Tag: M.W=350-400

Ge, Kai published the artcileNovel Computational Approach by Combining Machine Learning with Molecular Thermodynamics for Predicting Drug Solubility in Solvents, Formula: C18H19Cl2NO4, the main research area is antipyrine benzamide doxofylline gefitinib thermodn machine learning.

In this work, a novel strategy that combined mol. thermodn. and machine learning was proposed to accurately predict the solubility of drugs in various solvents. The strategy was based on 16 mol. descriptors representing drug-drug interactions and drug-solvent interactions including phys. parameters, pure perturbed-chain statistical associating fluid theory (PC-SAFT) parameters of drugs and solvents, and mixing rules. These mol. descriptors were inputted into five machine learning algorithms [multiple linear regression (MLR), artificial neural network (ANN), random forest (RF), extremely randomized trees (ET), and support vector machine (SVM)] to train the predictive model. A single-hidden-layer neural network was finally determined as the predictive model for predicting the solubility of drugs in various solvents. The drug solubility in the generalization evaluation set has also been successfully predicted, which indicates the good prediction performance of the model. Three directions for improving the model were summarized as adding mol. descriptors of drug-solvent interactions in the water system and drug-drug interactions in the organic solvent system and expanding the dataset to adequately obtain the features of multiple drugs. These findings show that the proposed model has the capability of solubility prediction, which is expected to provide important information for drug development and drug solvent screening.

Industrial & Engineering Chemistry Research published new progress about Drug discovery. 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

Achim, Marcela published the artcilePreparation and in vitro evaluation of felodipineloaded poly(ε-caprolactone) microspheres: quality by design approach, Category: pyridine-derivatives, the main research area is felodipine polycaprolactone microsphere polydispersity index drug development.

Felodipine was encapsulated into poly(ε-caprolactone) microspheres by the emulsion solvent evaporation method by employing the Quality by Design (QbD) strategy. Based on a risk anal., the influence of 4 critical process parameters (type of stirrer, stirring rate, shape of mixing vessel, aqueous phase volume) on the critical quality attributes of the microspheres (size, polydispersity, entrapment efficiency (EE)), was evaluated by a full factorial exptl. design. The microspheres’ morphol. and felodipine in vitro release were also studied. The particles’ size ranged between 39.8 and 302.5μm, and the polydispersity index varied from 0.279 to 0.517. Felodipine EE was above 93.59%. SEM (SEM) anal. revealed spherical particles, with imperfections and micropores on the surface. The microspheres exhibited an extended release of felodipine over a period of 12 h. In conclusion, the QbD approach helped understand the process parameters and their impact on the quality profile in the development of felodipine-loaded microspheres.

Farmacia (Bucharest, Romania) published new progress about Drug discovery. 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, Category: pyridine-derivatives.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Solomon, Samuel published the artcileInsights into the ameliorating ability of mesoporous silica in modulating drug release in ternary amorphous solid dispersion prepared by hot melt extrusion, HPLC of Formula: 72509-76-3, the main research area is mesoporous silica drug release solid dispersion hotmelt extrusion; Felodipine; Hotmelt Extrusion; Soluplus; Solvent less; Ternary dispersions.

In 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 phys. and chem. properties, release profiles of the prepared formulations and the surface concentrations of the various mol. species were investigated in detail. Formulations containing 25 wt% and 50 wt% of Felodipine demonstrated enhanced stability and solubility of the drug substance compared to its crystalline counterpart. Based on the Higuchi model, ternary formulations exhibited a 2-step or 3-step release pattern which can be ascribed to the release of drug mols. from the organic polymer matrix and the external silica surface, followed by a release from the silica pore structure. According to the Korsmeyer-Peppas model, the release rate and release mechanism are governed by a complex quasi-Fickian release mechanism, in which multiple release mechanisms are occurring concurrently and consequently. Stability studies indicated that after 6 mo storage of all formulation at 30% RH and 20°C, Felodipine in all formulations remained stable in its amorphous state except for the formulation comprised of 40 wt% Syloid AL-1FP with a 50 wt% drug load.

European Journal of Pharmaceutics and Biopharmaceutics published new progress about Drug 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, HPLC of Formula: 72509-76-3.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Sun, Lin published the artcileFelodipine-associated gingival overgrowth in a type 2 diabetic patient: a case report and literature review, Category: pyridine-derivatives, the main research area is type 2 diabetes gingival overgrowth felodipine; calcium channel blocker; drug-induced gingival overgrowth; felodipine.

Gingival overgrowth (GO) includes gingival enlargement and hyperplasia and may be induced by certain drugs, including calcium channel blockers (CCBs), particularly first-generation CCBs. However, to date, only few cases of GO induced by second- or third-generation CCBs have been reported. The present study reports on a case of a 48-yr-old diabetic male who was admitted to the First Hospital of Jilin University (Changchun, China) due to poor blood glucose control. This patient was diagnosed with GO. Review of the patient’s medical history revealed diagnoses of type 2 diabetes and hypertension, as well as the use of felodipine, a second-generation CCB, to control hypertension. The hypertensive drugs were replaced and the new drugs helped the patient control his blood glucose levels. Addnl., the patient was instructed on methods he could use to improve his oral hygiene, including rinsing of the teeth following each meal and increasing the frequency of tooth brushing per day. After 3 mo, the clin. symptoms of GO were relieved. The relevant literature was also reviewed to gain an improved understanding of the correlation between GO and CCBs, as well as diabetes and poor oral hygiene.

Experimental and Therapeutic Medicine published new progress about Adrenal gland. 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, Category: pyridine-derivatives.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Fu, Edouard L. published the artcileComparative Effectiveness of Renin-Angiotensin System Inhibitors and Calcium Channel Blockers in Individuals With Advanced CKD: A Nationwide Observational Cohort Study, Synthetic Route of 72509-76-3, the main research area is RAS inhibitor calcium channel blocker chronic kidney disease; Angiotensin-converting enzyme inhibitors (ACEi); CKD progression; advanced CKD; amlodipine; angiotensin receptor blockers (ARB); antihypertensive; calcium channel blockers (CCB); chronic kidney disease (CKD); comparative effectiveness; enalapril; end-stage kidney disease (ESKD); major adverse cardiovascular events (MACE); mortality; renoprotection.

It is unknown whether initiating renin-angiotensin system (RAS) inhibitor therapy in patients with advanced chronic kidney disease (CKD) is superior to alternative antihypertensive agents such as calcium channel blockers (CCBs). We compared the risks for kidney replacement therapy (KRT), mortality, and major adverse cardiovascular events (MACE) in patients with advanced CKD in routine nephrol. practice who were initiating either RAS inhibitor or CCB therapy. Observational study in the Swedish Renal Registry, 2007 to 2017.2,458 new users of RAS inhibitors and 2,345 CCB users with estimated glomerular filtration rates < 30 mL/min/1.73 m2 (CKD G4-G5 without KRT) who were being followed up by a nephrologist. As a pos. control cohort, new users of the same drugs with CKD G3 (estimated glomerular filtration rate, 30-60 mL/min/1.73 m2) were evaluated. RAS inhibitor vs. CCB therapy initiation. Initiation of KRT (maintenance dialysis or transplantation), all-cause mortality, and MACE (composite of cardiovascular death, myocardial infarction, or stroke). HRs with 95% CIs were estimated using propensity score-weighted Cox proportional hazards regression adjusting for demog., clin., and laboratory covariates. Median age was 74 years, 38% were women, and median follow-up was 4.1 years. After propensity score weighting, there was significantly lower risk for KRT after new use of RAS inhibitors compared with new use of CCBs (adjusted HR, 0.79 [95% CI, 0.69-0.89]) but similar risks for mortality (adjusted HR, 0.97 [95% CI, 0.88-1.07]) and MACE (adjusted HR, 1.00 [95% CI, 0.88-1.15]). Results were consistent across subgroups and in as-treated analyses. The pos. control cohort of patients with CKD G3 showed similar KRT risk reduction (adjusted HR, 0.67 [95% CI, 0.56-0.80]) with RAS inhibitor therapy compared with CCBs. Potential confounding by indication. Our findings provide evidence from real-world clin. practice that initiation of RAS inhibitor therapy compared with CCBs may confer kidney benefits among patients with advanced CKD, with similar cardiovascular protection. American Journal of Kidney Diseases published new progress about Aging, animal. 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

El Sayed, Mira published the artcileImpact of Simulated Intestinal Fluids on Dissolution, Solution Chemistry, and Membrane Transport of Amorphous Multidrug Formulations, Application In Synthesis of 72509-76-3, the main research area is multidrug formulation dissolution solubility membrane transport simulated intestinal fluid; FaSSIF; amorphous; fixed dose combination; flux; membrane transport; multidrug formulations; solubility; supersaturation.

The solution behavior and membrane transport of multidrug formulations were herein investigated in a biorelevant medium simulating fasted conditions. Amorphous multidrug formulations were prepared by the solvent evaporation method. Combinations of atazanavir (ATV) and ritonavir (RTV) and felodipine (FDN) and indapamide (IPM) were prepared and stabilized by a polymer for studying their dissolution (under non-sink conditions) and membrane transport in fasted state simulated intestinal fluid (FaSSIF). The micellar solubilization by FaSSIF enhanced the amorphous solubility of the drugs to different extents. Similar to buffer, the maximum achievable concentration of drugs in combination was reduced in FaSSIF, but the extent of reduction was affected by the degree of FaSSIF solubilization. Dissolution studies of ATV and IPM revealed that the amorphous solubility of these two drugs was not affected by FaSSIF solubilization. In contrast, RTV was significantly affected by FaSSIF solubilization with a 30% reduction in the maximum achievable concentration upon combination to ATV, compared to 50% reduction in buffer. This pos. deviation by FaSSIF solubilization was not reflected in the mass transport-time profiles. Interestingly, FDN concentrations remain constant until the amount of IPM added was over 1000 μg/mL. No decrease in the membrane transport of FDN was observed for a 1:1 M ratio of FDN-IPM combination. This study demonstrates the importance of studying amorphous multidrug formulations under physiol. relevant conditions to obtain insights into the performance of these formulations after oral administration.

Molecular Pharmaceutics published new progress about Amorphization. 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

Singh, Bharpoor published the artcileMouth dissolving tablets: an innovative deviation in drug delivery system, Recommanded Product: 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, the main research area is mouth dissolving tablet drug delivery system mental disability.

The main aim of novel drug delivery system is to develop a dosage form which is easy to administer, free from side effects, exhibit immediate release and offer enhanced bioavailability for better patient compliance. To achieve such results oral drug delivery system, preferably, tablets are the most widely accepted dosage forms which offer numerous advantages. Beside those advantages, Dysphagia is the most common disadvantage of conventional tablets which is associated with number of conditions like sudden exposure of allergies, mental disability, motion sickness, unconsciousness, unavailability of water etc. To get rid from these problems several innovative drug delivery systems have been developed like Mouth Dissolving Tablets (MDT′s) which dissolve in saliva within a few seconds, when put on tongue. These tablets can be administered anywhere and anytime, without the need of water and are thus quite suitable for children, elderly and mentally disabled patients.

Journal of Pharmaceutical Sciences and Research published new progress about AIDS (disease). 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

Guillemoto, Q. published the artcileTransfer of trace organic compounds in an operational soil-aquifer treatment system assessed through an intrinsic tracer test and transport modelling, Related Products of pyridine-derivatives, the main research area is trace organic compound transport modeling soil aquifer treatment system; Degradation; Reactive transport model; Soil-aquifer treatment; Sorption; Trace Organic Compounds.

Soil Aquifer Treatment (SAT) can provide supplementary treatment of trace organic compounds (TrOCs) such as pharmaceutical and industrial compounds present in Secondary Treated Wastewater (STWW). Concern on presence of unregulated TrOCs in natural systems has raised recently as well as the interest in SAT systems for remediation. The present study quantifies, at the field scale over35 m of lateral groundwater flow, the effectiveness of the Agon-Coutainville SAT system (Manche, Normandy, France) for TrOCs removal by sorption and biodegradation through monitoring of seven TrOCs (oxazepam, carbamazepine, benzotriazole, tolyltriazole, caffeine, paracetamol, ibuprofen) and major inorganic compounds as intrinsic tracers in STWW and groundwater during a 34-day STWW infiltration experiment during operational use of the SAT. Cationic exchanges and mixing between groundwater and STWW during the experiment were highlighted by major ions and geochem. simulations. Due to the low thickness of the unsaturated zone, a 1D anal. solution of the advection-dispersion equation (ADE) was applied on chloride data. Chloride was used as conservative intrinsic tracer to calibrate the horizontal flow and transport parameters such as the aquifer dispersion coefficient (D) and the average pore water velocity (ν) allowing estimation of the groundwater residence time. Transport and attenuation of the TrOCs were simulated assuming first-order degradation constant (μ) and linear retardation coefficient (R), calibrated to simulate the observed temporal changes in the breakthrough of TrOCs. Sorption was found to play a role in the transport of TrOCs, notably for oxazepam with a higher linear retardation coefficient value of 2.2, whereas no significant differences of retardation were observed for carbamazepine, tolyltriazole, benzotriazole (1.37, 1.35, 1.36 resp.). Estimated first order degradation rate constants, between 0.03d-1 for carbamazepine and 0.09d-1 for tolyltriazole, were generally high compared to the literature, possibly due to favorable redox conditions and important microbial activities within the system. This study provides evidence of the efficiency of the Agon-Coutainville SAT system for the removal of TrOCs.

Science of the Total Environment published new progress about Biodegradation. 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

Chen, Liuxi published the artcileEvaluation of polysaccharide-based chiral stationary phases in modern SFC-MS/MS for enantioselective bioanalysis., Product Details of C18H19Cl2NO4, the main research area is polysaccharide chiral stationary phase supercritical fluid chromatog mass spectrometry; supercritical fluid chromatog tandem mass spectrometry polysaccharide; SFC–MS/MS; chiral bioanalysis; chiral stationary phase; enantiomer; enantioselective bioanalysis; supercritical fluid chromatography.

Aim: The applicability of polysaccharide-based chiral stationary phases in modern supercritical fluid chromatog. (SFC)-MS/MS for chiral bioanal. was evaluated. Materials & methods: Ten popular polysaccharide-based chiral stationary phases (CSPs) were tested using a set of 23 drugs against three cosolvents. The effect of temperature and backpressure on separation was examined Results: The recommended order of CSPs for screening was determined Methanol with 0.1% NH4OH is proven to be the first choice of cosolvent. Temperature of 40°C and backpressure of 10 or 15 MPa are recommended starting conditions. Phospholipid elution profiles on the polysaccharide-based CSPs were reported for the first time under SFC conditions. Conclusion: A simplified screening protocol with straightforward method optimization approaches was generated for SFC chiral assay development in a reasonable time frame with a high success rate.

Bioanalysis published new progress about Blood analysis. 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, Product Details of C18H19Cl2NO4.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Agin, Fatma published the artcileElectroanalytical Methods for Determination of Calcium Channel Blockers, Application of 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, the main research area is review serum calcium channel blocker differential pulse voltammetry.

Background: Calcium Channel Blockers (CCBs) are widely used in the treatment of cardiovascular and ischemic heart diseases in recent years. They treat arrhythmias by reducing cardiac cycle contraction and also benefit ischemic heart diseases. Electroanal. methods are very powerful anal. methods used in the pharmaceutical industry because of the determination of therapeutic agents and/or their metabolites in clin. samples at extremely low concentrations (10-50 ng/mL). The purpose of this review is to gather electroanal. methods used for the determination of calcium channel blocker drugs in pharmaceutical dosage forms and biol. media selected mainly from current articles. Methods: This review mainly includes recent determination studies of calcium channel blockers by electroanal. methods from pharmaceutical dosage forms and biol. samples. The studies of calcium channel blockers electroanal. determination in the literature were reviewed and interpreted. Results: There are a lot of studies on amlodipine and nifedipine, but the number of studies on benidipine, cilnidipine, felodipine, isradipine, lercanidipine, lacidipine, levamlodipine, manidipine, nicardipine, nilvadipine, nimodipine, nisoldipine, nitrendipine, diltiazem, and verapamil are limited in the literature. In these studies, DPV and SWV are the most used methods. The other methods were used less for the determination of calcium channel blocker drugs. Conclusion: Electroanal. methods especially voltammetric methods supply reproducible and reliable results for the anal. of the analyte. These methods are simple, more sensitive, rapid and inexpensive compared to the usually used spectroscopic and chromatog. methods.

Current Analytical Chemistry published new progress about Blood analysis. 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 of 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem