Tag: M.W=350-400

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

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