Tag: M.W=350-400

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

R., Hema published the artcileRole of coformers in solubility enhancement of poorly soluble drugs through cocrystallization: an overview, Recommanded Product: 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, the main research area is review coformer solubility soluble drug cocrystn.

Improving the solubility of poorly soluble pharmaceuticals is a key problem in the pharmaceutical industry, and it can be solved using a range of methods, such as particle size reduction, surface modification, and other procedures. Cocrystn. is a new method for enhancing solubility in the pharmaceutical industry, which can be done with the help of cocrystal former (Coformer). These are watersol. stoichiometric cocrystals of the active pharmaceutical ingredient (API) with water-soluble small mol. coformers such as ascorbic acid, Nicotinamide, etc. Selection of coformer is a principal challenge in evolution of cocrystals, which can be done by various approaches such as trial and error, supra mol. synthon, virtual screening, etc. Hydrogen bonding, halogen bonding, and π -π interactions all play a part in the development of cocrystals. Moisture absorption, cocrystal reactant dissolution, cocrystal nucleation, and growth are all factors that impact crystal formation. Cocrystals can be prepared by various methods such as Solution evaporation method, Solution cooling crystallization, Solid state grinding, Liquid assisted grinding method, Hot melt extrusion, etc. This review complies the various research works on cocrystals.

International Journal of Pharmaceutical Sciences Review and Research published new progress about Chemical stability. 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

Ou, Xiao published the artcileA general method for cultivating single crystals from melt microdroplets, Recommanded Product: 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, the main research area is pharmaceutical crystal microdroplet.

The cultivation of single crystals from solution is usually a time-consuming trial-and-error process. Here, we report a general strategy for rapidly cultivating single crystals from melt microdroplets within tens of minutes at the microgram scale. This strategy was successfully applied to the important polymorphic system griseofulvin to provide missing structural information of Form III, for which single crystals could not be cultivated from solution, as well as to twenty clin. drugs to verify its generality.

Chemical Communications (Cambridge, United Kingdom) published new progress about Crystal polymorphs. 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

Ali, K. A. published the artcileThe thermal analysis of felodipine and ramipril: application to quality control, Quality Control of 72509-76-3, the main research area is Triacor felodipine ramipril quality control thermogravimetry.

Thermal behavior of Felodipine (FEL) and Ramipril (RAM) drugs was studied in drug substance, binary mixture and co-formulated tablets. Some thermal anal. methods such as thermogravimetric anal. (TGA), derivative thermogravimetry (DrTGA), DTA (DTA) and differential scanning calorimetry (DSC) were used to investigate the thermal behavior of both drugs. The thermogravimetric data allowed the determination of different thermodn. and kinetic parameters such as: Ea, ΔH, ΔS and ΔG. The drugs purity was found to be 99.88% and 99.92% for FEL and RAM, resp. The simplicity, speed and low cost of the thermal anal. justify its application in the quality control of pharmaceutical drugs.

Analytical Chemistry: An Indian Journal published new progress about Activation energy. 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, Quality Control of 72509-76-3.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Meere, Martin published the artcileModelling phase separation in amorphous solid dispersions, Synthetic Route of 72509-76-3, the main research area is amorphous solid dispersion phase separation; Amorphous solid dispersion; Drug diffusion; Mathematical model; Phase separation.

Much work has been devoted to analyzing thermodn. models for solid dispersions with a view to identifying regions in the phase diagram where amorphous phase separation or drug recrystallization can occur. However, detailed partial differential equation non-equilibrium models that track the evolution of solid dispersions in time and space are lacking. Hence theor. predictions for the timescale over which phase separation occurs in a solid dispersion are not available. In this paper, we address some of these deficiencies by (i) constructing a general multicomponent diffusion model for a dissolving solid dispersion; (ii) specializing the model to a binary drug/polymer system in storage; (iii) deriving an effective concentration dependent drug diffusion coefficient for the binary system, thereby obtaining a theor. prediction for the timescale over which phase separation occurs; (iv) calculating the phase diagram for the Felodipine/HPMCAS system; and (iv) presenting a detailed numerical investigation of the Felodipine/HPMCAS system assuming a Flory-Huggins activity coefficient The numerical simulations exhibit numerous interesting phenomena, such as the formation of polymer droplets and strings, Ostwald ripening/coarsening, phase inversion, and droplet-to-string transitions. A numerical simulation of the fabrication process for a solid dispersion in a hot melt extruder was also presented. Solid dispersions are products that contain mixtures of drug and other materials e.g. polymer. These are liable to sep.-out over time – a phenomenon known as phase separation This means that it is possible the product differs both compositionally and structurally between the time of manufacture and the time it is taken by the patient, leading to poor bioavailability and so ultimately the shelf-life of the product has to be reduced. Theor. predictions for the timescale over which phase separation occurs are not currently available. Also lacking are detailed partial differential equation non-equilibrium models that track the evolution of solid dispersions in time and space. This study addresses these issues, before presenting a detailed investigation of a particular drug-polymer system.

Acta Biomaterialia published new progress about Amorphous 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, Synthetic Route of 72509-76-3.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem