Category: 72509-76-3

Han, Xiuyuan published the artcileEffect Of epigallocatechin-3-gallate on the pharmacokinetics of amlodipine in rats, Product Details of C18H19Cl2NO4, the main research area is liver microsome amlodipine EGCG pharmacokinetics; Drug–drug interaction; EGCG; LC-MS/MS; amlodipine; pharmacokinetics.

This study investigates the effect of epigallocatechin-3-gallate (EGCG), a major ingredient of green tea, on the pharmacokinetics of amlodipine in rats. The pharmacokinetics of orally administered amlodipine (1 mg/kg) with or without EGCG pretreatment (30 mg/kg/day for 10 days) were investigated. Plasma concentrations of amlodipine were determined by using a sensitive and reliable liquid chromatog. with tandem mass spectroscopy (LC-MS/MS) method. The effects of EGCG on the metabolic stability of amlodipine were investigated by using rat liver microsome incubation systems. The results indicated that when the rats were pretreated with EGCG, the Cmax of amlodipine increased from 16.32 ± 2.57 to 21.44 ± 3.56 ng/mL (p < 0.05), the Tmax decreased from 5.98 ± 1.25 to 4.01 ± 1.02 h (p < 0.05), and the AUC0-t increased from 258.12 ± 76.25 to 383.34 ± 86.95 mug h L-1 (p < 0.05), which suggested that the pharmacokinetic behavior of amlodipine was affected after oral co-administration of EGCG. Addnl., the metabolic half-life was prolonged from 31.3 ± 5.6 to 52.6 ± 7.9 min (p < 0.05) with the pretreatment of EGCG. It can be speculated that the drug-drug interaction between EGCG and amlodipine might occur, which might have resulted from the metabolism inhibition of amlodipine by EGCG when they were co-administered. Xenobiotica published new progress about Blood. 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

Jamei, Masoud published the artcileCurrent status and future opportunities for incorporation of dissolution data in PBPK modeling for pharmaceutical development and regulatory applications: OrBiTo consortium commentary, Application of 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, the main research area is pharmaceutical pharmacokinetics felodipine ibuprofen; Biorelevant dissolution; Dissolution; Oral drug absorption; PBBM (Physiologically Based Biopharmaceutical Model); PBPK.

In vitro dissolution experiments are used to qual. assess the impact of formulation composition and process changes on the drug dosage form performance. However, the use of dissolution data to quant. predict changes in the absorption profile remains limited. Physiol.-based Pharmacokinetic(s) (PBPK) models facilitate incorporation of in vitro dissolution experiments into mechanistic oral absorption models to predict in vivo oral formulation performance, and verify if the drug product dissolution method is biopredictive or clin. relevant. Nevertheless, a standardized approach for using dissolution data within PBPK models does not yet exist and the introduction of dissolution data in PBPK relies on a case by case approach which accommodates from differences in release mechanism and limitations to drug absorption. As part of the Innovative Medicines Initiative (IMI) Oral Biopharmaceutics Tools (OrBiTo) project a cross-work package was set up to gather a realistic understanding of various approaches used and their areas of applications. This paper presents the approaches shared by academic and industrial scientists through the OrBiTo project to integrate dissolution data within PBPK software to improve the prediction accuracy of oral formulations in vivo. Some general recommendations regarding current use and future improvements are also provided.

European Journal of Pharmaceutics and Biopharmaceutics published new progress about Cecum. 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

Locatelli, Marcello published the artcileFabric-Phase Sorptive Membrane Array As a Noninvasive In Vivo Sampling Device For Human Exposure To Different Compounds, Category: pyridine-derivatives, the main research area is fabric sorption membrane array human exposure sampling device.

This study introduces an innovative device for the noninvasive sampling and chromatog. anal. of different compounds present in exhaled breath aerosol (EBA). The new sampling device, especially in light of the recent COVID-19 pandemic that forced many countries to impose mandatory facemasks, allows an easy monitoring of the subject′s exposure to different compounds they may come in contact with, actively or passively. The project combines the advantages of a fabric-phase sorptive membrane (FPSM) as an in vivo sampling device with a validated LC-MS/MS screening procedure able to monitor more than 739 chems. with an overall anal. time of 18 min. The project involves the noninvasive in vivo sampling of the EBA using an FPSM array inserted inside an FFP2 mask. The study involved 15 healthy volunteers, and no restrictions were imposed during or prior to the sampling process regarding the consumption of drinks, food, or drugs. The FPSM array-LC-MS/MS approach allowed us to effectively exploit the advantages of the two complementary procedures (the convenient sampling by an FPSM array and the rapid anal. by LC-MS/MS), obtaining a powerful and green tool to carry out rapid screening analyses for human exposure to different compounds The flexible fabric substrate, the sponge-like porous architecture of the high-efficiency sol-gel sorbent coating, the availability of a large cache of sorbent coatings, including polar, nonpolar, mixed mode, and zwitterionic phases, the easy installation into the facemask, and the possibility of sampling without interrupting regular activities provide FPSMs unparalleled advantages over other sampling techniques, and their applications are expected to expand to many other clin. or toxicol. studies.

Analytical Chemistry (Washington, DC, United States) published new progress about Drugs. 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

Moreau, Magali published the artcileA baseline assessment of emerging organic contaminants in New Zealand groundwater, Product Details of C18H19Cl2NO4, the main research area is emerging organic contaminant baseline assessment groundwater pollution New Zealand; Emerging organic contaminant; Groundwater; Groundwater quality; Monitoring; New Zealand; Waikato region.

Emerging organic contaminants (EOC) are manufactured compounds, used for a variety of purposes, are a rising concern for freshwater quality and human and aquatic health. Their occurrence in groundwater was demonstrated in several international surveys. This work conducted the first baseline survey on EOC occurrence in New Zealand groundwater, using a wide-screening approach (723 compounds) and a novel stratified to mean residence time (MRT) randomized design to inform future monitoring. A total of 61 sites were sampled: 51 baseline sites from State of the Environment network in the Waikato region, and 10 targeted sites near known EOC sources for comparison. EOC were detected at 91% of baseline sites at concentrations of 0.1-11,000 ng/L. Multiple EOC groups were encountered: pesticides (48 compounds), pharmaceuticals (11), industrial (10), preservatives/food additives (3), and personal care products (1). Similar EOC diversity and concentration range were observed at targeted sites, with the addition of drugs of abuse and life-style compounds EOC detections occurred across young (1-11 yr. MRT), intermediate (11-50 yr. MRT), and old (50-250 yr. MRT) groundwater with higher concentrations and more types of EOC detected at sites with the youngest groundwater. Concentrations of 73 compounds detected at baseline sites were comparable to those observed in overseas groundwater, with 28 compounds measured at concentrations greater than the European Union maximum admissible concentration for pesticides. Survey results were used to: review current pesticide monitoring; propose complementary monitoring; identify potential EOC groundwater tracers; and identify compounds for which cost-effective, national laboratory capability is needed. Waikato survey results demonstrated ubiquitous occurrence of un-monitored, unregulated EOC in groundwater and limitations for using targeted approaches to establish monitoring.

Science of the Total Environment published new progress about Aquifers. 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

Wu, Haixi published the artcileCase report: concurrence of dermatomyositis and autoimmune blistering diseases: two case reports and a literature review, Recommanded Product: 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, the main research area is prednisone methotrexate minocycline halometasone dermatomyositis autoimmune blistering disease; autoimmune blistering disease; bullous dermatomyositis; clinically amyopathic dermatomyositis; dermatomyositis; interstitial lung disease; malignancy.

Dermatomyositis (DM) is an idiopathic inflammatory myopathy primarily involving skin and muscles. Clin. amyopathic dermatomyositis (CADM), a subset of DM, presents with characteristic cutaneous manifestations without clin. evidence of myositis. Although rare, vesiculobullous eruptions could develop in DM patients. Such ‘bullous DM’ is commonly considered a sign of internal malignancy. However, some cases with similar presentations were diagnosed as autoimmune blistering disease eventually. Herein, we reported two cases of CADM with autoimmune blisters formed. Case 1 presented with vesicles and was diagnosed with CADM initially. However, this patient developed blisters again years later and was diagnosed with ‘pemphigus foliaceous’ (PF) accordingly. Case 2, with a history of nasopharyngeal carcinoma and CADM, developed bullous pemphigoid several days after using a heat patch on her abdomen. The association between disease occurrence and local skin damage might provide more evidence to support the ‘epitope spreading’ hypothesis. Moreover, we reviewed related literature and discussed the differences between the two disease entities in clin. presentations, pathogenesis, therapy, and the risk of complications.

Frontiers in Immunology published new progress about Abdomen. 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

Salehi, Niloufar published the artcileHierarchical Mass Transfer Analysis of Drug Particle Dissolution, Highlighting the Hydrodynamics, pH, Particle Size, and Buffer Effects for the Dissolution of Ionizable and Nonionizable Drugs in a Compendial Dissolution Vessel, 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 particle pH dissolution; bicarbonate buffer; computer-aided drug design; dissolution; in vitro model; mathematical model; solubility.

Dissolution is a crucial process for the oral delivery of drug products. Before being absorbed through epithelial cell membranes to reach the systemic circulation, drugs must first dissolve in the human gastrointestinal (GI) tract. In vivo and in vitro dissolutions are complex because of their dependency upon the drug physicochem. properties, drug product, and GI physiol. properties. However, an understanding of this process is critical for the development of robust drug products. To enhance our understanding of in vivo and in vitro dissolutions, a hierarchical mass transfer (HMT) model was developed that considers the drug properties, GI fluid properties, and fluid hydrodynamics. The key drug properties include intrinsic solubility, acid/base character, pKa, particle size, and particle polydispersity. The GI fluid properties include bulk pH, buffer species concentration, fluid shear rate, and fluid convection. To corroborate the model, in vitro dissolution experiments were conducted in the USP (USP) 2 dissolution apparatus A weakly acidic (ibuprofen), a weakly basic (haloperidol), and a nonionizable (felodipine) drug were used to study the effects of the acid/base character, pKa, and intrinsic solubility on dissolution 900 mL of 5 mM bicarbonate and phosphate buffers at pH 6.5 and 37°C was used to study the impact of the buffer species on drug dissolution To investigate the impacts of fluid shear rate and convection, the apparatus was operated at different impeller rotational speeds. Moreover, presieved ibuprofen particles with different average diameters were used to investigate the effect of particle size on drug dissolution In vitro experiments demonstrate that the dissolution rates of both the ionizable compounds used in this study were slower in bicarbonate buffer than in phosphate buffer, with the same buffer concentration, because of the lower interfacial buffer capacity, a unique behavior of bicarbonate buffer. Therefore, using surrogates (i.e., 50 mM phosphate) for bicarbonate buffer for biorelevant in vitro dissolution testing may overestimate the in vivo dissolution rate for ionizable drugs. Model simulations demonstrated that, assuming a monodisperse particle size when modeling, dissolution may overestimate the dissolution rate for polydisperse particle size distributions. The hydrodynamic parameters (maximum shear rate and fluid velocity) under in vitro conditions in the USP 2 apparatus under different rotational speeds are orders of magnitude higher compared to the in vivo situation. The inconsistencies between the in vivo and in vitro drug dissolution hydrodynamic conditions may cause an overestimation of the dissolution rate under in vitro conditions. The in vitro dissolution data supported the accuracy of the HMT for drug dissolution This is the first drug dissolution model that incorporates the effect of the bulk pH and buffer concentration on the interfacial drug particle solubility of ionizable compounds, combined with the medium hydrodynamics effect (diffusion, convection, shear, and confinement components), and drug particle size distribution.

Molecular Pharmaceutics published new progress about Buffers. 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

Zadymova, Natalia M. published the artcileMicroemulsions and microheterogeneous microemulsion-based polymeric matrices for transdermal delivery of lipophilic drug (Felodipine), Application In Synthesis of 72509-76-3, the main research area is microemulsion polymeric matrix transdermal drug delivery felodipine.

Transdermal administration of drugs is more effective than traditional methods: metabolism of a drug in the gastrointestinal tract and liver is excluded, and its constant concentration in blood is provided. In most cases, the main part of the transdermal patch (TP) is a polymer film (matrix) with good adhesion to skin, which contains a skin permeability enhancer (SPE) and a drug. Types of TPs differ in a way of drug incorporating into the matrix. In this work, a new type of polymer matrixes for the delivery of lipophilic drugs based on microemulsions is developed. An optimized direct microemulsion (IV type according to Winsor) is obtained; practically, all its components are SPEs. Microemulsion (ME) type is confirmed by conductometry and dynamic light-scattering methods. Solubilization capacity of ME in relation to the antihypertensive drug felodipine (FEL) is studied. This drug is characterized by poor water solubility and, consequently, by low bioavailability at oral administration (âˆ?15%). FEL solubility in ME exceeds its solubility in water by 2.2 × 104 times. ME efficiency as a carrier of FEL is shown using Franz diffusion cell and UV spectroscopy. The FEL-loaded microemulsion was used as the dispersed phase of the emulsion, and the dispersion medium of the emulsion was a solution of polymer adhesive (a mixture of polyisobutylenes with different mol. weights and polybutene) in heptane with optimized rheol. properties. This emulsified ME (i.e., inverse emulsion) is served as a basis for the microheterogeneous polymer matrix, which provides FEL release at a constant target rate during the day.

Colloid and Polymer Science 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

Yin, Xuezhi published the artcileA Novel Micron-Size Particulate Formulation of Felodipine with Improved Release and Enhanced Oral Bioavailability Fabricated by Coaxial Electrospray, Formula: C18H19Cl2NO4, the main research area is felodipine coaxial electrospray povidone K30 HPMC; absorption; bioavailability; micron particles.

The antihypertensive drug felodipine (FD) is a typical biopharmaceutics classification system (BCS) II drug; thus, improving the dissolution rate of FD is very important to enhance its bioavailability. Besides, according to the in situ “”close loop”” perfusion assay, we found that the jejunum is the main absorptive site, then the duodenum and ileum. Consequently, a novel micron-size particulate of FD in a core-shell structure was fabricated by a coaxial electrospray technique; within the drug delivery system, Hypromellose K4M (HPMC K4M) was selected as a sheath material to prolong the retention time in the upper GI tract, while povidone K30 (PVP K30) was mixed with FD in the inner layer. The dissolution study in three different media (0.02% Tween-80 solution; phosphate buffer containing 0.02% Tween-80, pH 6.8; and HCl solution containing 0.02% Tween-80, pH 1.2) demonstrated that FD-loaded coaxial electrospray particles (F-COES) could greatly improve the dissolution of FD. Furthermore, in vivo pharmacokinetics revealed that F-COES emerged no changes in the half-life but significantly prolonged the tmax and increased the oral bioavailability. Collectively, this work supplies a promising drug release system that will improve the dissolution and enhance the bioavailability simultaneously for those poorly water-soluble drugs mainly absorbed in the upper GI tract.

AAPS PharmSciTech 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

He, Yingmeng published the artcileEnhanced Oral Bioavailability of Felodipine from Solid Lipid Nanoparticles Prepared Through Effervescent Dispersion Technique, Application of 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, the main research area is felodipine solid lipid nanoparticle delivery glyceryl behenate oral bioavailability; effervescent dispersion technique; felodipine; oral bioavailability; solid lipid nanoparticles.

Felodipine (FLD), a dihydropyridine calcium channel blocker with excellent antihypertensive effect, is poorly soluble and undergoes extensive hepatic metabolism, which lead to poor oral bioavailability (about 15%) and limit its clinic application. The goal of this study was to develop solid lipid nanoparticles (SLNs) loading FLD to improve the oral bioavailability. The FLD loaded solid lipid nanoparticles (FLD-SLNs) were prepared by the effervescent dispersion technique developed by our laboratory, which might have some advantages over traditional methods. The FLD-SLNs showed desired particle characteristics with particle size (198.15 ± 1.82 nm), poly dispersity index (0.26 ± 0.02), zeta-potential (- 25.53 ± 0.60 mV), entrapment efficiency (95.65 ± 0.70%), drug loading (2.33 ± 0.10%), and a spherical appearance. Pharmacokinetic results showed that the FLD-SLNs presented 3.17-fold increase in area under the curve (AUC(0-t)) compared with free FLD after oral administration in beagle dogs, which indicated that SLNs prepared using the effervescent dispersion technique can improve the bioavailability of lipophilic drugs like felodipine by enhancement of absorption and reduction first-pass metabolism

AAPS PharmSciTech 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 of 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Pyka-Pajak, Alina published the artcileComparison of the utility of RP-TLC technique and different computational methods to assess the lipophilicity of selected antiparasitic, antihypertensive, and anti-inflammatory drugs, Computed Properties of 72509-76-3, the main research area is antiparasitic anti inflammatory drug lipophilicity RP TLC technique; Ościk’s equation; Soczewiński–Wachtmeister’s equation; anti-inflammatory drugs; antihypertensive drugs; antiparasitic drugs; lipophilicity.

The aim of this study was to assess the lipophilicity of selected antiparasitic, antihypertensive and non-steroidal anti-inflammatory drugs (NSAIDs) by means of reversed phase-thin layer chromatog. (RP-TLC) as well by using Soczewinski-Wachtmeister’s and J. Oscik’s equations. The lipophilicity parameters of all examined compounds obtained under various chromatog. systems (i.e., methanol-water and acetone-water, resp.) and those determined on the basis of Soczewinski-Wachtmeister’s and Oscik’s equations (i.e., RMWS and RMWO) were compared with the theor. ones (e.g., AlogPs, AClogP, milogP, AlogP, MlogP, XlogP2, XlogP3) and the exptl. value of the partition coefficient (logPexp). It was found that the RMWS parameter may be a good alternative tool in describing the lipophilic nature of biol. active compounds with a high and low lipophilicity (i.e., antihypertensive and antiparasitic drugs). Meanwhile, the RMWO was more suitable for compounds with a medium lipophilicity (i.e., non-steroidal anti-inflammatory drugs). The chromatog. parameter f0(a) can be helpful for the prediction of partition coefficients, i.e., AClogP, XlogP3, as well as logPexp of examined compounds

Molecules 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, Computed Properties of 72509-76-3.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem