system; TIM-1 model; Zein; amorphous solid dispersions; bioavailability; solid-state characterization; spray drying.

Felodipine has been widely used as a poorly water-soluble model drug for various studies to improve its oral bioavailability and in vivo efficacy. In this study, we developed amorphous solid dispersions (ASDs) via spray drying to enhance the bioavailability of felodipine through using natural zein protein as a novel polymeric excipient. The solid state characterization results demonstrated a single glass transition temperature (Tg) around 128.6°C and good phys. stability post 3 mo accelerated study under the condition of 40°C and 75% relative humidity (RH), which is possibly accounted for the mol. immobilization and hydrogen bonding interactions between felodipine and zein. By combining the in vitro dissolution study with TIM-1 gastrointestinal simulation investigation, it is indicated that felodipine was rapidly released from the ASD in 30 mins, and the supersaturation of felodipine was well maintained over 6 h, which resulted in a significant enhancement of felodipine bioavailability during simulated digestive processes in the upper GI tract. This study suggests that spray drying combined with natural excipient zein is an efficient formulation strategy for the development of ASDs with enhanced aqueous solubility and bioavailability.

Pharmaceutical Development and Technology published new progress about Crystal structure. 72509-76-3 belongs to class pyridine-derivatives, name is 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C18H19Cl2NO4, Application In Synthesis of 72509-76-3.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Cui, Haiming published the artcileThe effects of renin-angiotensin system inhibitors (RASI) in coronavirus disease (COVID-19) with hypertension: A retrospective, single-center trial, Safety of 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, the main research area is human covid19 renin angiotensin system inhibitor; Coronavirus disease 2019; Enfermedad Coronavirus 2019; Hipertensión; Hypertension; Renin-inhibidores del sistema de angiotensina; Renin–angiotensin system inhibitors.

A recent outbreak of coronavirus disease 2019 (COVID-19) occurs in the worldwide. Angiotensin-converting enzyme 2 (ACE2) can mediate coronavirus entry into host cells. Therefore, renin-angiotensin system inhibitors (RASI) were suspected of contributing to the increase of coronavirus infection. We aimed to analyze the effects of RASI in COVID-19 patients with hypertension.In this retrospective, single-center study, 27 COVID-19 patients with hypertension, who were admitted to the Shanghai Public Health Clin. Center from Jan. 25, 2020 to Jan. 31, 2020, were analyzed for clin. features, laboratory parameters, medications and the length of stay. All the patients were given antiviral and antihypertension treatment, of which 14 patients were treated with RASI and 13 patients without RASI. Comparing the two groups, we did not found statistically significant differences in clin. symptoms and laboratory tests. Furthermore, cough was not aggravated. Through the anal. of this small sample, RASI could be deemed safe and effective to control high blood pressure of COVID-19 patients. Further anal. with a larger sampling size is required to explore the underlying mechanisms.

Medicina Clinica published new progress about Antihypertensives. 72509-76-3 belongs to class pyridine-derivatives, name is 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C18H19Cl2NO4, Safety of 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

He, Fazhong published the artcileTRIB3 rs6037475 is a potential biomarker for predicting felodipine drug response in Chinese patients with hypertension, Formula: C18H19Cl2NO4, the main research area is felodipine hypertension biomarker Chinese; Tribbles homolog 3 (TRIB3); felodipine; hypertension; individualized drug therapy; pharmacogenetics.

Background: In this study, we aimed at exploring and validating the effect of TRIB3 polymorphism on antihypertensive drugs responses. Methods: A total of 830 hypertensive patients, who were administered with open-labeled hydrochlorothiazide (12.5 mg once daily) and randomly assigned to off-labeled felodipine (5 mg) or a matched placebo combination treatment (1:1), were selected from the Felodipine Event Reduction (FEVER) study. A strategy of screening 259 samples and validating the remaining 531 samples was implemented. Results: We found that TRIB3 rs6037475 CC genotype was associated with a reduction of diastolic blood pressure (DBP) (P=6.3×10-3) in the felodipine treatment group of screening set, and was also associated with a reduction of systolic blood pressure (SBP) (P=0.021), DBP (P=6.0×10-3) and mean arterial pressure (MAP) (P=0.021) in the felodipine treatment group of the validation set. Combined screening and validation set anal. found that patients with TRIB3 rs6037475 CC genotype had a significant higher mean SBP, DBP and MAP than those with TT genotype in the felodipine treatment group (CC vs. TT -10.2±0.74 vs. -17.8±0.21, P=7.8×10-3; -4.6±0.50 vs. -10.2±0.23, P=3.0×10-4; -6.5±0.54 vs. -12.7±0.14, P=3.0×10-4, resp.). Conclusions: These results suggest that TRIB3 rs6037475 genetic variation can be useful as a bio-marker for predicting felodipine drug response in Chinese patients with hypertension.

Annals of Translational Medicine published new progress about Antihypertensives. 72509-76-3 belongs to class pyridine-derivatives, name is 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C18H19Cl2NO4, Formula: C18H19Cl2NO4.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Kessing, Lars Vedel published the artcileAntihypertensive Drugs and Risk of Depression: A Nationwide Population-Based Study, Application In Synthesis of 72509-76-3, the main research area is population antihypertensive drug risk depression; antihypertensive agents; anxiety disorders; depressive disorder; diuretics; inflammation.

Hypertension, cardiovascular diseases, and cerebrovascular diseases are associated with an increased risk of depression, but it remains unclear whether treatment with antihypertensive agents decreases or increases this risk. The effects of individual drugs are also unknown. We used Danish population-based registers to systematically investigate whether the 41 most used individual antihypertensive drugs were associated with an altered risk of incident depression. Analyses of diuretics were included for comparisons. Participants were included in the study in Jan. 2005 and followed until Dec. 2015. Two different outcome measures were included: (1) a diagnosis of depressive disorder at a psychiatric hospital as an inpatient or outpatient and (2) a combined measure of a diagnosis of depression or use of antidepressants. Continued use of classes of angiotensin agents, calcium antagonists, and β-blockers was associated with significantly decreased rates of depression, whereas diuretic use was not. Individual drugs associated with decreased depression included 2 of 16 angiotensin agents: enalapril and ramipril; 3 of 10 calcium antagonists: amlodipine, verapamil, and verapamil combinations; and 4 of 15 β-blockers: propranolol, atenolol, bisoprolol, and carvedilol. No drug was associated with an increased risk of depression. In conclusion, real-life population-based data suggest a pos. effect of continued use of 9 individual antihypertensive agents. This evidence should be used in guiding prescriptions for patients at risk of developing depression including those with prior depression or anxiety and patients with a family history of depression.

Hypertension published new progress about Antihypertensives. 72509-76-3 belongs to class pyridine-derivatives, name is 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C18H19Cl2NO4, Application In Synthesis of 72509-76-3.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Fathima, Nazish published the artcilePrescribing pattern of drugs in the treatment of hypertension in a tertiary care teaching hospital: a prospective observational study, COA of Formula: C18H19Cl2NO4, the main research area is hypertension antihypertension morbidity combination therapy.

Hypertension is a common chronic medical condition which is identified as the 3rd leading risk factor for global burden of diseases. According to Joint National Committee guidelines, hypertension is defined as elevated systolic blood pressure of =140mmHg or diastolic blood pressure of �90mmHg. The objective of this study is to analyze the prescribing pattern associated with antihypertensives. A Prospective Observational study was carried out for a period of 6 mo in an inpatient department in Shamanur Shivashankarappa Institute of Medical Science and Research Center, a tertiary care teaching hospital, Davangere. The data was collected from case sheets of all inpatients taking at least one antihypertensive. A total of 150 prescriptions were analyzed, out of which, 88(58.66%) were males and 62(41.33%) were females. The mean age group of study population was found to be 60-80 years (52%). The most commonly reported co- morbidity along with hypertension was Diabetes mellitus 80 (53.33%). Monotherapy was most preferred therapy which was given in almost 76 (50.66%) followed by combination therapy. In monotherapy Calcium channel blockers 35(46.04%) was most commonly prescribed. The present study confirms that the Prescribing patterns of antihypertensive drugs were in concordance with joint national committee 8 guidelines for patients with different compelling indications. The most frequently prescribed class of drug as monotherapy was Calcium Channel Blockers, followed by diuretics, which was also the most commonly used class of drugs in combination therapy.

World Journal of Pharmaceutical Research published new progress about Antihypertensives. 72509-76-3 belongs to class pyridine-derivatives, name is 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C18H19Cl2NO4, COA of Formula: C18H19Cl2NO4.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Mizoguchi, Ryo published the artcileApplication of Co-Amorphous Technology for Improving the Physicochemical Properties of Amorphous Formulations, Recommanded Product: 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, the main research area is amorphous solid dispersion coamorhpous stability screening mixing enthalpy hygroscopicity; co-amorphous; hydrogen bonds; hygroscopicity; lipophilicity; mixing enthalpy; physical stability; screening.

Co-amorphous technol. was recently introduced to stabilize drugs in the amorphous state for drug development. We examined the predictability of the formation of co-amorphous systems and identified two reliable indicators of successful formation: (1) a neg. ΔHmix value and (2) small Δlog P between components. Moreover, we found that the stability of co-amorphous systems was improved when (1) ΔHmix was neg. and (2) amorphous forms of the constituent compounds were stable. Furthermore, we concluded that co-amorphous systems with small (neg. large) ΔHmix values had lower hygroscopicity. Typically, amorphous solid dispersions exhibit hygroscopicity because polymers exhibit large hygroscopicity. We proved the superiority of co-amorphous technol. over amorphous solid dispersion in this respect. Our results provide methods for (1) establishing a screening method and (2) improving hygroscopicity, which may make co-amorphous technol. more useful than amorphous solid dispersion technol.

Molecular Pharmaceutics published new progress about Amorphization (co). 72509-76-3 belongs to class pyridine-derivatives, name is 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C18H19Cl2NO4, Recommanded Product: 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Eid, Rania K. published the artcileEssential oils in niosomes for enhanced transdermal delivery of felodipine, COA of Formula: C18H19Cl2NO4, the main research area is felodipine essential oil niosome transdermal delivery; Lipid vesicles; dermal; eucalyptol; limonene; thermal analysis.

The fluidity of vesicular membrane affects vesicular transdermal drug delivery. Essential oils can be located in vesicular membrane imparting flexibility and influencing transdermal delivery. Accordingly, the objective was to investigate the effect of incorporation of essential oils in niosomes on felodipine transdermal delivery. Rigid niosomes comprising Span 60 with cholesterol (2:1, weight/weight) were used with clove, eucalyptus or lemon oils being incorporated in the vesicles at increasing concentrations The vesicle size and shape was monitored using SEM. Thermal anal. was used to monitor the thermal behavior. Drug entrapment efficiency, release and skin permeation were monitored. Niosomes were spherical with size ranging from 279 to 345 nm. The drug entrapment ranged from 97.9 to 98.8%. Thermal anal. confirmed the existence of oils within vesicular membrane and highlighted the membrane fluidizing effect. Drug release depended on the oil with clove oil or eucalyptus oil showing a trend of increased drug release compared with plain niosomes. In contrast, lemon oil reduced drug release rate. Skin permeation study reflected the superiority of oil containing niosomes. The results correlated with the fluidizing and penetration enhancing effects of oils. The study introduced essential oils as potential niosomes fluidizing agents for enhanced transdermal drug delivery.

Pharmaceutical Development and Technology published new progress about Behavior (thermal). 72509-76-3 belongs to class pyridine-derivatives, name is 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C18H19Cl2NO4, COA of Formula: C18H19Cl2NO4.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Patel, Nehanshu published the artcileComparative evaluation of different marketed brands of itraconazole, Formula: C18H19Cl2NO4, the main research area is itraconazole dissolution economic pharmaceutical analysis.

Efficacy of pharmaceutical dosage form generally depends on their formulation and manufacturing methods, hence it is likely that the quality of dosage form may vary. The free azole nitrogen competes for oxygen at the catalytic heme of cytochrome P 450 enzyme. Inhibition of cytochrome P 450 enzyme prevents the synthesis of ergosterolin fungal cell membranes by limiting the C14 demethylation of lanosterol, which is criticalfor the synthesis of ergosterol. The study was exclusively exptl. that used IP and otherstandard books to check in vitro quality of Itraconazole tablet using different anal. techniques and procedure. Test for weight variation, hardness, friability, disintegration time and dissolution were conducted. The dissolution test was performed at pH 6.8 for both brandsof the tablet. Further all the tablet passed weight variation, hardness, and friability and disintegration test as per the pharmacopoeial standard Hence we can conclude that both the brands of tablets are equal quantity of active pharmaceutical ingredient (API). Both the brands having higher and lower costs exert similar action.

World Journal of Pharmacy and Pharmaceutical Sciences published new progress about Cardiac arrhythmia. 72509-76-3 belongs to class pyridine-derivatives, name is 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C18H19Cl2NO4, Formula: C18H19Cl2NO4.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem